A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS.
A family of hexahydropyridines.
Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS. They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR AGONISTS.
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.
A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.
OXAZINES with a fused BENZENE ring.
Amides composed of unsaturated aliphatic FATTY ACIDS linked with AMINES by an amide bond. They are most prominent in ASTERACEAE; PIPERACEAE; and RUTACEAE; and also found in ARISTOLOCHIACEAE; BRASSICACEAE; CONVOLVULACEAE; EUPHORBIACEAE; MENISPERMACEAE; POACEAE; and SOLANACEAE. They are recognized by their pungent taste and for causing numbing and salivation.
Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.
Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
GLYCEROL esterified with FATTY ACIDS.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Compound isolated from Cannabis sativa extract.
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
A physiologically inactive constituent of Cannabis sativa L.
The plant genus in the Cannabaceae plant family, Urticales order, Hamamelidae subclass. The flowering tops are called many slang terms including pot, marijuana, hashish, bhang, and ganja. The stem is an important source of hemp fiber.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
Agents inhibiting the effect of narcotics on the central nervous system.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
The observable response an animal makes to any situation.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
A subgroup of TRP cation channels named after vanilloid receptor. They are very sensitive to TEMPERATURE and hot spicy food and CAPSAICIN. They have the TRP domain and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold.
Phenomena and pharmaceutics of compounds that bind to the same receptor binding-site as an agonist (DRUG AGONISM) for that receptor but exerts the opposite pharmacological effect.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
An increased sensation of pain or discomfort produced by mimimally noxious stimuli due to damage to soft tissue containing NOCICEPTORS or injury to a peripheral nerve.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
Compounds based on benzene fused to oxole. They can be formed from methylated CATECHOLS such as EUGENOL.
Elements of limited time intervals, contributing to particular results or situations.
Use of electric potential or currents to elicit biological responses.
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.
The most common inhibitory neurotransmitter in the central nervous system.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
Six-carbon alicyclic hydrocarbons.
The physical activity of a human or an animal as a behavioral phenomenon.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Depolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during neurotransmission. Excitatory postsynaptic potentials can singly or in summation reach the trigger threshold for ACTION POTENTIALS.
Drugs capable of inducing illusions, hallucinations, delusions, paranoid ideations, and other alterations of mood and thinking. Despite the name, the feature that distinguishes these agents from other classes of drugs is their capacity to induce states of altered perception, thought, and feeling that are not experienced otherwise.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
The function of opposing or restraining the excitation of neurons or their target excitable cells.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.
Injections into the cerebral ventricles.
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.
One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.
Compounds with BENZENE fused to AZEPINES.
A group of compounds that contain the structure SO2NH2.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
The excessive use of marijuana with associated psychological symptoms and impairment in social or occupational functioning.
The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
Purine bases found in body tissues and fluids and in some plants.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills.
Administration of a drug or chemical by the individual under the direction of a physician. It includes administration clinically or experimentally, by human or animal.
Compounds that contain a BENZENE ring fused to a furan ring.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.
A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Scales, questionnaires, tests, and other methods used to assess pain severity and duration in patients or experimental animals to aid in diagnosis, therapy, and physiological studies.
Established cell cultures that have the potential to propagate indefinitely.
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS.
Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).
A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.
The motor activity of the GASTROINTESTINAL TRACT.
Central gray matter surrounding the CEREBRAL AQUEDUCT in the MESENCEPHALON. Physiologically it is probably involved in RAGE reactions, the LORDOSIS REFLEX; FEEDING responses, bladder tonus, and pain.
Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
A peptide, of about 33 amino acids, secreted by the upper INTESTINAL MUCOSA and also found in the central nervous system. It causes gallbladder contraction, release of pancreatic exocrine (or digestive) enzymes, and affects other gastrointestinal functions. Cholecystokinin may be the mediator of satiety.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
BENZOIC ACID amides.
Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.
A family of heterotrimeric GTP-binding protein alpha subunits that were originally identified by their ability to inhibit ADENYLYL CYCLASES. Members of this family can couple to beta and gamma G-protein subunits that activate POTASSIUM CHANNELS. The Gi-Go part of the name is also spelled Gi/Go.
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
A group of 16-carbon fatty acids that contain no double bonds.
Seven membered heterocyclic rings containing a NITROGEN atom.
A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
Almond-shaped group of basal nuclei anterior to the INFERIOR HORN OF THE LATERAL VENTRICLE of the TEMPORAL LOBE. The amygdala is part of the limbic system.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.
Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
An enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.
An outbred strain of rats developed in 1915 by crossing several Wistar Institute white females with a wild gray male. Inbred strains have been derived from this original outbred strain, including Long-Evans cinnamon rats (RATS, INBRED LEC) and Otsuka-Long-Evans-Tokushima Fatty rats (RATS, INBRED OLETF), which are models for Wilson's disease and non-insulin dependent diabetes mellitus, respectively.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
Learning situations in which the sequence responses of the subject are instrumental in producing reinforcement. When the correct response occurs, which involves the selection from among a repertoire of responses, the subject is immediately reinforced.
A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
A group of compounds that are derivatives of methoxybenzene and contain the general formula R-C7H7O.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
Drugs that bind to and activate excitatory amino acid receptors.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
A loosely defined grouping of drugs that have effects on psychological function. Here the psychotropic agents include the antidepressive agents, hallucinogens, and tranquilizing agents (including the antipsychotics and anti-anxiety agents).
Compounds with a BENZENE fused to IMIDAZOLES.
Amount of stimulation required before the sensation of pain is experienced.
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.
The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed)
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Product of the CANNABIS plant, CANNABINOIDS, or synthetic derivatives thereof, used in the treatment of a wide range of clinical symptoms.
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
The action of a drug in promoting or enhancing the effectiveness of another drug.

CB(1) cannabinoid receptor antagonism promotes remodeling and cannabinoid treatment prevents endothelial dysfunction and hypotension in rats with myocardial infarction. (1/155)

1. To study the long-term effects of altered cannabinoid receptor activity on myocardial and vascular function, Wistar rats were treated with the selective CB(1) antagonist AM-251 (0.5 mg kg(-1) d(-1)), the potent synthetic cannabinoid HU-210 (50 micro g kg(-1) d(-1)) or vehicle for 12 weeks after coronary artery ligation or sham operation. 2. AM-251 further reduced the pressure-generating capacity, shifted the pressure volume curve to the right (P<0.05) and increased the left-ventricular operating volume (AM-251: 930+/-40 micro l vs control: 820+/-40 micro l vs HU-210: 790+/-50 micro l; P<0.05) in rats with large myocardial infarction (MI). 3. Left-ventricular CB(1) immunoactivity in rats 12 weeks after large MI was unaltered as compared with noninfarcted hearts. 4. Cannabinoid receptor activation through HU-210, a cannabinoid that alters cardiovascular parameters via CB(1) receptors, increased the left-ventricular end-diastolic pressure (LVEDP, P<0.05). However, it prevented the drop in left-ventricular systolic pressure (HU-210: 142+/-5 mm Hg; P<0.05 vs control: 124+/-3 mm Hg; and P<0.001 vs AM-251: 114+/-3 mm Hg) and prevented endothelial dysfunction (ED) in aortic rings of rats with large MI (P<0.05). 5. Compared with AM-251, HU-210 prevented the decline in the maximal rate of rise of left-ventricular pressure and the maximum pressure-generating ability (P<0.05). In rats with small MI, HU-210 increased cardiac index (P<0.01) and lowered the total peripheral resistance (P<0.05). 6. The study shows that during the development of congestive heart failure post-large MI, cannabinoid treatment increases LVEDP and prevents hypotension and ED. Presumed CB(1) antagonism promotes remodeling despite unchanged myocardial CB(1) expression.  (+info)

Vasodilator actions of abnormal-cannabidiol in rat isolated small mesenteric artery. (2/155)

1. The nonpsychoactive cannabinoid abnormal-cannabidiol (trans-4-[3-methyl-6-(1-methylethenyl)-2-cyclohexen-1-yl]-5-pentyl-1,3-benzenedio l) (abn-cbd) produced concentration-dependent relaxation of methoxamine-precontracted rat small mesenteric artery. Endothelial removal reduced abn-cbd potency six-fold without affecting the maximum relaxation. 2. In endothelium-intact vessels, abn-cbd was less potent under 60 mM KCl-induced tone and inhibited by combination of L-N(G)-nitroarginine methyl ester (L-NAME) (nitric oxide synthase inhibitor; 300 micro M), apamin (small conductance Ca(2+)-activated K(+) channels inhibitor; 50 nM) and charybdotoxin (inhibitor of intermediate conductance Ca(2+)-activated K(+) channels and large conductance Ca(2+)-activated K(+) channels BK(Ca); 50 nM). L-NAME alone or in combination with either toxin alone had little effect. 3. In intact vessels, relaxations to abn-cbd were inhibited by SR 141716A (cannabinoid receptor antagonist; 1 or 3 micro M). Concomitant addition of L-NAME, apamin and charybdotoxin had no further effect. Other cannabinoid receptor antagonists either had little (SR 144528; 1 micro M and AM 251; 1 micro M) or no effect (AM 630; 10 micro M and AM 281; 1 micro M). Inhibition of gap junctions, G(i/o) protein coupling and protein kinase A also had no effect. 4. Endothelium-independent relaxation to abn-cbd was unaffected by L-NAME, apamin plus charybdotoxin or capsaicin (10 micro M). Abn-cbd inhibited CaCl(2)-induced contractions in vessels with depleted intracellular Ca(2+) stores and stimulated with methoxamine or KCl. This was insensitive to SR 141716A (3 micro M) but greatly reduced in vessels stimulated with ionomycin (Ca(2+) ionophore; 1 micro M). 5. We conclude that abn-cbd relaxes the rat small mesenteric artery by endothelium-dependent activation of K(+) channels via SR 141716A-sensitive pathways, which do not involve CB(1) and CB(2) receptors. It also causes endothelium-independent, SR 141716A-insensitive, relaxation by inhibiting Ca(2+) entry through voltage-gated Ca(2+) channels.  (+info)

Cannabinoid receptor-mediated regulation of intracellular calcium by delta(9)-tetrahydrocannabinol in resting T cells. (3/155)

Cannabinoids exhibit broad immune modulating activity by targeting many cell types within the immune system, including T cells, which exhibit sensitivity, as evidenced by altered activation, proliferation, and cytokine expression. As a result of the critical role calcium plays in T cell function coupled with previous findings demonstrating disruption of the calcium-regulated transcription factor, nuclear factor of activated T cells, by cannabinoid treatment, the objective of the present investigation was to perform an initial characterization of the role of the cannabinoid receptors in the regulation of the intracellular calcium concentration ([Ca(2+)](i)) by delta(9)-tetrahydrocannabinol (delta(9)-THC) in T lymphocytes. Here, we demonstrate that delta(9)-THC robustly elevates [Ca(2+)](i) in purified murine splenic T cells and in the human peripheral blood acute lymphoid leukemia (HPB-ALL) human T cell line but only minimally elevates [Ca(2+)](i) in Jurkat E6-1 (dysfunctional cannabinoid receptor 2-expressing) human T cells. Removal of extracellular calcium severely attenuated the delta(9)-THC-mediated rise in [Ca(2+)](i) in murine splenic T cells and HPB-ALL cells. Pretreatment with cannabinoid receptor antagonists, SR144528 and/or SR141716A, led to an attenuation of delta(9)-THC-mediated elevation in [Ca(2+)](i) in splenic T cells and HPB-ALL cells but not in Jurkat E6-1 cells. Furthermore, pretreatment of HPB-ALL cells with SR144528 antagonized the small rise in [Ca(2+)](i) elicited by delta(9)-THC in the absence of extracellular calcium. These findings suggest that delta(9)-THC induces an influx of extracellular calcium in resting T cells in a cannabinoid receptor-dependent manner.  (+info)

Endocannabinoid system modulates relapse to methamphetamine seeking: possible mediation by the arachidonic acid cascade. (4/155)

We clarified the modulating action of the endocannabinoid system, and its possible mediation by the arachidonic acid cascade, on the reinstatement of methamphetamine (METH)-seeking behavior, using the intravenous self-administration paradigm in rats. Following 12 days of self-administration of METH, the replacement of METH with saline resulted in a gradual decrease in lever press responses (extinction). Under extinction conditions, METH-priming or re-exposure to cues previously paired with METH infusion markedly increased the responses (reinstatement of drug-seeking). The cannabinoid CB1 receptor antagonist, SR141716A, blocked this behavior. Although the cannabinoid agonist, Delta8-tetrahydrocannabinol (THC), had no effects by itself, coadministration of the agonist and METH at small doses reinstated the drug-seeking behavior. THC attenuated the effects of the reinstatement-inducing dose of METH, but enhanced the effect of cues. Either given repeatedly during the extinction or singly, 24 h before the first METH-priming or cues challenge, THC suppressed the reinstatement. In another set of experiments, we found that diclofenac, a cyclooxygenase inhibitor, also attenuated the reinstatement induced by exposure to cues or drug-priming. These results suggest that the endocannabinoid system, through possible mediation by the arachidonic acid cascade, serves as a modulator of the reinstating effects of METH-priming and cues. Extending the current view on the treatment of drug dependence, these results indicate that endocannabinoid-activating substances as well as cyclooxygenase inhibitors may be promising as antirelapse agents.  (+info)

Central effects of the cannabinoid receptor agonist WIN55212-2 on respiratory and cardiovascular regulation in anaesthetised rats. (5/155)

1 The primary aim was to study the central respiratory effects of cannabinoids (CB). To this end, the cannabinoid receptor agonist WIN55212-2 was injected into the cisterna magna of urethane-anaesthetised rats and changes in respiratory parameters were observed. The secondary aim was to observe the centrally elicited cardiovascular actions of WIN55212-2. Involvement of opioid mechanisms in the central effects of WIN55212-2 was also studied. 2 Intracisternal (i.c.) application of WIN55212-2 (1, 3, 10 and 30 microg kg(-1)) dose-dependently decreased the respiratory rate and minute volume. Tidal volume was slightly increased, whereas peak inspiratory flow remained unchanged. In addition, WIN55212-2 increased mean arterial pressure and the plasma noradrenaline concentration and decreased heart rate. 3 I.c. injection of WIN55212-3 (1, 3, 10 and 30 microg kg(-1)), an enantiomer of WIN55212-2 lacking affinity for cannabinoid receptors, elicited no effects. All effects of WIN55212-2 were prevented by the CB1 receptor antagonist SR141716 (2 mg kg(-1) i.v.). I.c. administration of the opioid receptor agonist DAMGO (0.1, 0.3, 1 and 3 microg kg(-1)) markedly lowered the respiratory rate, tidal volume, minute volume and peak inspiratory flow. These effects were attenuated by the opioid receptor antagonist naloxone (0.2 mg kg(-1) i.v.). In contrast, naloxone did not affect the respiratory and cardiovascular effects of i.c. administered WIN55212-2. 4 Our results show that activation of CB1 cannabinoid receptors in the brain stem depresses respiration and enhances sympathetic tone and cardiac vagal tone. Opioid mechanisms are not involved in these central cannabinoid effects.  (+info)

The cannabinomimetic arachidonyl-2-chloroethylamide (ACEA) acts on capsaicin-sensitive TRPV1 receptors but not cannabinoid receptors in rat joints. (6/155)

The vasoactive effects of the synthetic cannabinoid (CB) arachidonyl-2-chloroethylamide (ACEA) was tested in the knee joints of urethane-anaesthetised rats. Experiments were also performed to determine whether these vasomotor responses could be blocked by the selective CB(1) receptor antagonists AM251 (N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole- 3-carboxamide) (10(-9) mol) and AM281 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-c arboxamide) (10(-8) mol), as well as the selective CB(2) receptor antagonist AM630 (6-iodo-2-methyl-1-[2-4(morpholinyl)ethyl]-[1H-indol-3-yl](4-methoxyphenyl)methan one) (10(-8) mol). Peripheral application of ACEA (10(-14)-10(-9) mol) onto the exposed surface of the knee joint capsule caused a dose-dependent increase in synovial blood flow. The dilator action of the CB occurred within 1 min after drug administration and rapidly returned to control levels shortly thereafter. The maximal vasodilator effect of ACEA corresponded to a 30% increase in articular perfusion compared to control levels. The hyperaemic action of ACEA was not significantly altered by coadministration of AM251, AM281 or AM630 (P>0.05; two-way ANOVA). The transient receptor potential channel vanilloid receptor 1 (TRPV(1)) antagonist capsazepine (10(-6) mol) significantly reduced the vasodilator effect of ACEA on joint blood vessels (P=0.002). Furthermore, destruction of unmyelinated and thinly myelinated joint sensory nerves by capsaicin (8-methyl-N-vanillyl-6-nonenamide) treatment also attenuated ACEA responses (P<0.0005). These data clearly demonstrate a vasodilator effect of the cannabinomimetic ACEA on knee joint perfusion. Rather than a classic CB receptor pathway, ACEA exerts its vasomotor influence by acting via TRPV(1) receptors located on the terminal branches of capsaicin-sensitive afferent nerves innervating the joint.  (+info)

Anandamide-induced cell death in primary neuronal cultures: role of calpain and caspase pathways. (7/155)

Anandamide (arachidonoylethanolamide or AEA) is an endocannabinoid that acts at vanilloid (VR1) as well as at cannabinoid (CB1/CB2) and NMDA receptors. Here, we show that AEA, in a dose-dependent manner, causes cell death in cultured rat cortical neurons and cerebellar granule cells. Inhibition of CB1, CB2, VR1 or NMDA receptors by selective antagonists did not reduce AEA neurotoxicity. Anandamide-induced neuronal cell loss was associated with increased intracellular Ca(2+), nuclear condensation and fragmentation, decreases in mitochondrial membrane potential, translocation of cytochrome c, and upregulation of caspase-3-like activity. However, caspase-3, caspase-8 or caspase-9 inhibitors, or blockade of protein synthesis by cycloheximide did not alter anandamide-related cell death. Moreover, AEA caused cell death in caspase-3-deficient MCF-7 cell line and showed similar cytotoxic effects in caspase-9 dominant-negative, caspase-8 dominant-negative or mock-transfected SH-SY5Y neuroblastoma cells. Anandamide upregulated calpain activity in cortical neurons, as revealed by alpha-spectrin cleavage, which was attenuated by the calpain inhibitor calpastatin. Calpain inhibition significantly limited anandamide-induced neuronal loss and associated cytochrome c release. These data indicate that AEA neurotoxicity appears not to be mediated by CB1, CB2, VR1 or NMDA receptors and suggest that calpain activation, rather than intrinsic or extrinsic caspase pathways, may play a critical role in anandamide-induced cell death.  (+info)

2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand, induces rapid actin polymerization in HL-60 cells differentiated into macrophage-like cells. (8/155)

Delta9-Tetrahydrocannabinol, a major psychoactive constituent of marijuana, interacts with specific receptors, i.e. the cannabinoid receptors, thereby eliciting a variety of pharmacological responses. To date, two types of cannabinoid receptors have been identified: the CB1 receptor, which is abundantly expressed in the nervous system, and the CB2 receptor, which is predominantly expressed in the immune system. Previously, we investigated in detail the structure-activity relationship of various cannabinoid receptor ligands and found that 2-AG (2-arachidonoylglycerol) is the most efficacious agonist. We have proposed that 2-AG is the true natural ligand for both the CB1 and CB2 receptors. Despite the potential physiological importance of 2-AG, not much information is available concerning its biological activities towards mammalian tissues and cells. In the present study, we examined the effect of 2-AG on morphology as well as the actin filament system in differentiated HL-60 cells, which express the CB2 receptor. We found that 2-AG induces rapid morphological changes such as the extension of pseudopods. We also found that it provokes a rapid actin polymerization in these cells. Actin polymerization induced by 2-AG was abolished when cells were treated with SR144528, a CB2 receptor antagonist, and pertussis toxin, suggesting that the response was mediated by the CB2 receptor and G(i/o). A phosphoinositide 3-kinase, Rho family small G-proteins and a tyrosine kinase were also suggested to be involved. Reorganization of the actin filament system is known to be indispensable for a variety of cellular events; it is possible that 2-AG plays physiologically essential roles in various inflammatory cells and immune-competent cells by inducing a rapid actin rearrangement.  (+info)

Kiefer F, Jahn H, Tarnasker T, Helwig H, Briken P, Holbach R, Kampf P, Stracke R, Baehr M, Naber D et al. (2003) Comparing and combining naltrexone and acamprosate in relapse prevention of alcoholism. A double-blind, placebo-controlled study. Arch Gen Psychiatry 60: 92-99PubMedCrossRefGoogle Scholar ...
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Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. Lifestyle, diabetes, and cardiovascular risk factors 10 years after bariatric surgery
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Not too long ago, a drug called rimonabant seemed to be just such a magic bullet. Rimonabant blocked the receptors in the body that are sensitive to cannabinoids like THC. There are two known varieties of cannabinoid receptors, by the way, CB1 and CB2, though they stand among other multi-purpose receptors that are sensitive to…
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Coconut Shrimp and Broccoli with Macadamia nuts Recipe. What do you mean you dont see it? Its right there! Christina shouted through the phone. I was driving along the crunchy, iced-over roads. The cars in front of me rolled along slowly, a quiet steam pouring from their tailpipes into the crisp, blue morning. I frantically scanned the horizon. A gentle sloping hill covered with naked, wiry trees obscured my view to the North. To the West the road was littered with condos, houses, and the occasional strip mall. To the South was a river, topped by bridges, which were lit up like runway strips that sloped upwards. To the East was our towering city, the one we had just left behind.. We had parted ways in the elevator, briefcases in hand, freshly dressed in business attire. The phone call in the car was to continue a conversation which had been interrupted when a couple of residents two floors down, dressed in pajamas and winter coats, entered the elevator.. Beautiful dog Christina said, to ...
GPR55 is a cell membrane receptor that was first identified in the brain in 1999. It was also cloned that year. By looking at the gene sequence, its physical structure, and the specific molecules that interacted with it, scientists began to speculate that it might be a cannabinoid receptor like CB1 and CB2. The majority of scientists working in this field now seem to feel that GPR55 is indeed a cannabinoid receptor, although there is not yet 100 percent agreement.. In December 2007, a team of Swedish scientists published their findings on GPR55 in the British Journal of Pharmacology. It was entitled, The orphan receptor GPR55 is a novel cannabinoid receptor. In that same issue of the British Journal of Pharmacology, a team of researchers from Scotland published their findings. This was entitled, GPR55: a new member of the cannabinoid receptor clan? These early papers on GPR55 caused quite a stir among their colleagues and pharmaceutical companies took special notice as well.. It was already ...
In a well-publicized article in the February 23, 2005 issue of the Journal of Neuroscience, researchers from Spain describe changes in cannabinoid receptors in the brains of AD patients, as well as animal behavioral and in-vitro data suggesting that cannabinoid agonists can protect neurons by reducing microglial activation.. The headlines on this study were predictably tantalizing (see, for example, Marijuana May Block Alzheimers), but also misleading. The mass media stories barely dug beyond the papers stated implication that marijuanas active ingredients could stem the progression of neurodegeneration. In reality, however, the story is more complicated and still unfolding. To begin with, two cannabinoid receptors have been identified. CB1 is the major type in brain, expressed by all types of nervous system cells, and apparently responsible for the psychoactive effects of the drug. CB2 is mainly expressed in immune system cells, but also in microglia (Benito et al., 2003), and may mediate ...
Just How Cannabinoid Receptors Unlock Relief Of Pain and much more Youve heard the narrative that is well-worn Cannabis and cannabinoids are bad for you
TY - CHAP. T1 - Cannabinoid receptors and their ligands in brain and other tissues. AU - Pertwee, Roger Guy. PY - 1999/4/5. Y1 - 1999/4/5. M3 - Chapter. SN - 089603593X. SN - 978-0896035935 SP - 177. EP - 185. BT - Marihuana and Medicine. A2 - Nahas, G.G.. A2 - Sutin, K.M.. A2 - Harvey , D.J.. A2 - Agurell, S.. PB - Humana Press. CY - Totowa, NJ, USA. ER - ...
References for Abcams Cannabinoid Receptor I peptide (320-334) (ab45820). Please let us know if you have used this product in your publication
Fingerprint Dive into the research topics of Cannabinoid receptor activation in the nucleus tractus solitaries produces baroreflex-like responses in the rat. Together they form a unique fingerprint. ...
This unit describes the use of cannabinoid radioligands in competitive binding assays for determining affinity parameters (IC50, Ki) of unlabeled compounds at transfected CB1 and CB2 receptors expressed in cell lines
This unit describes the use of cannabinoid radioligands in competitive binding assays for determining affinity parameters (IC50, Ki) of unlabeled compounds at transfected CB1 and CB2 receptors expressed in cell lines
Pharmaxis in Australia was actively engaged in a research programme focused on developing orally-available, synthetic selective cannabinoid receptor ligands,
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A detailed view of the primary molecule through which cannabinoids-the active compounds in marijuana-exert their effects on the brain could help guide the design of targeted medicines.
Inhibition of PARP1 leads to a huge enhance in DSBs and to mobile dying in the absence of BRCA1 or two and/or in the absence of HR dependent DSB fix. This is
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Cannabinoid receptor 2 antibody (cannabinoid receptor 2 (macrophage)) for FACS, ICC/IF, IHC-P, WB. Anti-Cannabinoid receptor 2 pAb (GTX23561) is tested in Human, Mouse, Rat samples. 100% Ab-Assurance.
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Research has consistently shown that people consider harmful side effects of an action more intentional than helpful side effects. This phenomenon is known as the side-effect effect (SEE), which refers to the influence of moral considerations in judgments of intentionality and other non-moral concepts. There is an ongoing debate about how to explain this asymmetric pattern of judgment and the psychological factors involved in it. It has been posited that affective reactions to agents that bring about harmful side-effects could bias intentionality attributions in these cases, explaining the asymmetric pattern of intentionality judgments that we observe in the SEE. We call this the affective bias hypothesis (ABH). Evidence for the ABH is mixed, with some findings suggesting a role for affective processes, while others suggesting that affective processes play no role in the SEE. A possible explanation for these apparently contradictory results points to affective processes involved in the SEE being
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chains in the Genus database with same CATH superfamily 4KYO B; 1QQE A; 2IFU A; 2L6J A; 4HOQ A; 5ARG A; 4AM9 A; 3MA5 A; 2XGO A; 5DIZ A; 5BW8 C; 2P58 C; 3LKU A; 5BT1 A; 3LY8 A; 3U4T A; 2J9Q A; 4UQX A; 2VQ2 A; 3Q47 B; 3CK7 A; 1NZN A; 4G2V A; 4I9E A; 5D0Q D; 2HYZ A; 4I2W A; 1A17 A; 1QZ2 A; 4W9R A; 3CK8 A; 4G23 A; 2E2E A; 3GZ2 A; 2UWJ G; 2KCV A; 3MV2 B; 5AYW D; 1WM5 A; 1KT1 A; 3CKB A; 3MV3 B; 4EQF A; 5CCL A; 2FI7 A; 3AS4 A; 5D0O D; 3RJV A; 5M72 A; 4YVQ C; 3LY9 A; 3RKV A; 2Y4U A; 4UI9 K; 4H7X A; 4JA9 A; 3CKC A; 5HI7 A; 3PE4 A; 5FT9 A; 2HR2 A; 5FZS A; 3JYS A; 4B94 A; 5KJL A; 1PC2 A; 2Y4T A; 2NC9 A; 4JL0 A; 4ME2 A; 4U04 A; 3FFL A; 3LCA A; 4JHR A; 4N3C A; 3ZGQ A; 3ASD A; 4ABN A; 1KT0 A; 1ZBP A; 3N71 A; 4YVO A; 4BWR A; 2XPI A; 4HOT A; 4GCO A; 4UQY A; 2GW1 A; 2YHC A; 3MEK A; 4N3B A; 2KAT A; 4I17 A; 2UY1 A; 4Y6C A; 5A7D B; 2HO1 A; 4N39 A; 4F3V A; 3EDT B; 2AVP A; 4HOR A; 5EX3 A; 3R9A B; 4WNG A; 4LEU A; 3RIB A; 3E4B A; 2VSN A; 2UY1 B; 1P5Q A; 5BNW A; 2FEZ A; 2QFC A; 4XIF A; 3UQ3 A; 3OXL A; 1NA0 A; 5JJ6 A; ...
What we need is 100% enthusiastic support for scientific progress, combined with a clear understanding of what progress would be and a firm grip on what is done. Do we want to lose our jobs, and to have a large part of our population unable to earn a living? If not, then robotics might not be progress. Do we want to increase the rate of cancer and obesity? If not, then a diet based overwhelmingly on processed food might not be progress.. There is no possibility of making good ethical choices today, because there is no shared ethic. Communitarianism presupposes such an ethic, and we are far from having one.. Meanwhile, a co-worker today handed me a small tract called, Dare the School Build a New Social Order? Stay tuned!. ...
The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene. It is closely related to the cannabinoid receptor type 1, which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol, the active agent in cannabis, and other phytocannabinoids (plant cannabinoids). The principal endogenous ligand for the CB2 receptor is 2-arachidonoylglycerol (2-AG). CB2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol. The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the immune system. ...
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis. - Mechanism of Action & Protocol.
© 2014 The Authors. The cannabinoid receptor 2 (CB2R) has been linked with the regulation of inflammation, and selective receptor activation has been proposed as a target for the treatment of a range of inflammatory diseases such as atherosclerosis and arthritis. In order to identify selective CB2R agonists with appropriate physicochemical and ADME properties for future evaluation in vivo, we first performed a ligand-based virtual screen. Subsequent medicinal chemistry optimisation studies led to the identification of a new class of selective CB2R agonists. Several examples showed high levels of activity (EC50 <200nM) and binding affinity (K i <200nM) for the CB2R, and no detectable activity at the CB1R. The most promising example, DIAS2, also showed favourable in vitro metabolic stability and absorption properties along with a clean selectivity profile when evaluated against a panel of GPCRs and kinases.
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Cannabinoids have long been known to have potent psychotropic actions, but their wide-ranging effects on the cardiovascular system are just beginning to be unraveled.. In anesthetized rat models, intravenously administered anandamide produces a triphasic hemodynamic response (28): a brief period of vagally mediated bradycardia and hypotension, followed by a transitory pressor reaction, and a relatively prolonged vasodepressor response. The latter is the dominant effect of anandamide in animal models, and it results from CB1-mediated inhibition of norepinephrine release from presynaptic nerve terminals (29). In humans, acute administration of the cannabinoids produces vasodilation and tachycardia with a variable net effect on systemic blood pressure (30), but long-term use of THC results in CB1-mediated hypotension and bradycardia (31,32).. Although CB1receptors are mostly expressed on the neuronal terminals, there is evidence showing that other cell types express these receptors and participate ...
The cannabinoid receptors are cells spread throughout your body and there are at least two types of receptors that work as part of your endocannabinoid
Rimonabant is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. It is an inverse agonist for the cannabinoid receptor CB1. Its main avenue of effect is reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States. This decision was made after a U.S. advisory panel recommended the medicine not be approved because it may increase suicidal thinking and depression.
Several 3-acylindoles with high affinity for the CB(2) cannabinoid receptor and selectivity over the CB(1) receptor have been prepared. A variety of 3-acyl substituents were investigated, and the tetramethylcyclopropyl group was found to lead to high affinity CB(2) agonists (5, 16). Substitution at …
TY - JOUR. T1 - Cannabinoid receptor 2 activation. T2 - A means to prevent monocyte-endothelium engagement. AU - Buch, Shilpa J.. PY - 2013/11. Y1 - 2013/11. UR - http://www.scopus.com/inward/record.url?scp=84886695905&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=84886695905&partnerID=8YFLogxK. U2 - 10.1016/j.ajpath.2013.08.003. DO - 10.1016/j.ajpath.2013.08.003. M3 - Comment/debate. C2 - 24055258. AN - SCOPUS:84886695905. VL - 183. SP - 1375. EP - 1377. JO - American Journal of Pathology. JF - American Journal of Pathology. SN - 0002-9440. IS - 5. ER - ...
The digestive, nervous, circulatory and respiratory system are some of the well-known systems in the body, but theres a lesser known yet still important system most people havent heard of, the endocannabinoid system. This recently discovered system plays a major role in many of the our bodily functions, and is only b
What Does The Endocannabinoid System Do? The bodies largest neurotransmitter system important in maintaining health. Regulating cell function for homeostasis.
Cannabinoid/Terpene Profile. Cannabinoid profiling during the growing stage enables the identification of plants that might have unique cannabinoid profiles of interest. These plants can provide growers with differentiated products and a competitive advantage in the market. Performing an analysis of compounds like cannabidiolic acid (CBDA) while a plant is still growing provides useful information for the optimization of growing conditions. Terpene profiling is also important as terpenes are primarily responsible for the taste and smell of cannabis. A terpene profile will provide further data in developing differentiated strains or products with optimum organoleptic qualities.. ...
Fenofibrate, a common treatment for high cholesterol, may stimulate the same receptors as cannabinoids, which could lead to a new class of drugs.
Ischemia-reperfusion injury (IRI) is a common cause of acute kidney injury (AKI), which is an increasing problem in the clinic and has been associated with increased rates of mortality. Currently, therapies to treat AKI are not available, so identification of new targets which, upon diagnosis of AKI, can be modulated to ameliorate renal damage is essential. In this study, a novel cannabinoid receptor 2 (CB2) agonist, SMM-295, was designed, synthesized, and tested in vitro and in silico. In vivo testing of the CB2 agonist was performed using a mouse model of bilateral IRI, which is a common model to mimic human AKI. Molecular docking of SMM-295 into a CB2 active-state homology model showed that SMM-295 interacts well with key amino acids to stabilize the active-state. In HEK-293 cells, SMM-295 was capable of reducing cAMP production with a 66-fold selectivity for the CB2 versus the cannabinoid receptor 1 (CB1), and dose-dependently increased MAPK and Akt phosphorylation. In mice, SMM-295 was ...
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The aim of this research project is to develop peripherally restricted cannabinoid receptor 1 (CB1R) antagonists for alcoholic steatosis. Alcohol abuse has detr...
With a clean and minimalist style, this print depicts the names and chemical structures of 20 different cannabinoid molecules including THC, CBD, CBC, etc.
NEW YORK, September 13, 2017 /PRNewswire/ -- Biosynthesis Technology Could Transform Cannabinoid Production. NetworkNewsWire Editorial Coverage.
Sanity Group puts people first to improve patient access and drive innovation, and utilises the health benefits of cannabinoid medicines.
Cannabinoids affect the receptor sites that comprise the endocannabinoid system, helping to body to achieve homeostasis in certain conditions.
In a well-publicized article in the February 23, 2005 issue of the Journal of Neuroscience, researchers from Spain describe changes in cannabinoid receptors in the brains of AD patients, as well as animal behavioral and in-vitro data suggest. ...
The endocannabinoid system regulates food intake, energy, and glucose metabolism at both central and peripheral levels. We have investigated the mechanism by which it may control glucose uptake in skeletal muscle cells. Detectable levels of the cannabinoid receptor type 1 (CB1) were revealed in L6 cells. Exposure of differentiated L6 myotubes to the CB1 antagonist rimonabant (SR141716) selectively increased 2-deoxyglucose uptake (2-DG) in a time- and dose-dependent manner. A similar effect was induced by genetic silencing of CB1 by small interfering RNA. Protein expression profiling revealed that both the regulatory p85 and the catalytic p110 subunits of the phosphatidylinositol-3-kinase (PI3K) were increased by SR141716. No significant change in the cellular content of other known molecules regulating PI3K was observed. However, phosphoinositide-dependent kinase-1, Akt/protein kinase B, and protein kinase Cζ activities were rapidly induced after SR141716 treatment of L6 cells in a ...
Our endocannabinoid system regulates balance in vital aspects of our biology. When our endocannabinoid system isnt signally and functioning optimally we can suffer from what is called Clinical Endocannabinoid Deficiency (CED).
The endocannabinoid system plays a crucial role in regulating emotionality and social behaviour, however it is unknown whether this system plays a role in symptoms associated with autism spectrum disorders. The current study evaluated if alterations in the endocannabinoid system accompany behavioura …
Cite this article as:. Mauro Maccarrone, Editorial [Hot Topic:The Endocannabinoid System in the Brain: From Biology to Therapy (Guest Editor: Mauro Maccarrone)], Current Drug Targets - CNS & Neurological Disorders (2005) 4: 613. https://doi.org/10.2174/156800705774933078 ...
Scientists are beginning to understand the role nutrition plays in keeping your endocannabinoid system healthy. SOL*CBD outlines ways to nurture ECS with diet!
A new study from the University of Texas M. D. Anderson Cancer Centre has shown that the cannabinoid cell surface receptor CB1 plays a key role in suppressing tumour growth in colorectal
Cannabinoids (CBs) implicate in a number of physiological and pathological mechanisms in the central nervous system. The cannabinoid receptor family consists of two GPCRs, cannabinoid receptor 1 (CB1) and cannabinoid…. Read More Read More. ...
Researchers report the love hormone, oxytocin, could enhance the pleasure of social interactions be stimulating the production of anandamide.... Read More... ...
The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details ...
A pentacyclic hybrid cannabinoid (4) has been synthesized, which combines structural elements of traditional cannabinoids and cannabmimetic indoles. Cannabinoid 4 contains a 1-pentylindole structure fused to the 2,3-positions of the partially reduced hydroxydibenzopyran system of THC. The successful approach to 4 employed 9-benzoyl-5,7-dimethoxy-1,2,3,4-tetrahydrocarbazole (17) as the starting material.
On these proscar warnings terminals, CB1 and CB2 cannabinoid receptors have been reported to inhibit nociceptive transmission, and both receptors seem to be acti- vated by an endogenous cannabinoid tone (37,51в53). T.
"Cannabinoid Receptor Agonists and Antagonists". Current Pharmaceutical Design. 1 (3): 343-352. v t e. ... WIN 54,461 (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2 ...
It is a tricyclic aryl derivative that acts as a competitive antagonist at the CB2 cannabinoid receptor. Its activity at CB1 ... WIN 55,212-2 WIN 55,225 Howlett AC, Berglund B, Melvin LS (October 1995). "Cannabinoid Receptor Agonists and Antagonists". ...
Discovery and development of Cannabinoid Receptor 1 Antagonists Lan R, Liu Q, Fan P, Lin S, Fernando SR, McCallion D, et al. ( ... AM-251 is structurally very close to rimonabant; both are biarylpyrazole cannabinoid receptor antagonists. In AM-251, the p- ... February 1999). "Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists". Journal of ... "AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies ...
Cahill, K; Ussher, MH (16 March 2011). "Cannabinoid type 1 receptor antagonists for smoking cessation". The Cochrane Database ... Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class. Rimonabant is ... Pi-Sunyer FX, Aronne LJ, Heshmati HM, Devin J, Rosenstock J (Feb 2006). "Effect of rimonabant, a cannabinoid-1 receptor blocker ... Fong TM, Heymsfield SB (September 2009). "Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action ...
Previously, rimonabant which is a cannabinoid type 1 receptor antagonist was used to help in quitting and to moderate the ... Cahill K, Ussher MH (March 2011). "Cannabinoid type 1 receptor antagonists for smoking cessation". The Cochrane Database of ... Jo YH, Talmage DA, Role LW (December 2002). "Nicotinic receptor-mediated effects on appetite and food intake". Journal of ... Retrieved 2011-02-21.CS1 maint: unfit URL (link) Lancaster T, Stead LF (2000). "Mecamylamine (a nicotine antagonist) for ...
Cannabinoid receptor antagonist Lange JH, Kruse CG (2008). "Cannabinoid CB1 receptor antagonists in therapeutic and structural ... Lee HK, Choi EB, Pak CS (2009). "The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as ... Reggio, Patricia H. (2009). "Toward the design of cannabinoid CB1 receptor inverse agonists and neutral antagonists". Drug ... Drinabant (INN; AVE-1625) is a drug that acts as a selective CB1 receptor antagonist, which was under investigation varyingly ...
Cannabinoid receptor antagonist Janero DR, Makriyannis A (March 2009). "Cannabinoid receptor antagonists: pharmacological ... Lee HK, Choi EB, Pak CS (2009). "The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as ... Rosonabant (INN; E-6776) is a drug acting as a CB1 receptor antagonist/inverse agonist that was under investigation by Esteve ... Development of the drug for clinical use was apparently halted shortly after the related CB1 antagonist rimonabant was ...
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... Griffin G, Wray EJ, Martin BR, Abood ME (October 1999). "Cannabinoid agonists and antagonists discriminated by receptor binding ... April 1999). "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of ... Pertwee RG, Fernando SR, Griffin G, Ryan W, Razdan RK, Compton DR, Martin BR (November 1996). "Agonist-antagonist ...
Discovery and development of Cannabinoid Receptor 1 Antagonists NESS-040C5 Ruiu S, Pinna GA, Marchese G, Mussinu JM, Saba P, ... July 2003). "Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor". The ... August 2002). "Design, synthesis and biological activity of rigid cannabinoid CB1 receptor antagonists". Chemical & ... It is much more potent an antagonist, and more selective for the CB1 receptor over CB2, than the more commonly used ligand ...
"Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum". British Journal of Pharmacology. 128 ... CP 55,244 is a chemical compound which is a cannabinoid receptor agonist. It has analgesic effects and is used in scientific ...
Griffin G, Wray EJ, Martin BR, Abood ME (October 1999). "Cannabinoid agonists and antagonists discriminated by receptor binding ... It is a partial agonist at the cannabinoid receptor CB1, producing a maximal stimulation of 58.3% with a Ki of 8.45nM. ... April 1999). "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of ... yne-delta8-tetrahydrocannabinol at cannabinoid receptors". British Journal of Pharmacology. 128 (3): 735-43. doi:10.1038/sj.bjp ...
Griffin G, Wray EJ, Martin BR, Abood ME (1999). "Cannabinoid agonists and antagonists discriminated by receptor binding in rat ... O-1125 (3-(1,1-dimethylhexyl-6-dimethylcarboxamide)-Δ8-tetrahydrocannabinol) is a research chemical which is a cannabinoid ...
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... Griffin G, Wray EJ, Martin BR, Abood ME (October 1999). "Cannabinoid agonists and antagonists discriminated by receptor binding ... April 1999). "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of ... O-806 is a drug which is a cannabinoid derivative that is used in scientific research. ...
Cannabinoid receptor antagonist Lange JH, Coolen HK, van Stuivenberg HH, Dijksman JA, Herremans AH, Ronken E, et al. (January ... November 2005). "Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity". ... a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition Tasks in ... a cannabinoid CB1 receptor antagonist, attenuates ethanol and nicotine seeking and improves inhibitory response control in rats ...
Cannabinoid receptor Synthetic cannabinoid Cannabinoid receptor antagonist George I. Papakostas; Maurizio Fava (2010). ... 323-. ISBN 978-981-4287-59-3. Bambico, Francis Rodriguez; Gobbi, Gabriella (2008). "The cannabinoid CB1 receptor and the ...
Cannabinoid receptor antagonist Kim MA, Yun H, Kwak H, Kim J, Lee J (2008). "Design, chemical synthesis, and biological ... a cannabinoid-1 receptor inverse agonist". Tetrahedron. 64 (48): 10802-10809. doi:10.1016/j.tet.2008.09.057. Woods SC (November ... Otenabant (CP-945,598) is a drug which acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the ...
Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N (August 2007). "NOP receptor antagonist, JTC-801, blocks cannabinoid- ... JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. This was the fourth opioid ... "Small-molecule agonists and antagonists of the opioid receptor-like receptor (ORL1, NOP): ligand-based analysis of structural ... October 2002). "Characterization of nociceptin/orphanin FQ-induced pain responses by the novel receptor antagonist N-(4-amino-2 ...
Investigational medications include cannabinoids and the 5-HT3 receptor antagonist tropisetron. Low-quality evidence found an ... A systematic review found most cytokines levels were similar in patients and controls, except for IL-1 receptor antagonist, IL- ... Späth M (May 2002). "Current experience with 5-HT3 receptor antagonists in fibromyalgia". Rheumatic Diseases Clinics of North ... Decreased binding of μ-opioid receptor have been observed; however, it is unknown if this is a result of increased endogenous ...
Griebel, G.; Stemmelin, J.; Scatton, B. (2005). "Effects of the cannabinoid CB1 receptor antagonist rimonabant in models of ... Donatti, A.F.; Leite-Panissi, C.R.A. (2011). "Activation of corticotropin-releasing factor receptors from the basolateral or ...
THCV is a cannabinoid receptor type 1 antagonist and cannabinoid receptor type 2 partial agonist. Δ9-THCV has also been shown ... "Synthetic and plant-derived cannabinoid receptor antagonists show hypophagic properties in fasted and non-fasted mice". British ... Pertwee RG (January 2008). "The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9- ... Cannabinoid Cannabis Cannabivarin (CBV) Federal Analogue Act Medical cannabis Parahexyl Rimonabant (synthetic CB1 antagonist) ...
Cannabinoid receptor antagonist O-1269 Rinaldi-Carmona M, Barth F, Congy C, Martinez S, Oustric D, Pério A, et al. (September ... Surinabant (SR147778) is a cannabinoid receptor type 1 antagonist developed by Sanofi-Aventis. It is being investigated as a ... Gessa GL, Serra S, Vacca G, Carai MA, Colombo G (2005). "Suppressing effect of the cannabinoid CB1 receptor antagonist, ... Doggrell SA (March 2005). "Will the new CB1 cannabinoid receptor antagonist SR-147778 have advantages over rimonabant?". Expert ...
... is a drug that is a classical cannabinoid derivative, which acts as an antagonist for the CB1 receptor. This gives it an ... 2010). "The cannabinoid 1-receptor silent antagonist O-2050 attenuates preference for high-fat diet and activated astrocytes in ... January 2011). "Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB(1) receptor antagonist". ... and locomotion by a putative cannabinoid receptor 'silent antagonist'". European Journal of Pharmacology. 530 (1-2): 103-6. doi ...
... cannabinoid receptor antagonist SR144528 decreases mu-opioid receptor expression and activation in mouse brainstem: role of CB( ... February 1998). "SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor". The Journal of ... February 1999). "SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist". The ... "Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB(2) receptor". ...
... has been reported to be a cannabinoid receptor antagonist, a cPLA2 inhibitor and a ceramide synthase inhibitor. It ... interact with the CB1 cannabinoid receptor". Molecular Pharmacology. 70 (1): 41-50. doi:10.1124/mol.105.020552. PMID 16571654. ... Hla T, Lee MJ, Ancellin N, Paik JH, Kluk MJ (November 2001). "Lysophospholipids--receptor revelations". Science. 294 (5548): ... Phospho-fingolimod causes the internalization of S1P receptors, which sequesters lymphocytes in lymph nodes, preventing them ...
The propyl analog, THCV, is a cannabinoid receptor type 1 and cannabinoid receptor type 2 antagonist, while THC is a CB1 ... "Evidence that the plant cannabinoid Delta9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist". British ... "Isolation of a High-Affinity Cannabinoid for the Human CB1 Receptor from a Medicinal Cannabis sativa Variety: Δ 9 - ... Δ9-THCB, showed an affinity for the human CB1 (Ki = 15 nM) and CB2 receptors (Ki = 51 nM) comparable to that of Δ9-THC. The ...
Altmann; J. Gertsch (2010). "Falcarinol is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in ... It was shown that falcarinol acts as a covalent cannabinoid receptor type 1 inverse agonist and blocks the effect of anandamide ...
... a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats". British Journal of Pharmacology. ... PSNCBAM-1 is a negative allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 ZCZ-011 German N, Decker AM, ... "Diarylureas as Allosteric Modulators of the Cannabinoid CB1 Receptor: Structure-Activity Relationship Studies on 1-(4- ...
Santucci V, Storme JJ, Soubrié P, Le Fur G (1996). "Arousal-enhancing properties of the CB1 cannabinoid receptor antagonist SR ... All effects were abolished by the CB1 antagonist AM251, supporting the conclusion that these effects were cannabinoid-receptor ... later it was found that the most important receptors are the PPAR-alpha receptor, the TRPV receptor and the GPR55 receptor. ... The cannabinoid receptors CB1 and CB2, two G protein-coupled receptors that are located in the central and peripheral nervous ...
... a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists". Journal of ... PSB-SB-487 is a coumarin derivative which is an antagonist at the former orphan receptor GPR55. Unlike older GPR55 antagonists ... However it has poorer selectivity over other related receptors, acting as a weak antagonist at CB1 with a Ki of 1170nM, and a ... "Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold". Journal of Medicinal Chemistry. 56 ( ...
The effects of betulinic acid as an anticancer agent in breast cancer is found to be cannabinoid receptor dependent. Betulinic ... acid behaves as a CB1 antagonist and CB2 agonist. Regarding the mode of action of betulinic acid, little is known about its ... "Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer ...
CB1 Agonists (Cannabinoids). Dronabinol • Nabilone • Nonabine. D2/D3 Antagonists. Alizapride • Bromopride • Chlorpromazine • ... Receptor. Ligands. Agonists. Adamantanes: Amantadine • Memantine • Rimantadine; Aminotetralins: 7-OH-DPAT • 8-OH-PBZI • ... Antagonists. Typical Antipsychotics: Acepromazine • Azaperone • Benperidol • Bromperidol • Clopenthixol • Chlorpromazine • ... 5-HT3 Antagonists. Alosetron • Azasetron • Bemesetron • Cilansetron • Clozapine • Dazopride • Dolasetron • Granisetron • ...
WO application 2006069196, Pace JM, Tietje K, Dart MJ, Meyer MD, "3-Cycloalkylcarbonyl indoles as cannabinoid receptor ligands ... antagonists/inverse. agonists/antibodies). *AM-251. *AM-281. *AM-630. *AM-1387 ... cannabinoid receptor activity". Journal of Medicinal Chemistry. 53 (1): 295-315. doi:10.1021/jm901214q. PMID 19921781.. .mw- ... This cannabinoid related article is a stub. You can help Wikipedia by expanding it.. *v ...
Cannabinoid receptor antagonists. *CCR5 receptor antagonists. *Neurokinin 1 receptor antagonists. *5-HT3 antagonists ... The GABAA receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... and sigma receptors.[18] The neurosteroid Progesterone (PROG) that activates progesterone receptors expressed in peripheral and ...
Cannabinoid receptor antagonist(英語:Cannabinoid receptor antagonist). *Endocannabinoid enhancer(英語:Endocannabinoid enhancer) ( ... Glutamate receptor antagonist(英語:Excitatory amino acid antagonist) (NMDA(英語:NMDA receptor antagonist)) ... Endothelin receptor antagonist(英語:Endothelin receptor antagonist). *NK1 receptor antagonist(英語:NK1 receptor antagonist) ... 血清素受體拮抗劑(英語:Serotonin antagonist) (5-HT3(英語:5-HT3
Antagonist: A drug with a fast association & slow dissociation. Induced-fitEdit. As a drug approaches a receptor, the receptor ... The anti-obesity drugs rimonabant and taranabant are inverse agonists at the cannabinoid CB1 receptor and though they produced ... GABA receptors: GABA-A, GABA-C. GABA. Cl− , HCO−3 [11]. Glutamate receptors: NMDA receptor, AMPA receptor, and Kainate receptor ... toll-like receptors (TLRs), killer activated and killer inhibitor receptors (KARs and KIRs), complement receptors, Fc receptors ...
transmembrane signaling receptor activity. • Wnt-activated receptor activity. • G-protein coupled receptor activity. ... "Purification and molecular cloning of a secreted, Frizzled-related antagonist of Wnt action". Proc. Natl. Acad. Sci. U.S.A. 94 ... "Frizzled Receptors: FZD5". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ...
Cannabinoid. receptor antagonists. *Drinabant§. *Ibipinabant§. *Otenabant§. *Rimonabant‡. *Rosonabant§. *Surinabant§. * ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ...
See also: Receptor/signaling modulators • Muscarinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... Antagonists. (and NAMs). *18-MAC. *18-MC. *α-Neurotoxins (e.g., α-bungarotoxin, α-cobratoxin, α-conotoxin, many others) ... A-366,833 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors selective for the ... "Central nicotinic receptors: structure, function, ligands, and therapeutic potential". ChemMedChem. 2 (6): 746-767. doi:10.1002 ...
Cannabinoid receptor. References[edit]. .mw-parser-output .reflist{font-size:90%;margin-bottom:0.5em;list-style-type:decimal}. ... Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor) ... "Identification of GPR55 as a lysophosphatidylinositol receptor". Biochemical and Biophysical Research Communications. 362 (4): ...
Cannabinoids (e.g., cannabis, dronabinol, nabilone). *NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone) ... σ receptors, IC50=145μM. Pharmacokinetics[edit]. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ... Braga MF, Aroniadou-Anderjaska V, Post RM, Li H (March 2002). "Lamotrigine reduces spontaneous and evoked GABAA receptor- ...
... dopamine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, and 5-HT (serotonin) antagonists. ... H2-receptor antagonists, cytoprotectants, prostaglandin analogues. *Lower digestive tract: laxatives, antispasmodics, ... Leukotriene antagonists For endocrine problemsEdit. androgens, antiandrogens, estrogens, gonadotropin, corticosteroids, human ... General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ...
... dependent modulation of type 1 cannabinoid receptors in nerve cells". Journal of Neuroscience Research. 81 (2): 275-283. doi: ... and as cholesterol-dependent modulation of CB1 cannabinoid receptors in nerve cells. The catalytic efficiency (i.e., the ratio ... "Regulation by cannabinoid receptors of anandamide transport across the blood-brain barrier and through other endothelial cells" ... whereas AMT activity instead is reduced by activation of the CB2 cannabinoid receptor, which inhibits NOS and NO release, also ...
NK1 receptor antagonist *Aprepitant (Emend) is a commercially available NK1 Receptor antagonist ... Some synthetic cannabinoids such as Nabilone (Cesamet) or the JWH series.. *Sativex is an oral spray containing THC and CBD. It ... 5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they ... chemotherapy as a single drug as well as with other antiemetics such as 5-HT3 receptor antagonists and NK1 receptor antagonist ...
Due to blockade of D2 receptors in the central nervous system, D2 receptor antagonists like metoclopramide can also produce a ... Domperidone is a peripherally selective dopamine D2 and D3 receptor antagonist.[7] It has no clinically significant interaction ... Domperidone, sold under the brand name Motilium among others, is a peripherally selective dopamine D2 receptor antagonist that ... Barone JA (1999). "Domperidone: a peripherally acting dopamine2-receptor antagonist". The Annals of Pharmacotherapy. 33 (4): ...
Differential response to a selective cannabinoid receptor antagonist (SR141716: rimonabant) in female mice from lines ...
Mathiesen O, Imbimbo BP, Hilsted KL, Fabbri L, Dahl JB (August 2006). "CHF3381, a N-methyl-D-aspartate receptor antagonist and ... August 2003). "Antinociceptive activity of the N-methyl-D-aspartate receptor antagonist N-(2-Indanyl)-glycinamide hydrochloride ... non-competitive NMDA receptor antagonist.[1][2][10] A pilot study of indantadol for chronic cough was initiated in October 2009 ... a putative N-methyl-D-aspartate receptor antagonist". NeuroReport. 13 (16): 2071-4. doi:10.1097/00001756-200211150-00016. PMID ...
These substances are neuroleptic and are either an antagonist of dopamine at the postsynaptic level at the D2 receptor site or ... designer cannabinoids. *4-HTMPIPO. *5F-AB-FUPPYCA. *5F-AB-PINACA. *5F-ADB ... Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, ... a 5-HT2A/2C antagonist.[15] The selectivity and affinity of ergolines for certain 5-HT receptors can be improved by introducing ...
... all of which are NMDA receptor antagonists that produce a dissociative state at high doses). A further class of pharmaceuticals ... synthetic cannabinoid HU-211 ingestion[14] and various other medical and recreational drugs (e.g. ketamine, PCP or ...
Adenosine receptors Receptor. Gene. Mechanism [15]. Effects. Agonists. Antagonists A1 ADORA1. Gi/o → cAMP↑/↓ *Inhibition *↓ ... The adenosine receptors (or P1 receptors[1]) are a class of purinergic G protein-coupled receptors with adenosine as the ... A2A adenosine receptor[edit]. Main article: Adenosine A2A receptor. As with the A1, the A2A receptors are believed to play a ... The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors ...
Cannabinoids (e.g., cannabis, dronabinol, nabilone). *NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone) ... Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors.[22] ... See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine ... In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ...
Partial agonist at the mu opioid receptor; agonist at delta opioid receptor; antagonist at kappa opioid receptor.. Sublingual, ... Cannabinoid receptor partial agonist.. PO.. Bioavailability = 10-20%; protein binding = 90-99%; volume of distribution = 10 L/ ... Full agonist at kappa opioid receptors, partial agonist/antagonist at the mu opioid receptors.[39]. IM, IV, SC.. Protein ... Kappa opioid receptor agonist; mu opioid receptor antagonist/partial agonist.. IM, IV, SC.. Bioavailability = 60-70%; protein ...
... but other drugs such as CB1 receptor antagonists exist in this class too.[25][26] Drugs used to treat sleep disorders such as ... as well as inhibit the inhibitory effect of adenosine receptors on dopamine receptors,[67] however the implications for humans ... Kamiya T, Saitoh O, Yoshioka K, Nakata H (June 2003). "Oligomerization of adenosine A2A and dopamine D2 receptors in living ... Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ...
Receptor/signaling modulators. Leukotriene signaling modulators. Nuclear receptor modulators. This drug article relating to the ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ...
... κ-opioid receptor agonist and μ-opioid receptor antagonist.[4][5][6] ... with opioid receptors". Research Communications in Chemical Pathology and Pharmacology. 48 (2): 173-81. PMID 2992058.. ... with opioid receptors in isolated guinea pig ileum and mouse vas deferens preparations]". Nihon Yakurigaku Zasshi. Folia ...
"Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ... Prostaglandin E2 receptor 4 (EP4). അവലംബം[തിരുത്തുക]. *↑ 1.0 1.1 1.2 GRCh38: Ensembl release 89: ENSG00000050628 - Ensembl, May ... "EP3-2 receptor mRNA expression is reduced and EP3-6 receptor mRNA expression is increased in gravid human myometrium". Journal ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Galanin receptor 1 (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.[5] ... "Galanin Receptors: GAL1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it. *v ...
decoy receptors[8] for VEGF-B and PIGF. Angiopoietin 2. antagonist of angiopoietin 1. ... Cannabinoids[edit]. According to a study published in the August 15, 2004 issue of the journal Cancer Research, cannabinoids, ... Lee, SJ.; Nathans, D. (Mar 1988). "Proliferin secreted by cultured cells binds to mannose 6-phosphate receptors". J Biol Chem. ... Bevacizumab (brand name Avastin) traps VEGF in the blood, lowering the binding of VEGF to its receptors. This results in ...
Similarly, the appetite suppressant rimonabant (a cannabinoid receptor antagonist) had to be withdrawn when it was linked with ... opioids and cannabinoids and their action receptors inside the brain, DA, muscarinic and MOR and CB1 receptors respectively.[11 ... such as the leptin receptor and the MC-4 receptor) or are still awaiting characterization - Prader-Willi syndrome - in addition ... Opioid receptor-related processes in the nucleus accumbens and ventral pallidum affect the palatability of foods.[10] ...
Receptor. (ligands). DP (D2). DP1. *Agonists: Prostaglandin D2. *Treprostinil ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ...
... aspirin is combined with an ADP receptor inhibitor, such as clopidogrel, prasugrel, or ticagrelor to prevent blood clots. This ... Vitamin K antagonists. (inhibit II, VII, IX, X). *Coumarins: Acenocoumarol. *Coumatetralyl. *Dicoumarol ... via the action on arachidonic acid and NMDA receptors cascade.[101] ... "Salicylate induces tinnitus through activation of cochlear NMDA receptors". The Journal of Neuroscience. 23 (9): 3944-52. PMID ...
A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of ... cannabinoid receptor 1 (CB1) and 2 (CB2). Both receptors are 7-transmembrane G-protein coupled receptors (GPCRs) which inhibit ... This revived the research on cannabinoid receptor antagonists which were expected to help answer these questions. The use of ... 1994), "SR141716A, a potent and selective antagonist of the brain cannabinoid receptor", FEBS Letters, 350 (2-3): 240-244, doi: ...
Serra S, Brunetti G, Pani M, Vacca G, Carai MAM, Gessa GL, Colombo G (2002) Blockade by the cannabinoid CB1 receptor antagonist ... Serra S, Carai MAM, Brunetti G, Gomez R, Melis S, Vacca G, Colombo G, Gessa GL (2001) The cannabinoid receptor antagonist SR ... Carai M.A., Lobina C., Gessa G.L., Colombo G. (2005) Cannabinoid receptor antagonists: a perspective. In: Spanagel R., Mann K.F ... Colombo G, Vacca G, Serra S, Carai MAM, Gessa GL (2004) Suppressing effect of the cannabinoid CB1 receptor antagonist, SR ...
Cannabinoid Receptor Antagonists. *N-(1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)-4-phenylpiperidin-4-yl) ... Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists.. Fulp A1, Bortoff K, Zhang Y, ... Cannabinoid receptor 1 (CB1) antagonists are potentially useful for the treatment of several diseases. However, clinical ... Even though otenabant penetrates the CNS, it is unique among CB1 antagonists that have been clinically tested because it has ...
This impairment was blocked by AM251, a cannabinoid CB1 receptor antagonist, administered 30 min before the training trial or ... On the 7th day of withdrawal, a novel object recognition task was performed and the amount of cannabinoid CB1 receptor protein ... On the other hand, cannabinoid CB1 receptors have been implicated in learning/memory, and are highly expressed in the ... At this time, the level of cannabinoid CB1 receptor protein increased significantly in the hippocampus but not the prefrontal ...
This compound displays nanomolar affinity for the central cannabinoid receptor but is not active on the peripheral cannabinoid ... receptor. In vitro, SR141716A antagonises the inhibitory effects of cannabin … ... SR141716A is the first selective and orally active antagonist of the brain cannabinoid receptor. ... SR141716A, a potent and selective antagonist of the brain cannabinoid receptor FEBS Lett. 1994 Aug 22;350(2-3):240-4. doi: ...
However, neutral antagonists or CNS-sparing peripherally restricted antagonists of CB1R may be useful for ALD as these ... Past reports suggest that antagonism of the CB1 receptor (CB1R) is an emerging strategy to alcoholic liver disease. ... Inhibition of alcoholic steatosis by a type 1 cannabinoid receptor antagonist ESBRA 2015 Meeting Abstract P-16. ... Inhibition of alcoholic steatosis by a type 1 cannabinoid receptor antagonist: ESBRA 2015 Meeting Abstract P-16. Alcohol and ...
The present invention relates to a method to identify a true antagonist and an inverse agonist of a cannabinoid receptor (CB), ... In a further embodiment the cannabinoid receptor is CB1 or CB2. In a further embodiment the cannabinoid receptor is CB1 wherein ... As used herein, "CB receptor" refers to CB1 and CB2 receptors and any other member of the cannabinoid receptor family. Also ... However, the choice of the most effective CB receptor antagonist is complicated because CB receptor antagonists can exhibit a ...
Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Download Prime PubMed App to iPhone, iPad, ... AnimalsCHO CellsCannabinoid Receptor AntagonistsCricetinaeCricetulusIndolesMiceMice, 129 StrainMice, KnockoutPiperidines ... Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons.. Neuropharmacology. 2011 Sep; 61(4):778-88. ... Cannabinoid receptor antagonists have been utilized extensively in vivo as well as in vitro, but their selectivity has not been ...
... a pyrazole derivative with high affinity for rat and human CB1 cannabinoid receptors, has recently been reported to reverse ... Effects of the cannabinoid CB1 receptor antagonist SR141716A on the behavior of pigeons and rats. ... a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 350:240-244Google Scholar ... Physical withdrawal in rats tolerant to Δ9-tetrahydrocannabinol precipitated by a cannabinoid receptor antagonist. Eur J ...
Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist.. Hirst RA1, ... CB1 receptor - data and references - Guide to Pharmacology. *Cannabinoid receptors - overview and references - Guide to ... Cannabinoid receptor agonists displaced [3H]SR141716A in a dose-dependent manner, (pKi) nabilone (8.29 +/- 0.08), WIN 55,212-2 ... We describe the use of SR141716A, a central cannabinoid antagonist, in radioligand binding and adenylyl cyclase (AC) inhibition ...
Related Cannabinoid Receptor Products. * SB225002 New SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM ... Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold ... Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold ... AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. ...
Cannabinoid Receptors Global Pruritus Therapeutics Market: Regional Analysis. North America. U.S.. Europe. U.K.. Germany. ... Opioid Receptor Antagonists. Topical Immunomodulators. Antidepressants. Immunosuppressants. Topical Local Anesthetics. ... Pruritus Therapeutics Market (Antihistamines, Topical Corticosteroids, Opioid Receptor Antagonists, Topical Immunomodulators, ... cannabinoid receptors and others. This report also includes the current and forecast demand for the region of North America, ...
Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- ... Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- ...
The aim of this study was to determine if the neutral cannabinoid CB₁ receptor antagonist, AM4113, regulates body weight in the ... The aim of this study was to determine if the neutral cannabinoid CB₁ receptor antagonist, AM4113, regulates body weight in the ... We confirmed that the AM4113-induced reduction in food intake is mediated by CB₁ receptors using CB₁ receptor knockout mice. In ... These data suggest that blockade of an endocannabinoid tone acting at CB₁ receptors induces an initial, transient reduction in ...
Further, we examined the effects of SR141716A (Rimonabant), a selective cannabinoid CB1 receptor antagonist which has been ... Contextual renewal of nicotine seeking in rats and its suppression by the cannabinoid-1 receptor antagonist Rimonabant ( ... and as such these data provide further evidence for the use of CB1 antagonists in smoking cessation. ...
1995) Novel antagonist implicates the CB1 cannabinoid receptor in the hypotensive action of anadamide. Eur J Pharmacol 278:279- ... 1998) SR1442528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J Pharmacol Exp Ther 284:644-650. ... a highly selective CB1 receptor antagonist, but not by SR144528, a highly selective CB2 receptor antagonist. Thus, the results ... 1997) SR141716A, a cannabinoid receptor antagonist produces hyperalgesia in untreated mice. Eur J Pharmacol 319:R3-R4. ...
Use of antagonists in studies of cannabinoid receptor biology will be useful in separating receptor-dependent from receptor- ... or pyrazole cannabinoid receptor antagonists and may provide a novel approach to cannabinoid receptor antagonist development. ... LY320135, a Novel Cannabinoid CB1 Receptor Antagonist, Unmasks Coupling of the CB1 Receptor to Stimulation of cAMP Accumulation ... LY320135, a Novel Cannabinoid CB1 Receptor Antagonist, Unmasks Coupling of the CB1 Receptor to Stimulation of cAMP Accumulation ...
2009) Cannabinoid receptor CB1 antagonists: state of the art and challenges. Vitam Horm 81:159-189. ... Cannabinoid type 1 (CB1) receptor antagonists have been developed for the treatment of obesity, but a major disadvantage is ... 4-diarylpyrazoline CB1 receptor antagonists (Fig. 1) (Lange et al., 2005) and the prototypic CB1 receptor antagonist rimonabant ... Cannabinoid Type 1 Receptor Antagonists Modulate Transport Activity of Multidrug Resistance-Associated Proteins MRP1, MRP2, ...
The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ... The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ... The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ... The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ...
Sensitive Sodium Channels by the Cannabinoid 1 Receptor Antagonist AM 251 in Mammalian Brain, Basic and Clinical Pharmacology ... Abstract: The cannabinoid 1 receptor antagonist AM 251 is known to block the inhibitory effects of endocannabinoids and ... Inhibition of Voltage‐Sensitive Sodium Channels by the Cannabinoid 1 Receptor Antagonist AM 251 in Mammalian Brain. Liao, ... Comparative receptor binding analyses of cannabinoid agonists and antagonists. Thomas, Thomas; Gilliam, Gilliam; Burch, Burch; ...
The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the ... The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the ... The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the ... The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the ...
Nanoparticle Formulation of a Poorly Soluble Cannabinoid Receptor 1 Antagonist Improves Absorption by Rat and Human Intestine. ... The nanoparticle formulation indeed improved the absorption of the cannabinoid receptor 1 (CB-1) antagonist and the delivery ... Nanoparticle Formulation of a Poorly Soluble Cannabinoid Receptor 1 Antagonist Improves Absorption by Rat and Human Intestine ... Nanoparticles of Poorly Soluble CB-1 Antagonist. Sanna Siissalo, Hans de Waard, Marina H. de Jager, Rose Hayeshi, Henderik W. ...
Cannabinoid receptor subtypes. Cannabinoids and the zebra finch. Cannabinoid CB1 receptor and emotion. CB1 cannabinoid receptor ... CB1 cannabinoid receptor agonism isnt rewarding 01 02 03 04 05 06 07 08 09 10 11 12 13 14 15. HOME. Refs. HedWeb. Future ... This review examines the development of cannabinoid CB1 receptor antagonists as a new class of therapeutic agents for drug ... CANNABINOID CB1 ANTAGONISTS AS PROMISING NEW MEDICATIONS FOR DRUG DEPENDENCE by. Le Foll B, Goldberg SR. NIDA. J Pharmacol Exp ...
Cannabinoid-receptor antagonists. The central cannabinoid system has an increasingly recognized role in appetite and feeding ... Cannabinoid receptor antagonists and obesity. Curr Opin Investig Drugs. 2004 Apr. 5(4):389-94. [Medline]. ... Rimonabant, the most-developed CB1-receptor antagonist, caused a mean weight loss of 3-6 kg over a 1-year follow-up at doses of ... Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight ...
The CB1 antagonist SR141716A, but not the CB2 antagonist SR144528, is a GPR55 antagonist. (A) Summary calcium responses in ... The effects of cannabinoid compounds are largely mediated by cannabinoid receptors. CB1, cloned in 1990 (1), is widely and ... 2007) The orphan receptor GPR55 is a novel cannabinoid receptor. Br J Pharmacol 152:1092-1101.. ... Here, we provide further evidence that GPR55, a G protein-coupled receptor, is a cannabinoid receptor. GPR55 is highly ...
Two of the cannabinoid receptors, CB1 and CB2 are the key targets of this endocannabinoid system. ... The authors also compare this conformation to the structure of antagonist (AM6538)-bound CB1 receptor. While both AM10257 and ... Two of the cannabinoid receptors, CB1 and CB2 are the key targets of this endocannabinoid system. While CB1 is widely present ... 2019, August 29). Crystal Structure of the Human Cannabinoid Receptor CB2. News-Medical. Retrieved on September 19, 2019 from ...
Cannabinoid Receptor Antagonist。CAS 番号:158681-13-1,純度:99.79%。東京倉庫。溶解度:DMSO。高品質な生理・薬理活性化合物。Rimonabant ... AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies ... AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies ... AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction
"CB1 and CB2 cannabinoid receptor antagonists prevent minocycline-induced neuroprotection following traumatic brain injury in ... The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that ... CNR2, CB-2, CB2, CX5, Cannabinoid receptor type 2, cannabinoid receptor 2. ... G-protein coupled receptor activity. • signal transducer activity. • cannabinoid receptor activity. Cellular component. • ...
SR144528, an antagonist of the CB2 cannabinoid receptor, blocks the THC-mediated increase in tumor growth in vivo. BALB/c mice ... CB2 cannabinoid receptor antagonist prevents the THC-mediated increase in tumor growth in vivo. Based on previous studies, we ... CB2 cannabinoid receptor antagonist studies. To determine whether the THC effect on tumorigenicity in vivo is mediated through ... SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J. Pharmacol. Exp. Ther. 284: 644. ...
Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-( ... Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-( ... Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-( ... T1 - Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist ...
  • Gallate JE, Saharov T, Mallet PE, McGregor IS (1999) Increased motivation for beer in rats following administration of a cannabinoid CB1 receptor agonist. (springer.com)
  • THCV has also high affinity for CB 2 receptors and signals as a partial agonist , differing from both CBD and rimonabant. (wikipedia.org)
  • [10] The use of the cannabinoid agonist, THC, in its many preparations to enhance appetite is a well known fact. (wikipedia.org)
  • The first specific CB 1 receptor antagonist / inverse agonist was rimonabant , discovered in 1994. (wikipedia.org)
  • Past efforts to develop peripherally selective antagonists of CB1 have largely targeted rimonabant, an inverse agonist of CB1. (nih.gov)
  • The present invention relates to a method to identify a true antagonist and an inverse agonist of a cannabinoid receptor (CB), and to discriminate between them. (freepatentsonline.com)
  • and measuring the activity of the constitutively active CB receptor following contact with the inhibitory agent, wherein a decrease in the activity in the constitutively active CB receptor, compared to the activity of the constitutively active CB receptor in the absence of the inhibitory agent, indicates that the agent is an inverse agonist. (freepatentsonline.com)
  • CP-945598 HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB 1 receptor agonist CP-55940. (selleckchem.com)
  • The agonist-like effects of SR141716A, which were more striking in unprimed than in primed mice, suggested that the antagonist also could function as a partial agonist at the CB1 receptor. (aspetjournals.org)
  • [9] The C-terminus of CB 2 receptors appears to play a critical role in the regulation of ligand-induced receptor desensitization and downregulation following repeated agonist application, [9] perhaps causing the receptor to become less responsive to particular ligands. (wikipedia.org)
  • [13] Together, these results support the emerging concept of agonist-directed trafficking at the cannabinoid receptors. (wikipedia.org)
  • The analgesic effects of morphine (5 mg/kg), ACEA (a CB1 receptor agonist, 5 mg/kg), JWH-015 (a CB2 receptor agonist, 5 mg/kg), AM251 (1 mg/kg) and JTE907 (5 mg/kg) were considered at 30-min intervals (0, 30, 60, 90, and 120 min) by tail-flick and hot-plate analgesia tests. (cumhuriyet.edu.tr)
  • We found that the synthetic cannabinoid agonist WIN55,212-2 and the FAAH inhibitor URB597 both enhanced memory consolidation for inhibitory avoidance training. (frontiersin.org)
  • The primary endogenous agonist of the human CB 1 receptor is anandamide . (wikipedia.org)
  • WIN55212-2 is a synthetic cannabinoid agonist and selective to cannabinoid 1 (CB1) receptors, which are distributed mainly in the central nervous system. (bvsalud.org)
  • The present study investigated agonist-stimulated [35S]GTPgammaS binding by WIN55212-2 in rat brain membranes and determined the antagonism by selective opioid antagonists at the level of receptor-ligand interaction and intracellular signal transduction. (bvsalud.org)
  • In agonist-stimulated [35S]GTPgammaS binding by WIN55212-2, the values of EC50 and maximum stimulation (% over basal) were determined in the absence or presence of the micro, kappa and delta opioid receptor antagonists naloxone (20 nM), norbinaltorphimine (3 nM), and naltrindole (3 nM), respectively. (bvsalud.org)
  • It is described as a mixed agonist/antagonist at the cannabinoid receptor CB 1 , meaning that it acts as an antagonist when co-administered alongside a more potent CB 1 agonist, but exhibits weak partial agonist effects when administered by itself. (wikipedia.org)
  • WIN 54,461 (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2. (wikipedia.org)
  • The present study explored the effects of CB(1) receptor ligands on oral dyskinesia induced by the dopamine D(1) receptor agonist SKF81297 (SKF) and acute dystonia induced by the dopamine D(2) receptor antagonist haloperidol in Cebus apella monkeys. (sigmaaldrich.com)
  • SKF (0.3 mg/kg) was administered alone and in combination with the CB(1) agonist CP55,940 (0.0025-0.01 mg/kg) or the CB(1) antagonist SR141716A (0.25-0.75 mg/kg). (sigmaaldrich.com)
  • It is an inverse agonist for the cannabinoid receptor CB1. (drugbank.ca)
  • Both a CB1 receptor agonist and a CB2 receptor agonist reduced colon shrinkage, colon inflammation, and diarrhoea, with the CB1 receptor agonist being somewhat more effective. (cannabis-med.org)
  • Cannabinoid agonist signal transduction in rat brain: Comparison of cannabinoid agonists in receptor binding, G‐protein activation and adenylyl cyclase inhibition. (currentprotocols.com)
  • HU‐308: A specific agonist for CB2, a peripheral cannabinoid receptor. (currentprotocols.com)
  • Development of cannabinoid receptor (CB1 and CB2) agonist and antagonist. (uthsc.edu)
  • Abnormalities in Dynamic Brain Activity Caused by Mild Traumatic Brain Injury Are Partially Rescued by the Cannabinoid Type-2 Receptor Inverse Agonist SMM-189. (uthsc.edu)
  • They administered the rodents a dose of a CB1 receptor agonist, or a cannabinoid drug, in order to induce cannabis intoxication-like effects, such as sedation, hypothermia , and hypomotility. (medicalnewstoday.com)
  • Rimonabant is thought to be a CB 1 receptor antagonist/inverse agonist, but it is unclear whether modulation of other cannabinoid receptor activity could have beneficial metabolic effects without significant psychiatric effects. (diabetesjournals.org)
  • The inverse agonist MK-9470 makes it possible to produce in vivo images of the distribution of CB 1 receptors in the human brain with positron emission tomography . (thefullwiki.org)
  • Rimonabant (Sanofi-Aventis ® ), a cannabinoid receptor antagonist/ inverse agonist, has reached the market as a drug for the treatment of obesity in several countries. (scielo.br)
  • Analyses of the designed antagonist and agonist pairs provided insight into the activation mechanism of CB2. (worldhealth.net)
  • Nonetheless, infusions of a synthetic cannabinoid agonist into the fourth ventricle modestly increased feeding (Miller et al. (420magazine.com)
  • Anandamide behaves as a partial agonist of cannabinoid receptors with slightly greater CB1 than CB2 affinity, but with much lower CB2 than CB1 efficacy . (news-medical.net)
  • The first CBR antagonist, rimonabant , was described in 1994. (wikipedia.org)
  • Rimonabant blocks the CB 1 receptor selectively and has been shown to decrease food intake and regulate body-weight gain. (wikipedia.org)
  • And Δ 9 -tetrahydrocannabivarin (THCV), a naturally occurring cannabinoid, modulate the effects of THC via direct blockade of cannabinoid CB 1 receptors, thus behaving like first-generation CB 1 receptor inverse agonists, such as rimonabant . (wikipedia.org)
  • Further, we examined the effects of SR141716A (Rimonabant), a selective cannabinoid CB1 receptor antagonist which has been shown to attenuate cue-induced relapse to nicotine seeking, on context-induced reinstatement of nicotine seeking. (nih.gov)
  • In this study, we investigated the interaction of the prototypic CB1 receptor antagonist rimonabant and a series of 3,4-diarylpyrazoline CB1 receptor antagonists with MRP1, MRP2, MRP3, and MRP4 in vitro. (aspetjournals.org)
  • A number of CB1 receptor antagonists, including rimonabant, stimulated MRP2 and MRP3 transport activity at low substrate concentrations but inhibited E 2 17βG transport at high substrate concentrations. (aspetjournals.org)
  • Rimonabant was the first and only selective CB1 receptor antagonist approved for therapeutic use. (aspetjournals.org)
  • Exposure of differentiated L6 myotubes to the CB1 antagonist rimonabant (SR141716) selectively increased 2-deoxyglucose uptake (2-DG) in a time- and dose-dependent manner. (aspetjournals.org)
  • Rimonabant (SR141716), a CB1 receptor antagonist, blocks both the dopamine-releasing and the discriminative and rewarding effects of Delta(9)-THC in animals. (cannabis-marijuana.com)
  • Rimonabant hHydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an K i of 1.8 nM. (medchemexpress.com)
  • AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies. (medchemexpress.com)
  • Discovery of the cannabinoid receptors has led to the development of rimonabant, a cannabinoid-1 (CB1) antagonist. (blogspot.com)
  • Rimonabant, a selective CB1 antagonist, is a novel treatment option for obese and overweight individuals. (blogspot.com)
  • These drugs are used to suppress cannabinoid receptor activity (for example, rimonabant). (medicinenet.com)
  • Genetic deletion of CB1-receptors (CB1Rs) from principal neurons of the forebrain and pharmacological antagonism with rimonabant (5 mg/kg) caused longer seizure duration. (curehunter.com)
  • The first proof of concept that so-called cannabinoid 1 receptor (CB1R) inverse agonists might offer an obesity therapy came from studies of another drug, developed by Sanofi-Aventis, called rimonabant. (eurekalert.org)
  • Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. (drugbank.ca)
  • Rimonabant is a specific CB1 cannabinoid receptor antagonist. (drugbank.ca)
  • Developed by Sanofi-Aventis, Acomplia (rimonabant) is a selective CB1 endocannabinoid receptor antagonist indicated for the treatment of obesity. (drugdevelopment-technology.com)
  • This effect has been assumed to be CB 1 -mediated since the specific CB 1 antagonist SR 141716A ( Rimonabant ) blocks the effect. (thefullwiki.org)
  • CB 1 selective antagonists are used for weight reduction and smoking cessation (see Rimonabant ). (thefullwiki.org)
  • Thus, the objective of the present review is to discuss the potential psychiatric side-effects of CB1 receptor antagonists, such as rimonabant, which has been recently marketed in several countries for the treatment of smoking cessation, obesity and associated metabolic disorders. (scielo.br)
  • Foi realizada uma busca na literatura no PubMed e Scielo até fevereiro de 2009, com os termos "obesity", "rimonabant", "cannabinoids", "unwanted effects", "diabetes" , "smoking cessation" e "side effects" . (scielo.br)
  • Acomplia tablets contain the active ingredient rimonabant, which is a type of medicine called a cannabinoid-1 receptor antagonist. (netdoctor.co.uk)
  • Rimonabant works by blocking receptors called cannabinoid-1 receptors (CB1). (netdoctor.co.uk)
  • Rimonabant blocks CB1 receptors and so reduces cravings for these types of foods and helps decrease appetite and control hunger. (netdoctor.co.uk)
  • One of the ways this is being tested is by designing agonists and antagonists specifically against CB2 and assessing the effects. (news-medical.net)
  • therapeutic uses of agonists and antagonists of cannabinoids receptors. (booktopia.com.au)
  • C6 rat astroglioma cells were challenged with 1 μg/ml Aβ 1-42 in the presence or absence of selective agonists and antagonists of cannabinoid (CB)1 and CB2 receptors. (420magazine.com)
  • The endogenous cannabinoid system includes cannabinoid receptors, their endogenous ligands (endocannabinoids) and enzymes for their synthesis and degradation. (wikipedia.org)
  • Mansbach RS (1991) Effects of NMDA receptor ligands on sensorimotor gating in the rat. (springer.com)
  • A range of 13 commonly used non-cannabinoid ligands included at 100 microM were unable to displace [3H]SR141716A. (nih.gov)
  • Our findings indicate a role for the CB1 receptor subtype in cytokine modulation by CB ligands. (aspetjournals.org)
  • Findings from both clinical and preclinical studies suggest that ligands blocking CB1 receptors offer a novel approach for patients suffering from drug dependence that may be efficacious across different classes of abused drugs. (cannabis-marijuana.com)
  • [19] Many of these ligands appear to exhibit properties of functional selectivity at the CB 2 receptor: 2-AG preferentially activates the MAPK-ERK pathway, while noladin preferentially inhibits adenylyl cyclase. (wikipedia.org)
  • The actions of cannabinoids are also regulated by the endocannabinoid system (ECS) which includes enzymes involved in synthesis, uptake and degradation of endogenous cannabinoid ligands, and the CB1 and CB2 receptors. (frontiersin.org)
  • Both types of compounds mimic endogenous ligands and act through distinct G-protein-coupled receptor families known as cannabinoid ( Felder and Glass, 1998 ) and opioid ( Kieffer, 1995 ) receptors. (jneurosci.org)
  • The K D values of CB1 ligands in the ChEMBL database are predicted by QSAR random forest (RF) modeling for the CB1 receptor and known off-targets (TRPV1, mGlu5, 5-HT1a). (springer.com)
  • Endocannabinoids modulate striatal dopamine activity via type 1 cannabinoid (CB(1)) receptors, and studies in rats and humans suggest beneficial effects of CB(1) ligands on EPS. (sigmaaldrich.com)
  • The present review provides an overview of therapeutic potential of ligands and plants modulating cannabinoid receptors that may be of interest to pharmaceutical industry in search of new and safer drug discovery and development for future therapeutics. (hindawi.com)
  • cannabinoid receptor ligands also known as endocannabinoids are characterized by arachidonyl ethanolamide (anandamide, AEA) and 2-arachidonoyl glycerol (2-AG) [ 1 , 2 ] and the enzymes involved in synthesis and degradation of the endocannabinoids. (hindawi.com)
  • 4 The endogenous cannabinoid ligands arachidonoyl ethanolamide (anandamide) and 2-arachidonoylglycerol (2-AG) also lower blood pressure and heart rate in rodents. (ahajournals.org)
  • CB1 cannabinoid receptor ligands. (wikipedia.org)
  • Anti-inflammatory activity of cannabinoid receptor 2 ligands in primary hPDL fibroblasts. (uthsc.edu)
  • Furthermore, the existence of endogenous ligands that bind to these receptors (termed "endocannabinoids") has also been demonstrated, pointing towards the pharmacological and physiological importance of cannabinoid receptors. (news-medical.net)
  • Both the receptors and their endogenous ligands comprise the endocannabinoid system . (news-medical.net)
  • Serra S, Carai MAM, Brunetti G, Gomez R, Melis S, Vacca G, Colombo G, Gessa GL (2001) The cannabinoid receptor antagonist SR 141716 prevents acquisition of drinking behaviour in alcoholpreferring rats. (springer.com)
  • This search led to the discovery of the first endogenous cannabinoid (endocannabinoid), anandamide (arachidonoyl ethanolamide). (wikipedia.org)
  • Cannabinoid receptor agonists displaced [3H]SR141716A in a dose-dependent manner, (pKi) nabilone (8.29 +/- 0.08), WIN 55,212-2 (7.75 +/- 0.15), delta 9-tetrahydrocannabinol (7.29 +/- 0.21), delta 8-tetrahydrocannabinol (6.53 +/- 0.09) and anandamide (5.92 +/- 0.04). (nih.gov)
  • LY320135 functionally reversed anandamide-mediated adenylate cyclase inhibition in Chinese hamster ovary (CHO) cells stably expressing the CB1 receptor. (aspetjournals.org)
  • Pertussis toxin treatment of CHO cells expressing the CB1 receptor attenuated the anandamide-mediated inhibition of adenylate cyclase and unmasked a stimulatory effect of anandamide on adenylate cyclase. (aspetjournals.org)
  • These discoveries have led to a growing interest in determining the physiological role of anandamide, other fatty acid amides and cannabinoid receptors. (aspetjournals.org)
  • GPR55 is highly expressed in large dorsal root ganglion neurons and, upon activation by various cannabinoids (Δ 9 THC, the anandamide analog methanandamide, and JWH015) increases intracellular calcium in these neurons. (pnas.org)
  • This compound should prove to be a powerful tool for investigating the in vivo functions of the anandamide/cannabinoid system. (nih.gov)
  • Conversely, preventing the degradation of the endocannabinoid anandamide by an inhibitor of fatty acid amidohydrolase reduces blood pressure, cardiac contractility, and vascular resistance to levels in normotensive rats, and these effects are prevented by CB 1 antagonists. (ahajournals.org)
  • The new study describes a pathway-different than the one previously suggested-for the biosynthesis of neurotransmitter lipids, N-acyl ethanolamines (NAEs), which include the endogenous cannabinoid ("endocannabinoid") anandamide. (bio-medicine.org)
  • The endocannabinoid system (ECS), mainly through the action of anandamide (AEA) and 2-arachidonoylglycerol (2-AG) at cannabinoid (CB 1 , CB 2 ) and vanilloid (TRPV1) receptors, plays a crucial role in controlling functionality of sperm, with a clear impact on male reproductive potential. (plos.org)
  • Moreover, Aβ provoked down-regulation of CB1 receptors together with a reduction of anandamide concentration, whereas CB2 receptors were up-regulated and 2-arachidonoyl glycerol concentration was increased. (420magazine.com)
  • Among these endocannabinoids, arachidonoyl-ethanolamide (also known as anandamide) was among the first to be discovered, and there is compelling evidence that this ligand (as well as some of its metabolites) may also activate vanilloid VRI receptors. (news-medical.net)
  • Cannabinoid receptor pharmacology has been hampered by the availability of selective antagonists. (aspetjournals.org)
  • Not much is known about GPR18 and GPR55 subtypes and current research efforts in the field of cannabinoid receptors are directed towards exploring their pharmacology and physiological roles. (mdpi.com)
  • In the new study - published in the British Journal of Pharmacology - researchers have investigated possible avenues for attenuating the effects of intoxication with cannabis and synthetic cannabinoids. (medicalnewstoday.com)
  • New Developments in the Pharmacology of Cannabinoids. (news-medical.net)
  • SR141716A (Sanofi Recherche), a pyrazole derivative with high affinity for rat and human CB1 cannabinoid receptors, has recently been reported to reverse biochemical, physiological and behavioral effects induced by cannabinoid agonists. (springer.com)
  • Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist. (nih.gov)
  • We describe the use of SR141716A, a central cannabinoid antagonist, in radioligand binding and adenylyl cyclase (AC) inhibition studies in rat cerebella membranes. (nih.gov)
  • In addition, studies with SR141716A have provided evidence for the presence of CB1 receptors in peripheral tissues as well as in the central nervous system (CNS). (aspetjournals.org)
  • SR141716A was found to be selective and potent at the CB1 receptor and blocked WIN 55212-2-mediated behavioral responses. (aspetjournals.org)
  • In the first step, the authors created crystals of CB2 antagonist AM10257 which was obtained by optimizing the first known antagonist of CB1, SR141716A. (news-medical.net)
  • SR141716A is the first selective and orally active antagonist of the brain cannabinoid receptor. (nih.gov)
  • In vitro, SR141716A antagonises the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes. (nih.gov)
  • After intraperitoneal or oral administration SR141716A antagonises classical pharmacological and behavioural effects of cannabinoid receptor agonists. (nih.gov)
  • A cannabinoid receptor antagonist , also known simply as a cannabinoid antagonist or as an anticannabinoid , is a type of cannabinoidergic drug that binds to cannabinoid receptors (CBR) and prevents their activation by endocannabinoids . (wikipedia.org)
  • Endocannabinoids are eicosanoids acting as agonists for cannabinoid receptors, and they occur naturally in the body. (wikipedia.org)
  • Nicholson, Russell A. 2004-02-01 00:00:00 Abstract: The cannabinoid 1 receptor antagonist AM 251 is known to block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. (deepdyve.com)
  • Abstract: The cannabinoid 1 receptor antagonist AM 251 is known to block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. (deepdyve.com)
  • Among the different factors involved, of particular interest is the binding affinity of endocannabinoids, and their analogs, for other receptor families beyond cannabinoid receptors, such as the peroxisome proliferator-activated receptors (PPARs), and the transient receptor potential cation channel subfamily V member 1 (TRPV1). (frontiersin.org)
  • [13] The CB 1 receptor is activated by cannabinoids , generated naturally inside the body ( endocannabinoids ) or introduced into the body as cannabis or a related synthetic compound. (wikipedia.org)
  • Endogenous cannabinoids (endocannabinoids) are endogenous compounds that resemble the active ingredient of marijuana and activate the cannabinoid receptor in the brain. (jneurosci.org)
  • Cannabinoid receptors are responsible for the psychological effects of marijuana (Cannabis sativa), and natural "endocannabinoids" are important regulators of energy balance. (eurekalert.org)
  • Endocannabinoids released from the depolarized neuron bind to CB 1 receptors in the pre-synaptic neuron and cause a reduction in GABA release. (thefullwiki.org)
  • as such elucidating the molecular structure of the receptors that bind endocannabinoids is a key step towards developing drugs that can differentiate between the two known receptors. (worldhealth.net)
  • This impairment was blocked by AM251, a cannabinoid CB 1 receptor antagonist, administered 30 min before the training trial or co-administered with MDMA. (nature.com)
  • This increase of CB 1 receptor protein in the hippocampus was also blocked by the co-administration of AM251. (nature.com)
  • We investigated activation of sensory neurons by two cannabinoid antagonists - AM251 and AM630. (unboundmedicine.com)
  • In summary, these findings demonstrate alternative targets for the cannabinoid antagonists, AM251 and AM630, in peripheral antihyperalgesia which involve certain TRP channels. (unboundmedicine.com)
  • TY - JOUR T1 - Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. (unboundmedicine.com)
  • The aim of this study was to investigate the effects of AM251 (a selective CB1 antagonist) and JTE907 (a selective CB2 antagonist) on morphine analgesia and tolerance in rats. (cumhuriyet.edu.tr)
  • RESEARCH DESIGN AND METHODS Streptozotocin-induced diabetic mice were treated with N -(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,3-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (AM251), a selective CB1-receptor antagonist, at the dosage of 1 mg · kg −1 · day −1 via intraperitoneal injection for 14 weeks. (diabetesjournals.org)
  • In the cultures, TC decreased neuronal injury, intracellular oxidative stress, and mitochondrial depolarization following OGD/R, and the effects were reversed by AM630 but not by a CB1R antagonist, AM251. (medindia.net)
  • So, they designed a mouse model in which they tested the effect of a molecule called AM251 - which is a CB1 receptor antagonist - against cannabinoid intoxication. (medicalnewstoday.com)
  • Twenty minutes after receiving these cannabinoids and exhibiting signs of intoxication, the mice received a dose of 5 milligrams per kilogram of the AM251 molecule. (medicalnewstoday.com)
  • The selective cannabinoid 1 receptor (CB1R) antagonist AM251 [N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide] prevented the response, demonstrating CB1R mediation of 2-AG-induced coupling. (420magazine.com)
  • Angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), and calcium channel blockers, rather than beta-adrenergic blockers, should be considered as first-line therapy for hypertension in patients with type 2 diabetes mellitus who are obese. (medscape.com)
  • The therapeutic application of metabolic inhibitors , pharmacotherapy for obesity, immune therapy in type I diabetes and receptor agonists are just some of the topics being covered. (smi-online.co.uk)
  • Cannabinoid CB1 and CB2 receptor antagonists may be useful for their potential to increase or prolong opioid analgesia while attenuating the development of opioid tolerance. (cumhuriyet.edu.tr)
  • Opioid receptors and CB1 receptors have several similarities in terms of their intracellular signal transduction mechanisms, distributions, and pharmacological action. (bvsalud.org)
  • Ke values for opioid antagonist inhibition in the absence or presence of each opioid receptor antagonist were calculated using the following equation [nanomolar antagonist] / (dose ratio of EC50 - 1). (bvsalud.org)
  • Addition of selective opioid antagonists did not produce a significant rightward shift in the WIN55212-2 concentration-response curve, and Ke values were not applicable. (bvsalud.org)
  • Our results suggest that the functional activity of WIN55212-2-stimulated [35S]GTPgammaS binding was not affected by opioid antagonists in the rat brain membranes. (bvsalud.org)
  • Cannabinoid receptors are partly regulated by the mu opioid pathway. (bio.net)
  • mu opioid receptors. (bio.net)
  • To investigate the molecular basis for cannabinoid dependence and its possible relationship with the endogenous opioid system, we explored Δ9-tetrahydrocannabinol (THC) activity in mice lacking μ-, δ- or κ-opioid receptor genes. (jneurosci.org)
  • Thus, an opposing activity of μ- and κ-opioid receptors in modulating reward pathways forms the basis for the dual euphoric-dysphoric activity of THC. (jneurosci.org)
  • The existence of cross-tolerance between opioid and cannabinoid agonists has been supported by a variety of studies. (jneurosci.org)
  • Cross-dependence between opioid and cannabinoid compounds has also been reported. (jneurosci.org)
  • Sedation, in contrast, was not influenced by cannabinoid or opioid receptor blockage, and euphoria cannot be studied in mouse models. (pnas.org)
  • Opioid antagonists are what are given to help curb addiction in drug addicts. (robbwolf.com)
  • One study actually showed that oral administration of an antagonist opioid and a cannabinoid receptor inverse agent led to decreased eating in obese mice (Chen, 2003). (robbwolf.com)
  • The CB 1 cannabinoid receptor mediates many of the psychoactive effects of Δ 9 THC, the principal active component of cannabis. (pnas.org)
  • [5] [6] It is closely related to the cannabinoid receptor type 1 , which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol , the active agent in cannabis , and other phytocannabinoids (plant cannabinoids). (wikipedia.org)
  • The cannabis plant contains other minor cannabinoids that interact with the human endocannabinoid system, but their effects are far weaker and they are present in lower concentrations. (medicinenet.com)
  • Cannabinoids include the active constituents of Cannabis or are molecules that mimic the structure and/or function of these Cannabis -derived molecules. (frontiersin.org)
  • I recall an old study wherein they found that cannabis tolerance was proportional to the level of receptor retraction from the cell surface. (bio.net)
  • TC is a major cannabinoid derived from the essential oil of the flowering plant Cannabis sativa, but has a fundamentally different structure from classical cannabinoids. (medindia.net)
  • More than 60 different cannabinoids have been isolated from cannabis, the most prominent of which include THC and CBD. (cmaj.ca)
  • Native cannabis and cannabinoid derivatives may have effects on symptoms such as nausea, cachexia-anorexia, neurologic and cancer-related pain, chemosensory alterations and anxiety. (cmaj.ca)
  • The cannabinoid molecules are derived from Cannabis sativa plant which acts on the cannabinoid receptors types 1 and 2 (CB 1 and CB 2 ) which have been explored as potential therapeutic targets for drug discovery and development. (hindawi.com)
  • Pharmacological actions and therapeutic uses of cannabis and cannabinoids. (currentprotocols.com)
  • Synthetic cannabinoids are marketed and perceived as a safer and less harmful alternative to cannabis. (medicalnewstoday.com)
  • As the researchers explain, cannabis intoxication, or the feeling of "being high," occurs when the so-called CB1 brain receptors are activated. (medicalnewstoday.com)
  • There are few randomized smoked or vaporized cannabis trials in cancer on which to judge the benefits of these forms of cannabinoids on symptoms and the clinical course of cancer. (jnccn.org)
  • In total, there are at least 113 cannabinoids that have been discovered in cannabis. (metrotimes.com)
  • Cannabis sativa is a herbaceous plant that represents a source of more than sixty aromatic hydrocarbon compounds known as cannabinoids, and among them delta-9-tetrahydrocannabinol (usually abbreviated as THC) is the main psychotropic constituent. (news-medical.net)
  • Past reports suggest that antagonism of the CB1 receptor (CB1R) is an emerging strategy to alcoholic liver disease. (rti.org)
  • However, neutral antagonists or CNS-sparing peripherally restricted antagonists of CB1R may be useful for ALD as these compounds should have limited adverse effects. (rti.org)
  • In summary, RTI-13329-173B and other such peripherally selective CB1R antagonists should be further developed and investigated for alcoholic liver disease. (rti.org)
  • Cannabinoid-1 receptor (CB1R) antagonists reduce body weight and improve cardiometabolic abnormalities in experimental and human obesity, but their therapeutic potential is limited by neuropsychiatric side effects. (jci.org)
  • Here we have demonstrated that a CB1R neutral antagonist largely restricted to the periphery does not affect behavioral responses mediated by CB1R in the brains of mice with genetic or diet-induced obesity, but it does cause weight-independent improvements in glucose homeostasis, fatty liver, and plasma lipid profile. (jci.org)
  • [4] These findings raised further questions about the pharmacological and physiological role of the cannabinoid system. (wikipedia.org)
  • [11] It was then discovered that the blockage of the CB 1 receptor represented a new pharmacological target. (wikipedia.org)
  • Compton DR, Johnson MR, Melvin LS, Martin BR (1992) Pharmacological profile of a series of bicyclic cannabinoid analogs: classification as cannabimimetic agents. (springer.com)
  • Psychoactive cannabinoids (CBs) have a variety of pharmacological effects that are evoked through interactions with central or peripheral CB receptors. (aspetjournals.org)
  • CB 2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol . (wikipedia.org)
  • We tested two cannabinoid compounds with different pharmacological properties in the inhibitory avoidance task, and evaluated whether the observed effects are mediated by cannabinoid, PPARα or TRPV1 receptor activation. (frontiersin.org)
  • The potential value of this compound to researchers for pharmacological studies of the CB2 receptor and its potential role in immune function prompted the synthesis of the tritiated compound. (drugabuse.gov)
  • Other than CB1, genetic deletion or pharmacological blockade with SB366791 (1 mg/kg) of transient receptor potential vanilloid receptor 1 (TRPV1) had no effect on the duration of behavioral or electrographic seizure activity in the kindling model. (curehunter.com)
  • Ablation of cannabinoid receptor 1 receptors on GABAergic neurons inhibits running-induced anxiolysis, and pharmacological blockage of central and peripheral cannabinoid receptors inhibits analgesia. (pnas.org)
  • 1993), and proteins modulating their synthesis and inactivation (Piomelli, 2003) has afforded considerable pharmacological precision in elucidating various molecular, cellular, and behavioral actions of the cannabinoid system. (420magazine.com)
  • Since cannabinoids are characterized by low water and high lipid solubility, their pharmacological properties were classically ascribed to the perturbation of biological membranes and their phospholipid components. (news-medical.net)
  • In any case, the above-mentioned distribution pattern of CB1 receptors accounts for several notable pharmacological properties of their agonists, e.g. their tendency to impair memory and cognition, as well as to alter the motor function control. (news-medical.net)
  • The cannabinoid receptor agonists that have been used extensively in pharmacological experiments show equal binding affinity for both CB1 and CB2 receptors, or show merely marginal CB1 or CB2 selectivity. (news-medical.net)
  • Even though otenabant penetrates the CNS, it is unique among CB1 antagonists that have been clinically tested because it has properties that are normally associated with peripherally selective compounds. (nih.gov)
  • The effects of cannabinoid compounds are largely mediated by cannabinoid receptors. (pnas.org)
  • A recent study found that a variety of cannabinoid compounds stimulated GTPγS binding in cells stably expressing GPR55 ( 6 ). (pnas.org)
  • Preliminary studies of cannabinoids in patients with HD have shown that these compounds are safe in these patients. (clinicaltrials.gov)
  • Those studies, however, did not show efficacy because 1) they were underpowered from the statistical point of view, 2) were performed with isolated pure cannabinoids, instead of the more physiological stimulation with a mixture of compounds, and 3) they did use insensitive clinical parameters instead of sensitive end points, such as pathogenically important biomarkers. (clinicaltrials.gov)
  • The present invention pertains to cannabinoid (CB) receptor neutral antagonists, and especially CB1 neutral antagonists, and including, for example, certain 1,5-di-aryl-pyrazole compounds. (elsevier.com)
  • 5 Of these, there is a group of at least 66 compounds that contain only carbon, hydrogen, and oxygen and are known collectively as cannabinoids. (bmj.com)
  • Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS. (nih.gov)
  • Compounds that inhibit or block the activity of CANNABINOID RECEPTORS. (nih.gov)
  • Compounds and drugs that inhibit or block the activity of CCR5 RECEPTORS. (nih.gov)
  • Now that both cannabinoid structure receptors are known selective compounds can be design to target one of the receptors as well as agents with desired polypharmacological profiles to target both receptors together. (worldhealth.net)
  • This cannabinoid system produces different responses to compounds using two receptors known as the CB1 and CB2 receptors. (metrotimes.com)
  • The data support the assumption that compounds able to selectively block CB2 receptors may have therapeutic potential in controlling Aβ-related pathology, due to their beneficial effects devoid of psychotropic consequences. (420magazine.com)
  • Cannabinoid CB1 receptors are expressed in this brain reward circuit and modulate the dopamine-releasing effects of Delta(9)-THC and nicotine. (cannabis-marijuana.com)
  • it is not surprising that cannabinoids modulate emotional responses and emotional states, as well as cognitive and memory processes. (frontiersin.org)
  • The CNS represents a well-studied area and cancer is emerging in terms of understanding mechanisms by which cannabinoids modulate their activity. (frontiersin.org)
  • Classical cannabinoid agonists (structures shown in Table 1 ) bind to and activate cannabinoid receptors 1 and 2 (CB1, CB2) that modulate signal transduction cascades to produce various physiological and pathological outcomes. (frontiersin.org)
  • We have shown that synthetic cannabinoids also modulate the cyclooxygenase-2 (COX-2) signaling pathway in breast cancer cells. (aacrjournals.org)
  • Cannabinoids are known to modulate a multitude of monoamine receptors. (jnccn.org)
  • Therefore, a common property of CB1 and CB2 receptors is the ability to modulate the continuous release of diverse chemical messengers - CB1 receptors from neurons and CB2 receptors from immune cells. (news-medical.net)
  • Therefore, peripheral CB1 receptor antagonists might have therapeutic potential for improving metabolic risk in obese patients without causing psychiatric side effects. (aspetjournals.org)
  • T his review examines the development of cannabinoid CB1 receptor antagonists as a new class of therapeutic agents for drug addiction. (cannabis-marijuana.com)
  • What are the therapeutic uses of cannabinoids? (medicinenet.com)
  • Obtaining a comprehensive understanding of the diverse mechanisms of cannabinoid action may lead to the design and development of therapeutic agents with greater efficacy and specificity for their cellular targets. (frontiersin.org)
  • The 21st century will witness the unprecedented marketing of therapeutic drugs developed from cannabinoids and the endocannabinoid system. (booktopia.com.au)
  • Cannabinoids is a timely volume, which represents a comprehensive review of the most important issues in cannabinoid research as well as those of most likely therapeutic relevance. (booktopia.com.au)
  • Cortical type 2 cannabinoid (CB2) receptors might serve as potential therapeutic targets for cerebral ischemia suggests a new study published in the March issue of The American Journal of Pathology . (medindia.net)
  • The CB2 receptor is therefore considered as a very promising target for therapeutic approaches as well as for imaging. (mdpi.com)
  • Therefore, the plant based cannabinoid molecules proved to be promising and emerging therapeutic alternative. (hindawi.com)
  • These results indicate that CB1 and CB2 receptors could be used to develop novel therapeutic strategies against breast cancer growth and metastasis. (aacrjournals.org)
  • From a therapeutic perspective, any of these enzymes could represent an attractive drug target for a range of human disorders in which disruption of endocannabinoid signaling by cannabinoid receptor antagonists has proven beneficial. (bio-medicine.org)
  • Because of the legality of CBD, many researchers are now looking into the different therapeutic effects of this cannabinoid. (metrotimes.com)
  • Since many important intracellular proteins are Ca 2+ -dependent for activation, signal transduction through the CB 1 receptor may impair these secondary pathways and have a profound influence on the ability of viruses to replicate in neurons. (mdpi.com)
  • GPR55 activation by several cannabinoids increases intracellular calcium in HEK293 cells and DRG neurons. (pnas.org)
  • R6/2 treated mice treated with cannabinoids improve their clinical phenotype, their brain lesions, the synaptic density and the levels of BNDF, a neurotrophic factor which enhances survival and resistance of striatal neurons. (clinicaltrials.gov)
  • In neurons, where innate antiviral/pro-resolution responses include the activation of NOS-1, inhibition of Ca 2+ activity by cannabinoids, increased viral replication and disease. (mdpi.com)
  • In cell cultures composed of rat cortical neurons and glia exposed to oxygen-glucose deprivation and reoxygenation (OGD/R), TC decreased neuronal injury and mitochondrial depolarization, specifically through type 2 cannabinoid receptor (CB2R) pathways. (medindia.net)
  • We show that anxiolysis depends on intact cannabinoid receptor 1 (CB1) receptors on forebrain GABAergic neurons and pain reduction on activation of peripheral CB1 and CB2 receptors. (pnas.org)
  • The CB1 receptor is the most studied receptor of the endocannabinoid system and is densely expressed in the CNS by many classes of neurons [ 4 , 5 ]. (mdpi.com)
  • This effect is produced by interaction with CB 1 (or CB 1 -like) receptors, located on peripheral endings of sensory neurons involved in pain transmission. (thefullwiki.org)
  • Selective type 1 cannabinoid (CB1) receptor antagonists may assist with smoking cessation by restoring the balance of the endocannabinoid system, which can be disrupted by prolonged use of nicotine. (essentialevidenceplus.com)
  • Poncelet M, Maruani J, Calassi R, Soubrié P (2003) Overeating, alcohol and sucrose consumption decrease in CB1 receptor deleted mice. (springer.com)
  • Wang L, Liu J, Harvey-White J, Zimmer A, Kunos G (2003) Endocannabinoid signaling via cannabinoid receptor 1 is involved in ethanol preference and its age-dependent decline in mice. (springer.com)
  • Naassila M, Pierrefiche O, Ledent C, Daoust M (2004) Decreased alcohol self-administration and increased alcohol sensitivity and withdrawal in CB1 receptor knockout mice. (springer.com)
  • Furthermore, CB 1 receptor knockout mice showed no impairment of recognition performance on the withdrawal from MDMA. (nature.com)
  • We confirmed that the AM4113-induced reduction in food intake is mediated by CB₁ receptors using CB₁ receptor knockout mice. (biomedsearch.com)
  • In addition, in adipose tissue of CB 1 -receptor knockout mice, SR141716 had no effect on Acrp30 mRNA expression, demonstrating a CB 1 receptor mediating effect. (aspetjournals.org)
  • RESULTS In diabetic mice, the CB1 receptor was overexpressed within the glomeruli, predominantly by glomerular podocytes. (diabetesjournals.org)
  • Blockade of the CB1 receptor did not affect body weight, blood glucose, and blood pressure levels in either diabetic or control mice. (diabetesjournals.org)
  • Analysis in conditional cannabinoid 1 receptor-knockout mice reveals neuronal subpopulation-specific effects on epileptogenesis in the kindling paradigm. (curehunter.com)
  • Using a combination of pharmacologic, molecular genetic, and behavioral studies in mice, we demonstrate that cannabinoid receptors mediate acute anxiolysis and analgesia after running. (pnas.org)
  • 11 Cannabinoids fail to lower blood pressure after selective blockade of CB 1 5 or in CB 1 -knockout mice, 12,13 which implicates CB 1 in this effect. (ahajournals.org)
  • Treatment of normotensive rats and mice with CB 1 antagonists alone does not affect blood pressure, 3,5 and baseline blood pressure is similar in CB 1 -knockout mice and their wild-type littermates, 12,13 which indicates that CB 1 receptors are not tonically active. (ahajournals.org)
  • Experimental evidence has shown that cannabinoids inhibit the growth of tumor xenograft in mice ( 8 , 11 - 14 ). (aacrjournals.org)
  • In contrast, in genetically manipulated mice without CB1 receptors there was no effect on disease onset but significantly extended life span. (cannabis-med.org)
  • CBD is a very low-affinity CB 1 ligand, that can nevertheless affect CB 1 receptor activity in vivo in an indirect manner, while THCV is a high-affinity CB 1 receptor ligand and potent antagonist in vitro and yet only occasionally produces effects in vivo resulting from CB 1 receptor antagonism. (wikipedia.org)
  • Studies in rodents have shown that antagonism of this receptor leads to reduced food intake and weight reduction ( Boyd and Fremming, 2005 ). (aspetjournals.org)
  • Other findings indicated that the anti-ischemic effect of TC was not mediated by NMDA receptor antagonism or antioxidant activity. (medindia.net)
  • Effects of cannabinoid CB1 receptor agonism and antagonism on SKF81297-induced dyskinesia and haloperidol-induced dystonia in Cebus apella monkeys. (sigmaaldrich.com)
  • Analysis revealed AM10257's opposing functional profile of CB2 antagonism vs CB1, further structural analysis using mutagenesis studies and molecular docking revealed molecular basis of their function and selectivity for the two receptors. (worldhealth.net)
  • Immunohistochemical and biochemical findings revealed that selective agonism at CB1 and antagonism at CB2 receptors was able to blunt Aβ-induced reactive astrogliosis with subsequent overexpression of glial fibrillary acidic protein and S100B protein. (420magazine.com)
  • Cannabinoid receptor antagonists have been utilized extensively in vivo as well as in vitro, but their selectivity has not been fully examined. (unboundmedicine.com)
  • Researchers found that the cannabinoid trans-caryophyllene (TC) protected brain cells from the effects of ischemia in both in vivo and in vitro animal models. (medindia.net)
  • In vitro autoradiography of rat and mouse spleen slices, as spleen expresses a high physiological expression of CB2 receptors, demonstrated that [ 11 C]KP23 exhibits specific binding towards CB2. (mdpi.com)
  • Preclinical in vitro and in vivo studies suggest that cannabinoids may have anticancer activity. (jnccn.org)
  • Immunofluorescence and in vitro [35S]GTPγS autoradiography of rat tissue sections containing the PBN revealed the presence of cannabinoid receptors and their functional capability to couple to their G-proteins after incubation with the endocannabinoid 2-arachidonoyl glycerol (2-AG). (420magazine.com)
  • [1] [2] Cannabidiol (CBD), a naturally occurring cannabinoid, is a non-competitive CB 1 /CB 2 receptor antagonist. (wikipedia.org)
  • Two of them, tetrahydrocannabinol (THC) and cannabidiol (CBD), bind to the human endocannabinoid receptors CB1-R and CB2-R. Both THC and CBD have medical benefits, but only THC produces euphoric effects. (medicinenet.com)
  • Multiple studies, most of which are of moderate to low quality, demonstrate that tetrahydrocannabinol (THC) and oromucosal cannabinoid combinations of THC and cannabidiol (CBD) modestly reduce cancer pain. (jnccn.org)
  • CB 1 , cloned in 1990 ( 1 ), is widely and highly expressed in the CNS, where it likely mediates the majority of the psychotropic and behavioral effects of cannabinoids. (pnas.org)
  • [5] The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB 1 ) receptor, discovered in 1990. (wikipedia.org)
  • these are CB1 and CB2 receptors, cloned in 1990 and 1993, respectively. (news-medical.net)
  • Both receptors are 7-transmembrane G-protein coupled receptors ( GPCRs ) which inhibit the accumulation of cyclic adenosine monophosphate within cells. (wikipedia.org)
  • Like the CB 1 receptors, CB 2 receptors inhibit the activity of adenylyl cyclase through their Gi/Go α subunits. (wikipedia.org)
  • [13] Like noladin, the synthetic ligand CP-55,940 has also been shown to preferentially inhibit adenylyl cyclase in CB 2 receptors. (wikipedia.org)
  • The CB 1 receptor is expressed pre-synaptically at both glutaminergic and GABAergic interneurons and, in effect, acts as a neuromodulator to inhibit release of glutamate and GABA . (wikipedia.org)
  • Engagement of the CB 1 receptor by its endogenous or exogenous agonists may inhibit the release of Ca 2+ from intracellular or extracellular stores. (mdpi.com)
  • Several studies have shown that these phytocannabinoids show affinity, potency, selectivity, and efficacy towards cannabinoid receptors and inhibit endocannabinoid metabolizing enzymes, thus reducing hyperactivity of endocannabinoid systems. (hindawi.com)
  • Cannabinoids have been shown to inhibit tumor angiogenesis and directly induce apoptosis or cell cycle arrest in neoplastic cells ( 8 , 11 - 14 ). (aacrjournals.org)
  • Agonists of cannabinoid receptor 1 and 2 inhibit experimental colitis induced by OIL of mustard and by dextran sulfate sodium. (cannabis-med.org)
  • In the liver, activation of the CB 1 receptor is known to increase de novo lipogenesis , [ 5 ] Activation of presynaptic CB 1 receptors is also known to inhibit sympathetic innervation of blood vessels and contributes to the suppression of the neurogenic vasopressor response in septic shock . (thefullwiki.org)
  • The international team concluded substances activating one of the receptors can weaken or inhibit the other and vice versa, opening possibilities for drugs to target both receptors exclusively or together but in different ways. (worldhealth.net)
  • Arnone M, Maruani J, Chaperon F, Thiébot M-E, Poncelet M, Soubrié P, Le Fur G (1997) Selective inhibition of sucrose and alcohol intake by SR 141716, an antagonist of central cannabinoid (CB1) receptors. (springer.com)
  • This inhibition grows more pronounced when considered with the effect of activated CB 1 receptors to limit calcium entry into the cell, which does not occur through cAMP but by a direct G-protein-mediated inhibition. (wikipedia.org)
  • The activation of the CB 1 and CB 2 receptors causes the numerous intracellular effects which may be cell type and ligand specific and involve the inhibition of various voltage gated Ca +2 channels and adenylate cyclase activity and the activation of K + channels, resulting in lower levels of cAMP along with activation of MAPK pathways [ 5 ]. (hindawi.com)
  • In a mouse model for amyotrophic lateral sclerosis the application of a synthetic cannabinoid (WIN55,212-2) and the inhibition of endocannabinoid degradation delayed disease onset without affecting life span. (cannabis-med.org)
  • Lallemand F, Soubrié PH, De Witte PH (2001) Effects of CB1 cannabinoid receptor blockade on ethanol preference after chronic ethanol administration. (springer.com)
  • [4] [9] Two types of cannabinoid receptors , CB 1 and CB 2 , responsible for the effects of THC were discovered and cloned in the early 1990s. (wikipedia.org)
  • However, clinical development of several CB1 antagonists was halted due to central nervous system (CNS)-related side effects including depression and suicidal ideation in some users. (nih.gov)
  • These results suggest that SR is an effective antagonist of the psychoactive effects of cannabinoids. (springer.com)
  • CB1 receptors are present at high densities in the forebrain and cerebellum consistent with the observed effects of CBs on cognition and movement. (aspetjournals.org)
  • and the well known behavioral effects of cannabinoid agonists ( Mechoulam, 1986 ), it is likely that this receptor regulates short-term memory, coordination of movement and emotions. (aspetjournals.org)
  • The CB2 receptor may mediate some of the peripheral effects of THC, such as immunosuppression ( Martin, 1986 ). (aspetjournals.org)
  • This study investigates the effects of SR141716, a selective CB 1 receptor antagonist that reduces food intake and body weight of rodents, on Acrp30 mRNA expression in adipose tissue. (aspetjournals.org)
  • Cannabinoid type 1 (CB1) receptor antagonists have been developed for the treatment of obesity, but a major disadvantage is that they cause unwanted psychiatric effects. (aspetjournals.org)
  • Selective targeting of peripheral CB1 receptors might be an option to circumvent these side effects. (aspetjournals.org)
  • Blockade of CB1 receptor activity by genetic invalidation also decreases rewarding effects of opiates and alcohol in animals. (cannabis-marijuana.com)
  • [8] The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the immune system. (wikipedia.org)
  • In vivo administration of a specific antagonist of the CB2 cannabinoid receptor also blocked the effects of THC. (jimmunol.org)
  • Marijuana smoke produces its psychotropic effects by delivering milligram quantities of cannabinoids, including primarily Δ-9-tetrahydrocannabinol (THC), 3 to the lung ( 1 ). (jimmunol.org)
  • The recent documentation of specific cannabinoid receptor expression by leukocytes has generated increased interest in the immunomodulatory effects of THC ( 7 , 12 ). (jimmunol.org)
  • The aim of this study was to investigate which receptor subtype mediates cannabinoid effects on memory consolidation for emotionally arousing experiences. (frontiersin.org)
  • WIN55,212-22 effects on memory consolidation were predominantly mediated by CB1 receptor activation but CB2 receptors were involved as well. (frontiersin.org)
  • Our findings drive beyond the classical hypothesis centered on the unique role of CB1 receptor activation for cannabinoid effects on memory, and reveal new insights in the neural mechanisms of memory consolidation. (frontiersin.org)
  • Upon activation, CB 1 receptor exhibits its effects mainly through activation of G i , which decreases intracellular cAMP concentration by inhibiting its production enzyme , adenylate cyclase , and increases mitogen-activated protein kinase (MAP kinase) concentration. (wikipedia.org)
  • Cannabinoids produce many of their cellular and organ system effects by interacting with the well-characterized CB1 and CB2 receptors. (frontiersin.org)
  • However, it has become clear that not all effects of cannabinoid drugs are attributable to their interaction with CB1 and CB2 receptors. (frontiersin.org)
  • Although the blockade of cannabinoid type-1 receptor (CB1) had been suggested as a therapeutical means against CIAPS, the use of orthosteric CB1 receptor full antagonists is strongly limited by undesired side effects and low efficacy. (nature.com)
  • Unlike agents which activate CB1 receptors, selective CB2R receptor agonists do not have psychoactive side effects. (medindia.net)
  • They can be divided into "specific" agents, e.g., affecting an identifiable molecular mechanism unique to target cells bearing receptors for that agent, and "nonspecific" agents, those producing effects on different target cells and acting by diverse molecular mechanisms. (nih.gov)
  • Cannabinoids exert their effects through an endogenous cannabinoid system in the central and peripheral nervous system. (mdpi.com)
  • Also, these naturally derived molecules possess the least adverse effects opposed to the synthetically derived cannabinoids. (hindawi.com)
  • 5,6 Cannabinoids interact with G protein-coupled receptors to produce their effects. (ahajournals.org)
  • Not much is known, however, about the effects and mechanism of action of synthetic nonpsychotic cannabinoids on breast cancer growth and metastasis. (aacrjournals.org)
  • These effects were reversed by CB1 and CB2 antagonists AM 251 and SR144528, respectively, suggesting involvement of CB1 and CB2 receptors. (aacrjournals.org)
  • In the present study, therefore, we analyzed the effects of synthetic cannabinoids on breast cancer cells. (aacrjournals.org)
  • Although these studies point to the potential application of cannabinoids as antitumor agents in various human cancer cells, not much is known about the molecular mechanism of cannabinoid-mediated antimetastatic and tumurogenic effects. (aacrjournals.org)
  • Authors note that the demonstration of CB1 receptor effects "reinforce the importance of neuronal activation in intestinal inflammation. (cannabis-med.org)
  • Researchers suggest that the beneficial effects of cannabinoids were mediated by non-CB1 receptor mechanisms. (cannabis-med.org)
  • Findings may counter the potentially life-threatening effects of intoxication with synthetic cannabinoids. (medicalnewstoday.com)
  • In fact, the NIDA caution, the side effects of synthetic cannabinoids are often "unpredictable and, in some cases, severe or even life-threatening. (medicalnewstoday.com)
  • Synthetic cannabinoids act on the same receptor, but intoxication with these substances may have more dire effects than marijuana. (medicalnewstoday.com)
  • Experimental evidence has suggested that drugs that enhance cannabinoid type-1 (CB1) receptor activity may induce anxiolytic and antidepressant effects, whilst the opposite has been reported with antagonists. (scielo.br)
  • Patients taking CB1 receptor antagonists should be carefully investigated for psychiatric side-effects. (scielo.br)
  • CB2 receptors are found in the immune system, and CB1 receptors responsible for psychoactive effects are found in the nervous system. (worldhealth.net)
  • Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. (selleckchem.com)
  • [11] Based on computer modeling, ligand interactions with CB 2 receptor residues S3.31 and F5.46 appears to determine differences between CB 1 and CB 2 receptor selectivity. (wikipedia.org)
  • Target selectivity is defined as a difference in target binding to different receptors, and tissue selectivity is defined as a difference in target binding to the same target in different tissues. (springer.com)
  • Here, we clarified the role of the cannabinoid system in cognitive impairment during withdrawal from MDMA using the novel object recognition task. (nature.com)
  • This compound displays nanomolar affinity for the central cannabinoid receptor but is not active on the peripheral cannabinoid receptor. (nih.gov)
  • Reported here are our efforts toward developing a peripherally selective CB1 antagonist based on the otenabant scaffold. (nih.gov)
  • Our efforts have resulted in an orally absorbed compound that is a potent and selective CB1 antagonist with limited penetration into the CNS. (nih.gov)
  • have been identified, cloned and sequenced to date and are members of the superfamily of G-protein-coupled receptors. (aspetjournals.org)
  • Both CB 1 and CB 2 are 7-transmembrane G protein-coupled receptors that engage predominantly the G i/o family of G proteins. (pnas.org)
  • As is commonly seen in G protein-coupled receptors, the CB 2 receptor has seven transmembrane spanning domains, [10] a glycosylated N-terminus , and an intracellular C-terminus . (wikipedia.org)
  • The CB 1 receptor shares the structure characteristic of all G-protein-coupled receptors, possessing seven transmembrane domains connected by three extracellular and three intracellular loops, an extracellular N-terminal tail, and an intracellular C-terminal tail. (wikipedia.org)
  • [8] [9] The receptor may exist as a homodimer or form heterodimers or other GPCR oligomers with different classes of G-protein-coupled receptors . (wikipedia.org)
  • These function through two different specific cell surface G-protein coupled receptors, CB1 and CB2 ( 6 , 7 ). (aacrjournals.org)
  • CB 1 receptors are thought to be the most widely expressed G protein-coupled receptors in the brain. (thefullwiki.org)
  • Cannabinoids bind not only to classical receptors (CB1 and CB2) but also to certain orphan receptors (GPR55 and GPR119), ion channels (transient receptor potential vanilloid), and peroxisome proliferator-activated receptors. (jnccn.org)
  • [14] [15] CB 1 receptors are present in highest concentration in the brain but can also be found in the periphery. (wikipedia.org)
  • On the other hand, cannabinoid CB 1 receptors have been implicated in learning/memory, and are highly expressed in the hippocampus, a region of the brain believed to have an important function in certain forms of learning and memory. (nature.com)
  • These reports suggest that the activation of the brain cannabinoid system impairs working memory. (nature.com)
  • In a biochemical study, Gonzalez et al (2002) reported that chronic exposure to morphine increased levels of cannabinoid CB 1 receptor mRNA and CB 1 receptor binding in the brain. (nature.com)
  • LY320135 is a selective antagonist for the brain CB1 receptor, having greater than 70-fold higher affinity for the CB1 than the peripheral CB2 receptor. (aspetjournals.org)
  • The CB1 receptor is expressed in brain and peripheral tissues such as adipose, skeletal muscle, liver, gut, and pancreas ( Di Marzo, 2008 ). (aspetjournals.org)
  • In the vas deferens, it antagonized several cannabinoids more potently than THC and was also more potent against CP55940 and R -(+)-WIN55212 in this tissue than in brain membranes. (thecannabisadvisory.com)
  • The most severe neuropathological lesions observed in HD take place in the striatum, one brain area important in motor control and rich in cannabinoid receptors (CBR). (clinicaltrials.gov)
  • Endocannabinoid receptors are concentrated in the brain, but are also present in nerve tissues all over the body. (medicinenet.com)
  • Pain Sensitivity Brain-derived neurotrophic factor, or BDNF, plays a critical role in learning and memory by actions at the TrkB receptor. (drugabuse.gov)
  • Short-term studies also suggest that the drug, called taranabant--the second drug designed to fight obesity by blocking cannabinoid receptors in the brain--causes people to consume fewer calories and burn more, researchers report in the January issue of Cell Metabolism, a publication of Cell Press. (eurekalert.org)
  • To extend those findings to humans in the new studies, the researchers first used positron emission tomography (PET) imaging to identify a dose that would bind about 30 percent of cannabinoid receptors in the human brain. (eurekalert.org)
  • To date, 2 such receptors have been identified: cannabinoid-1 receptors (CB 1 ), expressed at high levels in the brain 7 but also present in peripheral tissues, including the heart 8 and the vasculature, 9,10 and CB 2 , expressed by immune and hematopoietic cells. (ahajournals.org)
  • Isolation and structure of a brain constituent that binds to the cannabinoid receptor. (currentprotocols.com)
  • The cannabinoid receptor type 1 , often abbreviated to CB 1 , is a G protein-coupled cannabinoid receptor located in the brain . (thefullwiki.org)
  • CBD targets the CB1 and CB2 receptors in the brain to alleviate different medical problems. (metrotimes.com)
  • The CB1 receptors found in a particular area of the brain called the mesolimbic system are involved in controlling our intake of highly palatable, sweet or fatty foods. (netdoctor.co.uk)
  • Within the brain, there is a highly heterogeneous distribution of CB1 receptors, as their expression is found in the cerebral cortex, globus pallidus, substantia nigra, endopeduncular nucleus, hippocampus, cerebellum, and in some parts of thalamus and amygdala (as well as in some other regions). (news-medical.net)
  • They include antagonists , inverse agonists , and antibodies of CBRs. (wikipedia.org)
  • The invention further relates to the use of these true antagonists and inverse agonists in the treatment of CB associated disorders such as obesity, psychiatric and neurological disorders. (freepatentsonline.com)
  • CB 2 receptors are mostly located in the immune and haematopoietic systems. (wikipedia.org)
  • The Endocannabinoid system with cannabinoid receptors between immune cell and neuron. (news-medical.net)
  • In contrast, the response of cells expressing the CB 2 receptor may influence not only the responses in that cell, but may alter the course of the host innate and adaptive immune response to the pathogen, suppressing inflammation and the development of virus-specific cellular and humoral responses. (mdpi.com)
  • The CB2 receptor on the other hand is found predominantly in cells of the immune system, spleen, lymph nodes but has very low or undetectable expression levels in the CNS under basal conditions [ 6 , 7 ]. (mdpi.com)
  • The CB1 receptor is predominantly expressed in the central nervous system, whereas the CB2 receptor is expressed by immune cells. (aacrjournals.org)
  • There was a high number of CB2 receptors in immune cells that infiltrated the inflamed tissue. (cannabis-med.org)
  • This study compares newly discovered structures to those of the CB1 receptor, and deems the two receptors to be the Yin and Yang of the human endocannabinoid system, which is a signalling system that regulates biological processes such as pain, immune function, metabolism, and neuronal activities among others. (worldhealth.net)
  • On the other hand, CB2 receptors are predominantly found on immune cells (most notably natural killer cells and B-cells), where they play an important role in modulating cytokine release in both health and disease. (news-medical.net)
  • Few other modifications, such as the addition of an amide group along with the 1-adamantyl group at C-3 position and stabilization of the ligand-CB2 receptor increased the affinity of the antagonist for CB2 and also promoted CB2 crystals. (news-medical.net)
  • CB2 has a strong electron density in the ligand-binding pocket that determines the placement of the antagonist. (news-medical.net)
  • [5] [7] The principal endogenous ligand for the CB 2 receptor is 2-arachidonoylglycerol (2-AG). (wikipedia.org)
  • A promising 2-oxoquinoline derivative designated KP23 was synthesized and radiolabeled and its potential as a ligand for PET imaging the CB2 receptor was evaluated. (mdpi.com)
  • Relationships between ligand affinities for the cerebellar cannabinoid receptor CB1 and the induction of GDP/GTP exchange. (currentprotocols.com)
  • Durnett-Richardson J, Aanonsen L, Groves N, Jackson D, Hargreaves K (1995) Involvement of the spinal cannabinoid receptor in nociception. (springer.com)
  • 1995), receptors responsible for their signaling (Devane et al. (420magazine.com)
  • Spicing things up: synthetic cannabinoids. (nature.com)
  • Currently, there are three general types of cannabinoids: phytocannabinoids, and endogenous and synthetic cannabinoids. (aacrjournals.org)
  • More and more people are turning to synthetic cannabinoids, or "legal highs," as an alternative to marijuana. (medicalnewstoday.com)
  • Additionally, it has been reported that the number of deaths related to the use of synthetic cannabinoids has tripled in recent years, and the Centers for Disease Control and Prevention (CDC) have referred to the substances as an "emerging public health threat. (medicalnewstoday.com)
  • In general, increasing the length and bulk of the substituent was associated with increased receptor affinity and efficacy (as measured in a guanosine 5'-triphosphate-gamma-[S-35] assay). (elsevier.com)
  • However, in most instances, receptor affinity and efficacy increases were no longer observed after a certain chain length was reached. (elsevier.com)
  • An investigation of the efficacy of cannabinoids in treating insomnia in chronic, non-malignant pain patients is therefore warranted. (clinicaltrials.gov)
  • 3,5 However, an increase in the hypotensive efficacy of cannabinoids has been noted in spontaneously hypertensive rats (SHR). (ahajournals.org)
  • It has been suggested that GPR55 is a novel cannabinoid receptor (reviewed in ref. 4 ). (pnas.org)
  • Currently two subtypes of cannabinoid receptors have been isolated and cloned: CB1 and CB2. (mdpi.com)
  • In this study, we clarified the mechanism underlying the cognitive impairment that develops during MDMA withdrawal from the standpoint of the cannabinoid CB 1 receptors. (nature.com)
  • The impairment of recognition memory during withdrawal from MDMA may result from the activation of cannabinoid CB 1 receptors in the hippocampus. (nature.com)
  • Activation of GPR55 by Cannabinoids Increases Intracellular Calcium. (pnas.org)
  • [12] These interactions induce a conformational change in the receptor structure, which triggers the activation of various intracellular signaling pathways. (wikipedia.org)
  • [16] Activation of the MAPK-ERK pathway by CB 2 receptor agonists acting through the G βγ subunit ultimately results in changes in cell migration [17] as well as in an induction of the growth-related gene Zif268 (also known as Krox-24, NGFI-A, and egr-1). (wikipedia.org)
  • The URB597-induced memory enhancement was dependent on the activation not only of CB1 and CB2 receptors but, notwithstanding, PPAR-α and TRPV1 receptors were involved as well. (frontiersin.org)
  • Alternatively, in some rare cases CB 1 receptor activation may be coupled to G s proteins, which stimulate adenylate cyclase . (wikipedia.org)
  • Transient endocannabinoid release is triggered by voltage-dependent Ca 2+ influx and is upregulated by group I metabotropic glutamate receptor activation. (jneurosci.org)
  • Here we show that muscarinic acetylcholine receptor (mAChR) activation also enhances transient endocannabinoid release (DSI) and induces persistent release. (jneurosci.org)
  • Activation of these receptors by endogenous cannabinoids, such as anadamide, increases appetite. (drugdevelopment-technology.com)
  • Activation of peripheral CB1 receptors contributes to hemorrhagic and endotoxin -induced hypotension . (thefullwiki.org)
  • At this time, the level of cannabinoid CB 1 receptor protein increased significantly in the hippocampus but not the prefrontal cortex or striatum. (nature.com)
  • CP-945598 HCl inhibits CB 1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. (selleckchem.com)
  • [1] CP-945598 HCl has low affinity with K i of 7.6 μM for human CB 2 receptors. (selleckchem.com)
  • The corresponding amide analogues were compared to the hydrazides to determine the effect of the second nitrogen on receptor binding affinity. (elsevier.com)
  • 2) or the antagonist [H-3]5, 14 exhibited the highest CB, affinity. (elsevier.com)