Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Receptors, Cannabinoid: 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.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Receptor, Cannabinoid, CB2: A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.Benzoxazines: OXAZINES with a fused BENZENE ring.Cyclohexanols: 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.Naphthalenes: 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.Cannabinoid Receptor Antagonists: Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.Dronabinol: 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.Cannabinoid Receptor Modulators: Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS.Receptors, Drug: 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.MorpholinesEndocannabinoids: 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.Pyrazoles: 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.Polyunsaturated Alkamides: 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.Piperidines: A family of hexahydropyridines.BornanesArachidonic AcidsAnalgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Glycerides: GLYCEROL esterified with FATTY ACIDS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.AmidohydrolasesRats, Sprague-Dawley: 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.Cannabidiol: Compound isolated from Cannabis sativa extract.Pain: An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.Calcium Channel Blockers: A class of drugs that act by selective inhibition of calcium influx through cellular membranes.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Monoacylglycerol Lipases: An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23.Synaptic Transmission: 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.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Pain Measurement: 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.Mice, Inbred C57BLSerotonin Receptor Agonists: 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.Neurons: 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.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Signal Transduction: 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.Cannabinol: A physiologically inactive constituent of Cannabis sativa L.Cannabis: 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.Serotonin 5-HT1 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.Cells, Cultured: 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.Disease Models, Animal: 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.Serotonin 5-HT2 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Ligands: 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)Indoles: 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.Receptors, Opioid, mu: 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.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Guanosine 5'-O-(3-Thiotriphosphate): 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.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).Receptors, Opioid, kappa: 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.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Mice, Knockout: 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.CHO Cells: 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.GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.Behavior, Animal: The observable response an animal makes to any situation.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.Drug Inverse Agonism: 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.Brain: 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.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Carbamates: 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.Hippocampus: 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.Ethanolamines: AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.TRPV Cation Channels: 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.Receptors, Opioid: 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.Cyclic AMP: 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.Benzodioxoles: Compounds based on benzene fused to oxole. They can be formed from methylated CATECHOLS such as EUGENOL.Receptors, Dopamine D2: 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.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.ResorcinolsBinding, Competitive: 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.Pertussis Toxin: 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.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.Hallucinogens: 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.Histamine Agonists: Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.Mice, Inbred ICRMotor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Drug Tolerance: 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.Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Hyperalgesia: 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.Cyclohexanes: Six-carbon alicyclic hydrocarbons.Patch-Clamp Techniques: 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.

Cannabinoid receptor activation in the rostral ventrolateral medulla oblongata evokes cardiorespiratory effects in anaesthetised rats. (1/177)

1. The nature of the cardiorespiratory effects mediated by cannabinoids in the hindbrain is poorly understood. In the present study we investigated whether cannabinoid receptor activation in the rostral ventrolateral medulla oblongata (RVLM) affects cardiovascular and/or respiratory function. 2. Initially, we looked for evidence of CB1 receptor gene expression in rostral and caudal sections of the rat ventrolateral medulla (VLM) using reverse transcription-polymerase chain reaction. Second, the potent cannabinoid receptor agonists WIN55,212-2 (0.05, 0.5 or 5 pmol per 50 nl) and HU-210 (0.5 pmol per 50 nl) or the CB1 receptor antagonist/inverse agonist AM281 (1 pmol per 100 nl) were microinjected into the RVLM of urethane-anaesthetised, immobilised and mechanically ventilated male Sprague-Dawley rats (n=22). Changes in splanchnic nerve activity (sSNA), phrenic nerve activity (PNA), mean arterial pressure (MAP) and heart rate (HR) in response to cannabinoid administration were recorded. 3. The CB1 receptor gene was expressed throughout the VLM. Unilateral microinjection of WIN55,212-2 into the RVLM evoked short-latency, dose-dependent increases in sSNA (0.5 pmol; 175+/-8%, n=5) and MAP (0.5 pmol; 26+/-3%, n=8) and abolished PNA (0.5 pmol; duration of apnoea: 5.4+/-0.4 s, n=8), with little change in HR (P<0.005). HU-210, structurally related to Delta9-tetrahydrocannabinol (THC), evoked similar effects when microinjected into the RVLM (n=4). Surprisingly, prior microinjection of AM281 produced agonist-like effects, as well as significantly attenuated the response to subsequent injection of WIN55,212-2 (0.5 pmol, n=4). 4. The present study reveals CB1 receptor gene expression in the rat VLM and demonstrates sympathoexcitation, hypertension and respiratory inhibition in response to RVLM-administered cannabinoids. These findings suggest a novel link between CB1 receptors in this region of the hindbrain and the central cardiorespiratory effects of cannabinoids. The extent to which these central effects contribute to the cardiovascular and respiratory outcomes of cannabis use remains to be investigated.  (+info)

Involvement of cannabinoid receptors in gut motility and visceral perception. (2/177)

From a historical perspective to the present day, all the evidence suggests that activation of cannabinoid receptors (CBRs) is beneficial for gut discomfort and pain, which are symptoms related to dysmotility and visceral perception. CBRs comprise G-protein coupled receptors that are predominantly in enteric and central neurones (CB1R) and immune cells (CB2R). In the last decade, evidence obtained from the use of selective agonists and inverse agonists/antagonists indicates that manipulation of CB1R can alter (1) sensory processing from the gut, (2) brain integration of brain-gut axis, (3) extrinsic control of the gut and (4) intrinsic control by the enteric nervous system. The extent to which activation of CB1R is most critical at these different levels is related to the region of the GI tract. The upper GI tract is strongly influenced by CB1R activation on central vagal pathways, whereas intestinal peristalsis can be modified by CB1R activation in the absence of extrinsic input. Actions at multiple levels make the CB1R a target for the treatment of functional bowel disorders, such as IBS. Since low-grade inflammation may act as a trigger for occurrence of IBS, CB2R modulation could be beneficial, but there is little supporting evidence for this yet. The challenge is to accomplish CBR activation while minimizing adverse effects and abuse liabilities. Potential therapeutic strategies involve increasing signaling by endocannabinoids (EC). The pathways involved in the biosynthesis, uptake and degradation of EC provide opportunities for modulation of CB1R and some recent evidence with inhibitors of EC uptake and metabolism suggest that these could be exploited for therapeutic gain.  (+info)

Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons. (3/177)

The prototypical aminoalkylindole cannabinoid WIN 55,212-2 (WIN-2) has been shown to produce antihyperalgesia through a peripheral mechanism of action. However, it is not known whether WIN-2 exerts this action directly via cannabinoid receptors located on primary afferents or if other, perhaps indirect or noncannabinoid, mechanisms are involved. To address this question, we have examined the specific actions of WIN-2 on trigeminal ganglion (TG) neurons in vitro by quantifying its ability to modulate the evoked secretion of the proinflammatory neuropeptide CGRP as well as the inflammatory mediator-induced generation of cAMP. WIN-2 evoked CGRP release from TG neurons in vitro (EC(50)=26 microm) in a concentration- and calcium-dependent manner, which was mimicked by the cannabinoid receptor-inactive enantiomer WIN 55,212-3 (WIN-3). Moreover, WIN-2-evoked CGRP release was attenuated by the nonselective cation channel blocker ruthenium red but not by the vanilloid receptor type 1 (TRPV1) antagonist capsazepine, suggesting that, unlike certain endogenous and synthetic cannabinoids, WIN-2 is not a TRPV1 agonist but rather acts at an as yet unidentified cation channel. The inhibitory effects of WIN-2 on TG neurons were also examined. WIN-2 neither inhibited capsaicin-evoked CGRP release nor did it inhibit forskolin-, isoproteranol- or prostaglandin E(2)-stimulated cAMP accumulation. On the other hand, WIN-2 significantly inhibited (EC(50)=1.7 microm) 50 mm K(+)-evoked CGRP release by approximately 70%. WIN-2 inhibition of 50 mm K(+)-evoked CGRP release was not reversed by antagonists of cannabinoid type 1 (CB1) receptor, but was mimicked in magnitude and potency (EC(50)=2.7 microm) by its cannabinoid-inactive enantiomer WIN-3. These findings indicate that WIN-2 exerts both excitatory and inhibitory effects on TG neurons, neither of which appear to be mediated by CB1, CB2 or TRPV1 receptors, but by a novel calcium-dependent mechanism. The ramifications of these results are discussed in relation to our current understanding of cannabinoid/vanilloid interactions with primary sensory neurons.  (+info)

Central effects of the cannabinoid receptor agonist WIN55212-2 on respiratory and cardiovascular regulation in anaesthetised rats. (4/177)

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. (5/177)

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)

Long-lasting increase of alcohol relapse by the cannabinoid receptor agonist WIN 55,212-2 during alcohol deprivation. (6/177)

Alcoholism is characterized by successive relapses. Recent data have shown a cross-talk between the cannabinoid system and ethanol. In this study, male Wistar rats with a limited (30 min sessions), intermittent, and extended background of alcohol operant self-administration were used. The relapse to alcohol after 1 week of alcohol deprivation was evaluated. Two weeks later, the animals were treated with the cannabinoid agonist WIN 55,212-2 (R-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxa zin-6-yl]-1-naphthalenylmethanone mesylate) (0, 0.4, 2.0, and 10.0 mg/kg, s.c.) during a similar alcohol deprivation period, and alcohol relapse during 2 weeks was assessed. A conditioned place preference (CPP) paradigm was used to study the rewarding properties of the cannabinoid agonist. Locomotor activity was also recorded. All doses of WIN 55,212-2 produced aversion in the CPP paradigm. The doses of 2.0 and 10.0 mg/kg resulted in an important suppression of spontaneous locomotor activity and a progressive weight loss during the next 2 weeks. The single alcohol deprivation was followed by a transient increase in their responding for alcohol from a range of 20-24 lever presses at baseline to a range of 38-48 responses in the first and second days (alcohol deprivation effect). However, the administration of WIN 55,212-2 during ethanol deprivation produced similar increased responses for alcohol but in a long-term way (at least over 2 weeks). These findings suggest that noncontingent chronic exposure to cannabinoids during alcohol deprivation can potentiate the relapse into alcohol use, indicating that functional changes in the cannabinoid brain receptor may play a key role in ethanol relapse.  (+info)

2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand, induces rapid actin polymerization in HL-60 cells differentiated into macrophage-like cells. (7/177)

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)

The endocannabinoid system: physiology and pharmacology. (8/177)

The endogenous cannabinoid system is an ubiquitous lipid signalling system that appeared early in evolution and which has important regulatory functions throughout the body in all vertebrates. The main endocannabinoids (endogenous cannabis-like substances) are small molecules derived from arachidonic acid, anandamide (arachidonoylethanolamide) and 2-arachidonoylglycerol. They bind to a family of G-protein-coupled receptors, of which the cannabinoid CB(1) receptor is densely distributed in areas of the brain related to motor control, cognition, emotional responses, motivated behaviour and homeostasis. Outside the brain, the endocannabinoid system is one of the crucial modulators of the autonomic nervous system, the immune system and microcirculation. Endocannabinoids are released upon demand from lipid precursors in a receptor-dependent manner and serve as retrograde signalling messengers in GABAergic and glutamatergic synapses, as well as modulators of postsynaptic transmission, interacting with other neurotransmitters, including dopamine. Endocannabinoids are transported into cells by a specific uptake system and degraded by two well-characterized enzymes, the fatty acid amide hydrolase and the monoacylglycerol lipase. Recent pharmacological advances have led to the synthesis of cannabinoid receptor agonists and antagonists, anandamide uptake blockers and potent, selective inhibitors of endocannabinoid degradation. These new tools have enabled the study of the physiological roles played by the endocannabinoids and have opened up new strategies in the treatment of pain, obesity, neurological diseases including multiple sclerosis, emotional disturbances such as anxiety and other psychiatric disorders including drug addiction. Recent advances have specifically linked the endogenous cannabinoid system to alcoholism, and cannabinoid receptor antagonism now emerges as a promising therapeutic alternative for alcohol dependence and relapse.  (+info)

PubMed journal article The cannabinoid receptor agonist WIN 55,212-2 inhibits antigen-induced plasma extravasation in guinea pig airway were found in PRIME PubMed. Download Prime PubMed App to iPhone, iPad, or Android
33. The method of claim 32, wherein the CB-2 receptor inverse agonist comprises a compound of ##STR00190## wherein D and D are independently --H, --OH, --ORa, (C1-C6)alkyl or ##STR00191## Ra, Ra, and Ra are independently selected from the group consisting of H, straight or branched chain (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C14)aryl, (C3-C14)hetero cyclo alkyl-(C1-C6)alkylene-, (C3-C14)hetero aryl-(C1-C6)alkylene-, or (C3-C14)aryl(C1-C6)alkylene-; A, B and Q are each independently (C1-C6)alkylene, (C2-C6)alkenylene or (C2-C6)alkynylene, e, f and g independently are integers between 0 and 6 inclusive; V, W, X, Y, and Z are each independently a bond, --C(R)2--, --CR--, --NR--, --N--, --O--, --C(O)--, or --S--, wherein no two adjacent members of V, W, X, Y, and Z are simultaneously --O--, --S--, or --NR--; R is H, --OH, --ORa, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, (C1-C6)haloalkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, --NH2, --NH(C1-C6)alkyl, --N[(C1-C6)alkyl]2, ...
Evidence from in vitro and in vivo experiments suggests that cannabinoid receptor agonists can reduce tumor growth and induce apoptosis in several tumor types, including melanoma, breast and prostate cancer, colon cancer, leukemia, and glioma. However, to our knowledge, the response to cannabinoid treatment has not been studied in sarcomas yet. Here, we investigated the effects of cannabinoid receptor agonists in the sarcoma tposRMS, which we not only confirmed to express high levels of CB1 mRNA but also showed expression on the protein level by Western blot and immunohistochemistry.. In vitro, cannabinoid receptor agonists HU210, THC, and Met-F-AEA exerted an antiproliferative and proapoptotic action on tposRMS cells through activation of the CB1 receptor. The specificity of this effect for CB1 was shown by two means: First, the cell viability in fibroblasts or tnegRMS control cell lines, which express only low levels of CB1, is not affected. Second, the CB1-specific antagonist AM251 was able ...
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.
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 ...
3. S. Ghosh, A. Preet, J.E. Groopman, and R.K. Gaju, "Cannabinoid Receptor CB 2 Modulates the CXCL 12/ CXCR 4-Mediated Chemotaxis of T Lymphocytes," Molecular Immunology, Vol. 43 (2006); A. Preet, R.K. Ganju, and J.E. Groopman, "∆ 9 -Tetrahydrocannabinol Inhibits Epithelial Growth Factor-Induced Lung Cancer Cell Migration in Vitro as Well as Its Growth and Metastasis in Vivo," Oncogene, Vol. 27 (2008); X. Zhang, Y. Maor, J.F. Wang, G. Kunos, and J.E. Groopman, "Endocannabinoid-like N-arachidonoyl Serine Is a Novel Pro-angiogenic Mediator," British Journal of Pharmacology, Vol. 160 (2010); A. Preet, Z. Qamri, M. Nasser, A. Prasad, K. Shilo, X. Zou, J.E. Groopman, and R. Ganju, "Cannabinoid Receptors, CB 1 and CB 2, as Novel Targets for Inhibition of Non-Small Cell Lung Cancer Growth and Metastasis," Cancer Prevention Research, Vol. 4 (2011); A. Shrivastava, P.M. Kuzontkoski, J.E. Groopman, and A. Prasad, "Cannabidiol Induces Programmed Cell Death in Breast Cancer Cells by Coordinating the ...
The cannabinoid receptor agonist WIN 55,212-2 reduces the initial cerebral damage after hypoxic-ischemic injury in fetal lambs. Alonso-Alconada D,
Hello Again, I have a couple more days of leveling left for our 15x48 intex. Upon your advice, Im going with the Krysatl Clear SWS. My wife just picked up the 14 Intex 1600 GPH sand filter. I just noticed a sale on the Intex 2650 GPH sand filter, with a price differance of only about $20. Do you guys think I should upgrade to the big guy, or is it just too much on my 15x48? (Which I think is approx 4400 gallons.) Thanks again!
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 ...
G protein-coupled receptor 119 also known as GPR119 is a G protein-coupled receptor that in humans is encoded by the GPR119 gene. GPR119, along with GPR55 and GPR18, have been implicated as novel cannabinoid receptors. GPR119 is expressed predominantly in the pancreas and gastrointestinal tract in rodents and humans, as well as in the brain in rodents. Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats. GPR119 has also been shown to regulate incretin and insulin hormone secretion. As a result, new drugs acting on the receptor have been suggested as novel treatments for obesity and diabetes. A number of endogenous and synthetic ligands for this receptor have been identified: 2-Oleoylglycerol Anandamide AR-231,453 MBX-2982 Oleoylethanolamide (Endogenous Ligand) PSN-375,963 PSN-632,408 GRCh38: Ensembl release 89: ENSG00000147262 - Ensembl, May 2017 GRCm38: Ensembl release 89: ENSMUSG00000051209 - Ensembl, May 2017 "Human PubMed Reference:". ...
The IP Industry Base is a public available database about the global market of IP practitioners. Currently is provides high-quality profiles of more than 4900 companies, 15620 professionals and 4260 places. The service of the IP Industry Base is dedicated to technology managers, IP professionals and IPR academia. The open data of the IP Industry Base aims to create transparency for the market of IP practitioners.
Aminoalkylindoles (AAIs) are a family of cannabinergic compound that act as a cannabinoid receptor agonist. They were invented by pharmaceutical company Sterling-Winthrop in the early 1990s as potential nonsteroidal anti-inflammatory agents. Aminoalkylindole are now commonly found in synthetic cannabis designer drugs. In the United States, the DEA added the aminoalkylindole JWH-200 to Schedule I of the Controlled Substances Act on 1 March 2011 for 12 months. Emmanuel S. Onaivi (2006). Marijuana and Cannabinoid Research: Methods and Protocols. Springer. pp. 128-. ISBN 978-1-59259-999-8. "Synthetic Cannabinoids". American Association for Clinical Chemistry. 2013-02-01. Retrieved 2013-11-17. "Schedules of Controlled Substances: Temporary Placement of Five Synthetic Cannabinoids Into Schedule I". Federal Register. 2011-03-01. Retrieved 2013-11-17. Aminoalkylindoles, ...
Oral malignancies can be associated with increased pain, but current research suggests that a cannabis-based spray may reduce this morbidity.
Cannabis sativa is also popularly known as marijuana. It is being cultivated and used by man for recreational and medicinal purposes from many centuries.. Study of cannabinoids was at bay for very long time and its therapeutic value could not be adequately harnessed due to its legal status as proscribed drug in most of the countries.. The research of drugs acting on endocannabinoid system has seen many ups and down in recent past. Presently, it is known that endocannabinoids has role in pathology of many disorders and they also serve "protective role" in many medical conditions.. Several diseases like emesis, pain, inflammation, multiple sclerosis, anorexia, epilepsy, glaucoma, schizophrenia, cardiovascular disorders, cancer, obesity, metabolic syndrome related diseases, Parkinsons disease, Huntingtons disease, Alzheimers disease and Tourettes syndrome could possibly be treated by drugs modulating endocannabinoid system.. Presently, cannabinoid receptor agonists like nabilone and dronabinol ...
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
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
cell loss following experimentally induced stroke. We have recently reported that myocardial infarct size, as well as necroapoptosis and inflammation in
tudy This study Our stock This study This study This study This study This study Y. Ma et al., This study Y Ma et al., This study This study This study This
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.
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 ...
Greenmedinfo.com - Natural Health Resource - The worlds most widely referenced, open access, natural medicine database, with 30,000+ study abstracts and growing daily
Side effects of dronabinol include a sudden feeling of warmth, memory loss, hallucination and lack of balance, states Everyday Health. Doctors prescribe dronabinol on the basis that its benefits...
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. ...
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 ...
Mitragynine is structurally related to both the yohimbe alkaloids and voacangine. It is more distantly related to other tryptamine-based psychedelic drugs such as psilocybin and LSD. In low doses Kratom has a stimulating effect producing heightened energy and an increase in the ability to concentrate. Kratom is legal everywhere except in Thailand where its possession until recently was punishable by death. The government has declared that it may now be used in the treatment of opiate addiction and depression. The dosage for preparations using the dried leaf is 3 to 5 grams and less if smoked.. New York NY USA: Tayor and Francis 2010; pp. The cannabinoid receptor agonist WIN 55212-2 mesylate blocks the development of hyperalgesia produced by capsaicin in rats. WIN 55212-2 mesylate a high affinity cannabinoid agonist in a rat model of neuropathic pain. The neurobiology of cannabinoid analgesia. Synergistic interactions between cannabinoid and opioid analgesics. Interactions between delta ...
TY - PAT. T1 - 1,5-diaryl-pyrazoles as cannabinoid receptor neutral antagonists useful as therapeutic agents. AU - Greig, Iain Robert. AU - Ross, Ruth Alexandra. AU - Pertwee, Roger Guy. PY - 2008/8/21. Y1 - 2008/8/21. N2 - 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. The present invention also pertains to the use of such compounds in the treatment of diseases and disorders that are ameliorated by treatment with a neutral antagonist of the cannabinoid type 1 (CB1) receptor, for example: an eating disorder; obesity; a disease or disorder characterised by an addiction component; addiction; withdrawal; smoking addiction; smoking withdrawal; drug addiction; drug withdrawal; smoking cessation therapy; a bone disease or disorder; osteoporosis, Pagets disease of bone; bone related cancer; a disease or disorder with an inflammatory or autoimmune component; ...
We have investigated the adaptive changes of the human central cannabinoid receptor (CB1) stably expressed in Chinese hamster ovary cells (CHO-CB1), after agonist (CP 55,940) or selective CB1 inverse agonist (SR 141716) treatment. CB1 receptor density and affinity constant as measured by binding assays with both tritiated ligands remained essentially unchanged after varying period exposure of CHO-CB1 cells (from 30 min to 72 hr) to saturating concentrations of CP 55,940 or SR 141716. However, using a C-myc-tagged version of the CB1 receptor, FACS analysis and confocal microscopy studies on CB1 expression indicated that the agonist promoted a disappearance of cell surface receptor although inverse agonist increased its cell surface density. Taken together these results suggest that 1) agonist induces internalization of the receptor into a cellular compartment that would be still accessible to both the hydrophobic ligands CP 55,940 or SR 141716; 2) inverse-agonist promotes externalization of the ...
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 …
Nonmelanoma skin cancer is one of the most common malignancies in humans. Different therapeutic strategies for the treatment of these tumors are currently being investigated. Given the growth-inhibiting effects of cannabinoids on gliomas and the wide tissue distribution of the two subtypes of cannabinoid receptors (CB1 and CB2), we studied the potential utility of these compounds in anti-skin tumor therapy. Here we show that the CB1 and the CB2 receptor are expressed in normal skin and skin tumors of mice and humans. In cell culture experiments pharmacological activation of cannabinoid receptors induced the apoptotic death of tumorigenic epidermal cells, whereas the viability of nontransformed epidermal cells remained unaffected. Local administration of the mixed CB1/CB2 agonist WIN-55,212-2 or the selective CB2 agonist JWH-133 induced a considerable growth inhibition of malignant tumors generated by inoculation of epidermal tumor cells into nude mice. Cannabinoid-treated tumors showed an ...
Pharmaxis in Australia was actively engaged in a research programme focused on developing orally-available, synthetic selective cannabinoid receptor ligands,
Host: Core A (Dr. Sean Xie group), CVS Conference Room, School of Pharmacy, UPitt. Research Progress Update/Demonstration: Yan Zhang (master student) gave a talk titled as "Modeling Simulation on Cannabinoid Receptor CB2 Signaling Pathway via Desensitization and Resensitization" Yan Zhang integrated several models, including the previously reported cubic ternary complex (CTC) model with new component updated for the CB2 desensitization and resensitization kinetics.. Dr. Zhiwei Feng (Research Associate) gave a talk titled as "Computer Modeling of 3D Structures of Cannabinoid Receptor Subtype CB2 activated through G-protein Coupling Process" Dr. Feng presented the work on the influence of agonist and inverse agonist on the inactive and active state of CB2 from conformation to drug discovery. Dr. Feng also talked about the γ-secretase project for identifying the binding pocket with the DruGui program developed by Dr. Bahars group. γ-secretase is a potential target for Alzheimers ...
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.. ...
Abstract The possible role of the CB2 receptor (CB2r) in psychiatric disorders has been considered. Several animal models use knockout (KO) mice that...
Fenofibrate, a common treatment for high cholesterol, may stimulate the same receptors as cannabinoids, which could lead to a new class of drugs.
Structure, properties, spectra, suppliers and links for: 2-(3-Hydroxyphenyl)-3-(4-morpholinylmethyl)-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-diox.
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.
According to researchers at the University of Colorado Anschutz Medical Campus, cannabinoids contain anti-inflammatory properties that could make them useful to medically treat a wide-range of skin diseases.
The aim of this research project is to develop peripherally restricted cannabinoid receptor 1 (CB1R) antagonists for alcoholic steatosis. Alcohol abuse has detr...
Finally, we used the model predictions to understand which mechanisms could explain the effect of GABA on STDP rules. For this purpose, we first implemented the model by exploring the signaling pathways involved in the reversed STDP in GABAAR blockade conditions. It has been shown previously that for corticostriatal STDP, LTP is dependent on NMDAR activation and LTD relies on type-1 cannabinoid receptor (CB1R) activation (Adermark and Lovinger, 2007; Shen et al., 2008; Fino et al., 2010). Interestingly, the signaling pathways required for STDP induction were similar in control and GABAAR blockade conditions (Fig. 8). LTP induced by post-pre pairings in control or pre-post pairings with PTX (50 μm) were NMDAR activation dependent, because they were blocked by D-AP5, an NMDAR blocker (50 μm, n = 5 for post-pre pairings in control and n = 6 for pre-post pairings with PTX; Fig. 8A). Indeed, when D-AP5 was applied together with PTX, pre-post pairings did not induce LTP anymore (111.3 ± 7.7%, p , ...
Buy dronabinol.online no script - Aldactone | Buy Online Without A Prescription And No Membership.... Revitol Stretch Mark Removal.
Endogenous cannabinoid receptor ligands (endocannabinoids) such as anandamide and 2-arachidonoyl glycerol have been isolated20,70 and are able to bind and
Previous experiments have shown that LTP of field potential recordings in the hippocampus is blocked by cannabinoid receptor activation (Nowicky et al., 1987; Collins et al., 1994, 1995; Terranova et al., 1995). This inhibition could be caused by a direct effect on the protein(s) involved in long-term synaptic plasticity. Activation of cannabinoid receptors has been found to inhibit the production of cAMP via activation of a G-protein to which the receptor is coupled (Bidaut-Russell et al., 1990; Deadwyler et al., 1995). This decrease in cAMP could, in turn, reduce the activity of cAMP-dependent protein kinase, which has been identified as an important modulator of LTP (Brandon et al., 1997). Other direct effects on proteins involved in LTP and LTD are possible. However, cannabinoid receptor-mediated G-protein activation is also known to inhibit release of neurotransmitter in cultured hippocampal neurons (Shen et al., 1996). To determine whether cannabinoid receptor activation inhibits long-term ...
Title:Latest Progress in the Identification of Novel Synthetic Ligands for the Cannabinoid CB2 Receptor. VOLUME: 14 ISSUE: 5. Author(s):Shuang Han, Jiong-Jiong Chen and Jian-Zhong Chen. Affiliation:College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Rd, Hangzhou 310058, Zhejiang, P. R. China.. Keywords:Cannabinoid receptors, CB2, GPCRs, selective ligand, structure-activity relationship.. Abstract:Cannabinoid receptors, belonging to the superfamily of G-protein coupled receptors, play a major role in pathophysiology of a wide range of disparate diseases. Cannabinoid CB2 receptor, which mainly locates in peripheral tissues, represents as a promising drug target for the treatment of pain, osteoporosis, liver disorders, and so on without serious CNS side effects. In the past decades, the identification and optimization of selective ligands for the CB2 receptor has been a major objective in drug discovery. In the present review, we describe recent advances in the development of ...
Basal Ganglia. CB1 receptors are expressed throughout the basal ganglia and have well established effects on movement in rodents. As in the hippocampus, these receptors inhibit the release of glutamate or GABA transmitter, resulting in decreased excitation or reduced inhibition based on the cell they are expressed in. Consistent with the variable expression of both excitatory glutamate and inhibitory GABA interneurons in both the basal ganglias direct and indirect motor loops, synthetic cannabinoids are known to influence this system in a dose-dependent triphasic pattern. Decreased locomotor activity is seen at both higher and lower concentrations of applied cannabinoids, while an enhancement of movement may occur upon moderate dosages. However, these dose-dependent effects have been studied predominately in rodents and the physiological basis for this triphasic pattern warrants future research in humans. Effects may vary based on the site of cannabinoid application, input from higher cortical ...
With Sativex approved in a number of countries and expected to find approval in many more in the coming months, the concept of cannabinoid medicine has been proved as more than a kooky herbal remedy. "The Sativex approval has validated the platform; it says you can make a medicine out of these materials and in this way. So big pharma have said, Fine, thats great; now we understand. I think that you will find a lot more interest in the cannabinoid system now that Sativex has been approved.". So what is the current state of cannabinoid research? As the head of one of the worlds leading cannabinoid research groups, Guy is well-positioned to comment. One of his fundamental tasks is to debunk the myths and preconceptions about this emerging area of science. "We have to take more care to provide far more fundamental data than if wed just invented a molecule and said, Look, this is what it does, please accept it. So there is an education process. And its very cultural, very different throughout ...
The aim of this study was to determine if the neutral cannabinoid CB₁ receptor antagonist, AM4113, regulates body weight in the rat via changes in food intake. We confirmed that the AM4113-induced reduction in food intake is mediated by CB₁ recep
PRF readers can get free access to a selected Journal of Pain paper each month, thanks to the American Pain Society. Get the free full text of the selection from the December 2017 issue here.. ...
Exogenous cannabinoids or receptor antagonists may influence many cellular and systemic host responses. The anti-inflammatory activity of cannabinoids may compromise host inflammatory responses to acute viral infections, but may be beneficial in persistent infections. In neurons, where innate antiviral/pro-resolution responses include the activation of NOS-1, inhibition of Ca2+ activity by cannabinoids, increased viral replication and disease. This review examines the effect(s) of cannabinoids and their antagonists in viral infections.
Researchers report the love hormone, oxytocin, could enhance the pleasure of social interactions be stimulating the production of anandamide.... Read More... ...
This meta-analysis is open to some biases, and they all have the potential to overestimate the efficacy and to underestimate the harm of cannabinoids. The trials we included were of acceptable quality according to the Oxford quality scale, with 25 of 30 trials scoring 3 or 4. In 70% of trials an adequate method of blinding was described. Most crossover trials used a double dummy design. Cannabinoids were given as tablets or intramuscular injection, so any psychological effect of smoking a joint was not a factor. However, cannabinoids showed specific adverse effects that control treatments did not, and their incidence was high. In one trial of oral nabilone, many patients identified which drug they received because of the adverse effects experienced.59 In a series of 100 blinded dronabinol and placebo treatments, nurses correctly identified the active treatment in 85% and patients in 95%; seven of the 10 errors were made by patients on the first drug trial of the study.63 We must therefore assume ...
This meta-analysis is open to some biases, and they all have the potential to overestimate the efficacy and to underestimate the harm of cannabinoids. The trials we included were of acceptable quality according to the Oxford quality scale, with 25 of 30 trials scoring 3 or 4. In 70% of trials an adequate method of blinding was described. Most crossover trials used a double dummy design. Cannabinoids were given as tablets or intramuscular injection, so any psychological effect of smoking a joint was not a factor. However, cannabinoids showed specific adverse effects that control treatments did not, and their incidence was high. In one trial of oral nabilone, many patients identified which drug they received because of the adverse effects experienced.59 In a series of 100 blinded dronabinol and placebo treatments, nurses correctly identified the active treatment in 85% and patients in 95%; seven of the 10 errors were made by patients on the first drug trial of the study.63 We must therefore assume ...
Dr. Saoirse OSullivan is a leading researcher in the field of cannabinoid research. Awarded the title of International Cannabinoid Research Society Young Investigator of the Year in 2016, Dr OSullivan has published numerous papers on the role of cannabinoid receptors in health and disease. SelectScience spoke to Dr OSullivan to find out more about her work.
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…
Kat Arney July 4, 2014 Additional information:. We often see websites with long lists of scientific papers claiming that cannabis is a "cure" for various cancers. However, when we look at the detail of the data and the experimental detail of the research, it becomes clear that although they may be interesting and build evidence to show that cannabinoids may one day bring benefits for cancer patients, they are far from being a cure. The main point to realise is that virtually all these studies have been done in cancer cells grown in the lab or in animals. These are quite artificial systems and are much less complex than a real cancer growing in a patient. For example, most experiments with cells grown in the lab use cancer cells that were originally taken from a tumour many years ago, but have been grown for a long time in the lab - known as cell lines. One problem with such cells is that they are all very similar on a genetic and molecular level, but we know that in real cancers, the cells can ...
Tetra BioPharma is developing a cannabinoid based therapeutics, acting by inhibition of the hedgehog signalling pathway, for the treatment of cancer and ocular
THCV is a cannabinoid that has garnered much attention for its ability to suppress appetite. The obscure compound is explored and explained in this post.
NEW YORK, September 13, 2017 /PRNewswire/ -- Biosynthesis Technology Could Transform Cannabinoid Production. NetworkNewsWire Editorial Coverage.
The ECS is comprised of two cannabinoid receptors (CB), CB1 and CB2, which belong to the G-coupled protein receptor super family, whose members influence various cellular processes by sensing extracellular signalling molecules (Mechoulam and Parker, 2013). CB1 is most abundantly expressed in the central and peripheral nervous system, with the exception of the brain stem region (Hu and Mackie, 2015). CB1 is also present, although less abundant, in peripheral organs such as the digestive tract, epidermis, adipose tissue, and skeletal muscle, as well as the cardiovascular, lymphatic, and respiratory systems (Mackie, 2006). CB2 receptor expression, on the other hand, is mainly restricted to immune cells and tissues, but has recently been described in certain glial and neuronal cell subpopulations, as well as in bone and liver (Mackie, 2006 ...
Rabbit polyclonal Cannabinoid Receptor II antibody validated for WB, IHC, ICC/IF and tested in Human, Mouse and Rat. Referenced in 5 publications and 8…
Evolab , the leader in advanced cannabis extraction and scientifically-informed product development, today announced its partnership with Realm of Caring , with the shared goals
Barchart.com Inc. is the leading provider of real-time or delayed intraday stock and commodities charts and quotes. Keep tabs on your portfolio, search for stocks, commodities, or mutual funds with screeners, customizable chart indicators and technical analysis.
Offentliggørelse af Den Europæiske Revisionsrets beretning om effektiviteten af ECBs forvaltning i regnskabsåret 2004 og ECBs svar
Cannabinoid agonists, including marijuana containing delta-9-tetrahydrocannabinol (THC), are found rewarding by humans. In addition to human self-reports and experimental studies that show marijuana is rewarding, contributions from preclinical studies also have implicated cannabinoid receptors in reward-motivated behavior. One way to assess these preclinical effects of cannabinoids is intracranial self-stimulation (ICSS), where an animal performs a response to receive electrical stimulation of a specific brain area or circuit known to be involved in reward. Drugs of abuse, such as psychomotor stimulants, facilitate responding for ICSS. While a few studies have shown facilitating effects of cannabinoids in rats, several have shown the opposite effect, and no studies so far have evaluated cannabinoids in mouse ICSS. Furthermore there are no studies evaluating specific inhibitors of endocannabinoid catabolic enzymes in ICSS in any species. In these studies we assessed the cannabinoid agonist THC, as well
Prolonged exposure of rats to the synthetic cannabinoid receptor ligand, CP-55,940 (0.4 mg/kg, i.p. for 11 days), induced tolerance to analgesia, to the reduction in spontaneous locomotor activity and the incidence of splayed hind limbs. One hour after the last injection on day 11, the rats were killed and in situ hybridization was used to investigate the effect of treatment on G-protein alpha-subunit expression throughout the brain. Chronic cannabinoid exposure markedly reduced G alpha(s), G alpha(i) and G alpha(o) mRNA levels. The message for the alpha(s)-subunit was decreased in all the brain areas containing the basal autoradiographic signal; the decrease ranging from 25% in the thalamus to 45% in the mesencephalon. Also the basal G alpha(i) expression was reduced in tolerant rats showing the greatest decrease in the forebrain (63%) in the cerebellum (58%) and in the mesencephalon (38%). The reduction in G alpha(o) expression (25%) was more localized, being present only in the rostral portion of the
There is convincing evidence that mammalian tissues express at least two types of cannabinoid receptor, CB1 and CB2, and that the endogenous cannabinoid, anandamide, and certain other eicosanoid agonists for known cannabinoid receptors can also activate vanilloid (VR1) receptors. Evidence is now also emerging that in addition to these established receptors for cannabinoids, other pharmacological targets for eicosanoid and / or non-eicosanoid cannabinoids are present in neuronal or non-neuronal tissues that include brain, spinal cord, microglial cells, heart, certain arteries, small intestine, vas deferens and peritoneum. Among new receptors to have been proposed for cannabinoids are CB2-like receptors in mouse paw and peritoneum, receptors for abnormal-cannabidiol in microglial cells and in arterial endothelial and non-endothelial cells, Gprotein coupled receptors for R-(+)-WIN55212 and anandamide in brain and spinal cord, receptors for Δ9- tetrahydrocannabinol and cannabinol on perivascular ...
Cannabinoids interact with your body by way of naturally occurring cannabinoid receptors embedded in cell membranes throughout your body. There are cannabinoid receptors in your brain, lungs, liver, kidneys, immune system, and more. Both the therapeutic and psychoactive properties of marijuana occur when a cannabinoid activates a cannabinoid receptor. Research is still ongoing on just how extensive their impact is on our health, but to date its known that cannabinoid receptors play an important role in many body processes, including metabolic regulation, cravings, pain, anxiety, bone growth, and immune function.. One of the earliest uses of medical marijuana was for the treatment of glaucoma. This is a condition that increases pressure in the eyeball, damaging the optic nerve and causing loss of vision. According to the National Eye Institute marijuana can decrease the pressure inside the eye."Studies in the early 1970s showed that marijuana, when smoked, lowered intraocular pressure (IOP) in ...
Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta, Georgia (J.L.N., Y.L., K.T.W., S.G.B., S.S., D.L.L.); School of Biological & Chemical Sciences, Queen Mary, University of London, London, United Kingdom (M.E., M.R.E.); Neuroscience of Drug Abuse Research Program, Julius L. Chambers Biomedical/Biotechnology Research Institute, North Carolina Central University, Durham, North Carolina, (S.M., A.C.H.); and Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia (H.H., D.E.S ...
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 ...
Laboratory and animal studies have shown that cannabinoids may be able to kill cancer cells while protecting normal cells. A study in mice showed that cannabinoids may protect against inflammation of the colon and may have potential in reducing the risk of colon cancer and possibly in its treatment. A laboratory study of delta-9-THC in hepatocellular carcinoma (liver cancer) cells showed that it damaged or killed the cancer cells.. Unlike conventional treatments for cancer complementary and alternative therapies are often not covered by insurance companies. Cannabinoid Brain Development patients should check with their insurance provider to find out about coverage for complementary and alternative therapies. Cancer patients considering complementary and alternative therapies should discuss this decision with their doctor nurse or pharmacist as they would any therapeutic approach because some complementary and alternative therapies may interfere with their standard treatment or may be harmful ...
Background Huntington disease (HD) is caused by the expansion of a CAG repeat within exon 1 of the huntingtin (HTT) gene. Although the variation in age at onset (AO) is partly explained by the lengths of the expanded repeat, the unexplained variation in AO is heritable, emphasising the role of modifier genes on disease expression. Identification of modifier genes can confirm intracellular pathways already suspected to be involved in pathophysiological processes related to HD pathogenesis. Since down regulation of type 1 cannabinoid (CB1) receptors is a key pathogenic event in HD, it has been suggested that activation of these receptors in patients may attenuate disease progression. ...
THC, it generally does not feature psychoactive (or narcotic) properties. Due to this (lack of) a function, its probable to utilize therapeutic attributes of Pot without getting high. The explanation for this big difference between the two ingredients is the fact, while THC immediately interacts with the CB1 and CB2 receptors in the body, CBD uses a rather oblique method towards the receptors.. Sensations in your brain and human anatomy are now being controlled by cannabinoid receptors, which are made to talk with Cannabinoids in plants which in turn are created by the mind for use in the torso according to necessity. A some of the frequent feelings which are underneath the get a handle on of cannabinoid receptors contain appetite, temper, pain, experience and memory.. While made to talk with the natural Endocannabinoids which are obviously created by the brain within the individual body. There are occasions that the human body needs additional security against the sounds (appetite, mood, ...
CB 2 agonists demonstrate remarkable anti inflammatory properties but , your , idea of receptor attraction has some merit, at least with respect to the , CB , 1 receptor. I recall an old study wherein they found that cannabis , tolerance , was proportional to the level of receptor retraction from the cell , surface. I wonder if, as with mu opioid tolerance, this effect is mediated by a PKC. Would inhibiting that PKC result in elevation of cannabinoid receptor levels? Also, B-cell proliferation appears to be partly under the regulation of a CB, although the research hasnt clarified it well yet. Ive always wondered if the way loss of gut bacteria knocks out the mu opioid and cannabinoid receptors of the gut wasnt also kicking antibody/B-cell production into needless overdrive (hence the use of B-cell depletion agents in autoimmune condition). , This does raise some worrying questions with respect to the chronic , ingestion of the same but the studies tend to find little ill effects. , ...
..increased CB1R levels could be a confounding effect of antipsychotic medication in schizophrenia that is circumveneted by high fat feeding.
Definition : Immunoassay reagents intended to perform qualitative analyses on a body fluid sample (typically urine) to detect cannabinoid levels and/or cannabinoid metabolite levels in a short period of time, typically several minutes.. Entry Terms : "Metabolite Determination Reagents, Cannabinoid, Rapid Test" , "Marijuana Rapid Test Determination Reagents" , "Marijuana Determination Reagents" , "Hashish Rapid Test Determination Reagents" , "Hashish Determination Reagents" , "Cannabinoid Determination Reagents" , "Cannabinoid Metabolite Reagents, Rapid Test" , "Cannabinoid Determination Reagents, Rapid Test" , "Reagents, Immunoassay, Rapid Test, Drug-of-Abuse, Cannabinoid/Metabolite". UMDC code : 20118 ...
Panag Pharmas (Panag), a subsidiary of Tetra, PPP003 is a synthetic cannabinoid drug that selectively acts at the type 2 cannabinoid receptor (CB2R). "Panags scientific team and academic collaborators have been studying the role of the CB2R in acute immune responses for over a decade. The active molecule in PPP003 can reduce inflammation and dampen pro-inflammatory cytokine release, therefore, PPP003 should be carefully examined as a candidate drug to help reduce symptoms of acute lung inflammation and immune system dysregulation in those SARS-CoV-2 patients at risk", states Tetras CSO, Dr. Melanie Kelly, Ph.D.. Guy Chamberland, CEO & CRO of Tetra commented, "It is a time for all pharmaceutical companies to contribute to the management of COVID-19 patients. We agree with our Canadian political leaders this is a time of national emergency. Our Panag team has been performing research on the prevention and management of severe systemic immune dysregulation such as sepsis since the early 2000s. ...
Dissolvable cannabinoids, such as powdered THC, are made possible through intense emulsification, extensive drying, and proprietary judge dosing. Learn the possibilities behind hydrophilic cannabinoids and why its taken so long to manufacture them.
Inflammation and oxidative stress are involved in many diseases. Chronic inflammation may be caused by autoimmune disorders, untreated infections or illnesses, and often plays a role in conditions such as asthma, cancer, and diabetes. Factors such as smoking, obesity, or stress may also contribute to chronic inflammation.. CBD has been touted as a potent plant-derived anti-inflammatory.. While inflammation is necessary to help protect the body as it heals, a state of ongoing or chronic inflammation is undesirable and can be a source of significant pain, anxiety, and is sometimes linked with depression. CBD has been touted as a potent plant-derived anti-inflammatory. Is there research to support its use in the treatment of acute and chronic inflammation?. What the Research Says. Research has shown that CBD is able to modulate the immune system. While CBD does not have much affinity for the bodys cannabinoid receptors, CB1 and CB2, it does affect other receptors and targets. CBD binds to TRPV1 ...
Marinol: Dronabinol is a member of the family of medications known as cannabinoids. Dronabinol is also known as THC (delta-9-tetrahydrocannabinol). This medication was developed after it was discovered that the THC found in marijuana was effective in treating severe nausea and vomiting associated with cancer chemotherapy.
此為系統發信請勿直接回覆。若您希望取消訂閱本公司電子報,請按這裡寄送退訂訊息給我們,謝謝 ...
All these effects are thought to be caused by cannabinoids locking onto the CB1 and CB2 cannabinoid receptors. It also looks like cannabinoids can exert effects on cancer cells that dont involve cannabinoid receptors, although it isnt yet clear exactly whats going on there.. So far, the best results in the lab or animal models have come from using a combination of highly purified THC and cannabidiol (CBD), a cannabinoid found in cannabis plants that counteracts the psychoactive effects of THC. But researchers have also found positive results using synthetic cannabinoids, such as a molecule called JWH-133.. Its not all good news though, as theres also evidence that cannabinoids may also have undesirable effects on cancer.. For example, some researchers have found that although high doses of THC can kill cancer cells, they also harm crucial blood vessel cells, although this may help their anti-cancer effect by preventing blood vessels growing into a tumour. And under some circumstances, ...
Inflammation serves an important role in the pathogenesis of idiopathic pulmonary fibrosis (IPF). Cannabinoid receptor 2 (CB2R) is a receptor predominantly expressed in the immune system. CB2R agonists can be used to treat a wide range of inflammation‑related diseases. Pirfenidone has been demonstrated to be effective for IPF treatment. The aim of present study was to investigate whether CB2R activation mediates the antifibrotic effect of pirfenidone. For that purpose, mice were intravenously injected with bleomycin (BLM; 5 mg/kg/day). pirfenidone (300 mg/kg/day) was then orally administered for 15 days. Lung pathological alterations in the mice were evaluated by Massons trichrome staining. The mRNA and protein levels of CB2R in lung tissues were measured by reverse transcription‑quantitative PCR and western blotting. The levels of inflammatory factors were determined by ELISA. The effect of pirfenidone on WI38 cell viability was evaluated by MTT assay. The results demonstrated that CB2R ...
Critical appraisal of the potential use of cannabinoids in cancer management Belinda J Cridge, Rhonda J Rosengren Department of Pharmacology and Toxicology, University of Otago, Dunedin, New Zealand Abstract: Cannabinoids have been attracting a great deal of interest as potential anticancer agents. Originally derived from the plant Cannabis sativa, there are now a number of endo-, phyto- and synthetic cannabinoids available. This review summarizes the key literature to date around the actions, antitumor activity, and mechanisms of action for this broad range of compounds. Cannabinoids are largely defined by an ability to activate the cannabinoid receptors – CB1 or CB2. The action of the cannabinoids is very dependent on the exact ligand tested, the dose, and the duration of exposure. Some cannabinoids, synthetic or plant-derived, show potential as therapeutic agents, and evidence across a range of cancers and evidence in vitro and in vivo is starting to be accumulated. Studies have now been
Aims: Cannabinoid 1(CB1) receptors are closely correlated to the dopaminergic system and involved in cognitive function. Since statins have been used to regulate the progression of Parkinsons disease (PD) via its anti-inflammation and neuroprotective effects, we asked if statins affect the CB1 receptors in the 6-hydroxydopamine (6-OHDA) lesioned rat. Methods: The PD rat model was established by injecting 6-OHDA into the unilateral medial forebrain bundle; while rats were orally pre-treated with simvastatin (1 or 10 mg/kg/day), or saline for 5 days before surgery, and the same treatments for each group were continued for 3 weeks post-surgery. [3H] SR141716A binding autoradiography was adopted to investigate the alterations in CB1 receptor density in the brains. Findings: The 6-OHDA induced a remarkable downregulation of CB1 receptor density in the prefrontal cortex, caudate putamen, nucleus accumbens, cingulate cortex, hippocampus, and substantia nigra; while simvastatin (10 mg/kg/day) significantly
Cannabinoid Complex by Boulder Botanicals: Is it legal? How effective is this full spectrum phytocannabinoid formula? How does Cannabinoid Complex work? Is this CBD supplement safe? Read this and more in our full review of Boulder Botanicals Cannabinoid Complex.
The areas of the brain where cannabinoid receptors are most prevalently located are consistent with the behavioral effects produced by cannabinoids. Brain regions in which cannabinoid receptors are very abundant are the basal ganglia , associated
Close The Infona portal uses cookies, i.e. strings of text saved by a browser on the users device. The portal can access those files and use them to remember the users data, such as their chosen settings (screen view, interface language, etc.), or their login data. By using the Infona portal the user accepts automatic saving and using this information for portal operation purposes. More information on the subject can be found in the Privacy Policy and Terms of Service. By closing this window the user confirms that they have read the information on cookie usage, and they accept the privacy policy and the way cookies are used by the portal. You can change the cookie settings in your browser. ...
20 represent a novel chemotype of potent and CB 2/CB 1 selective cannabinoid CB 2 receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable log P ...
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.
6.1 ~ The Cannabinoids Cannabis notorious resin is a complex mixture of cannabinoids, terpenes, and waxes, etc. There are about 100 known cannabinoids...
Like CBD, CBG isolate is non-psychoactive. However, scientists are still researching how CBG fully affects humans. For example, theyre exploring how different non-psychoactive cannabinoids like CBG can offer clinical uses.. You can buy CBG isolate bulk to experience the benefits for yourself. For example, some reports suggest that CBG is a partial agonist for cannabinoid receptors. This means that CBG could serve purposes that differ from CBDs known abilities. Though its possible CBG could help patients with other ailments, its also likely theres some overlap.. For starters, CBG can alter your mind in a way that might help ease anxiety and depression symptoms. CBG could also help counteract the effects of THC the same way CBD is able to.. Like CBD, CBD is able to activate CB1 receptors. This ability means CBG can decrease psycho-activation, which allows CBD and CBG to help you counteract the "high" you experience from THC.. ...
Amyris, Inc. (Nasdaq: AMRS), a leader in the development and production of sustainable ingredients for the Health & Wellness, Clean Beauty and Flavors & Fragrances markets, today reported that it has successfully shipped the first cannabinoid to its partner, LAVVAN. Amyris is also well on its way to
When eaten, these interact the human brains cannabinoid receptors and also have a profound effect on the Minds functions as well as the body. Both equally get the job done almost in a secure way more info but then their results and functions diverge a little from there onwards as THC has psychoactive results which lead to a sense of "superior" that brings about deficiency of psychological and Bodily coordination, loss of cognitive judgement, as well as the direst of all - problems Along with the law. It mimics the consequences of anandamide which happens to be a neurotransmitter that the Mind produces to control sleeping and ingesting together with the notion of suffering ...
Nabilone is used for the treatment of nausea as well as for the stimulation of appetite. The initial dose is, in fact, 1 mg daily. Doses can be increased to 2 mg twice daily to maximal effect. IN...
Sometimes the mundane recording of lot information and the time-consuming review of multiple chromatograms suddenly all seems worthwhile when it helps to solve a problem. In this case, careful troubleshooting explains an issue with a cannabinoid metabolite assay.
ECB Deals $5 ECB wyb 1 Bayer Contour Meter $14.99 Limit 1 $3 ECB wyb Claritin Non-Drowsy 24 hr Tablets 12 hr RediTabs 30 ct or 24 hr Liquid-Gels 24 ct $19.99 Limit 1 $7 ECB wyb Prilosec OTC 42 ct $24.99 Limit 1 $3.00 off any one Prilosec OTC (12/31/10) P&G 11/28 $7.00 off any two 42 ct.
Looks for amino acid and/or nucleotide patterns and/or small ligands coordinated to a given prosthetic centre. Files have to be in the local file system and contain proper extension.. ...
The actions of THC result from its partial agonist activity at the cannabinoid receptor CB1 (Ki = 10 nM[20]), located mainly in the central nervous system, and the CB2 receptor (Ki = 24 nM[20]), mainly expressed in cells of the immune system.[21] The psychoactive effects of THC are primarily mediated by the activation of cannabinoid receptors, which result in a decrease in the concentration of the second messenger molecule cAMP through inhibition of adenylate cyclase.[22]. The presence of these specialized cannabinoid receptors in the brain led researchers to the discovery of endocannabinoids, such as anandamide and 2-arachidonoyl glyceride (2-AG). THC targets receptors in a manner far less selective than endocannabinoid molecules released during retrograde signaling, as the drug has a relatively low cannabinoid receptor efficacy and affinity. In populations of low cannabinoid receptor density, THC may act to antagonize endogenous agonists that possess greater receptor efficacy.[23] THC is a ...
Cannabinoid receptor partial agonist.. PO.. Bioavailability = 10-20%; protein binding = 90-99%; volume of distribution = 10 L/ ... Partial agonist at the mu opioid receptor; agonist at delta opioid receptor; antagonist at kappa opioid receptor.. Sublingual, ... 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 ...
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... "Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum". British Journal of Pharmacology. 128 ... "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of Pharmacology. ... This cannabinoid related article is a stub. You can help Wikipedia by expanding it.. *v ...
... (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2 ... "Cannabinoid Receptor Agonists and Antagonists". Current Pharmaceutical Design. 1 (3): 343-352. ...
WIN 55,212-2 WIN 55,225 Howlett AC, Berglund B, Melvin LS (October 1995). "Cannabinoid Receptor Agonists and Antagonists". ... It is a tricyclic aryl derivative that acts as a competitive antagonist at the CB2 cannabinoid receptor. Its activity at CB1 ...
... is an indole-based synthetic cannabinoid that is a potent agonist of the CB1 receptor and has been sold online as a designer ... a synthetic cannabinoid receptor agonist". Clinical Toxicology: 1-2. doi:10.1080/15563650.2016.1227832. ISSN 1556-3650. PMID ... "Analysis and clinical findings of cases positive for the novel synthetic cannabinoid receptor agonist MDMB-CHMICA". Clinical ... "Clinical toxicity following analytically confirmed use of the synthetic cannabinoid receptor agonist MDMB-CHMICA. A report from ...
"Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB2 Receptor Inverse Agonists". ... Additionally, honokiol increases free cytoplasmic Ca2+ in rat cortical neurons.[10] Honokiol is a weak cannabinoid CB2 receptor ... occurring derivative 4-O-methylhonokiol was shown to be a potent and selective cannabinoid CB2 receptor inverse agonist and to ... However, honokiol has been shown to achieve anxiolysis with fewer motor or cognitive side effects than GABAA receptor agonists ...
Mallet PE, Beninger RJ (1996). "The endogenous cannabinoid receptor agonist anandamide impairs memory in rats". Behavioural ... This metabolite of paracetamol is a potent agonist at the TRPV1 vanilloid receptor, a weak agonist at both CB1 and CB2 ... These distinct effects are mediated primarily by CB1 cannabinoid receptors in the central nervous system, and CB2 cannabinoid ... Cannabinoid receptors. Boston: Academic Press. pp. 233-258. ISBN 0-12-551460-3. Wang, J.; Ueda, N. (2009). "Biology of ...
... (codenamed MK-0364) is a cannabinoid receptor type 1 inverse agonist that was investigated as a potential treatment ... "Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1- ... "Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists." Bioorganic & Medicinal Chemistry Letters. ... Cannabinoid receptor antagonist Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, et al. " ...
... which was originally proposed to act as a selective agonist for the CB1 cannabinoid receptor. It is a 12-amino acid polypeptide ... of cannabinoid CB1 receptors. It is shown that pepcan-12 opposite acts as a potent CB2 cannabinoid receptor positive allosteric ... "Novel endogenous peptide agonists of cannabinoid receptors". The FASEB Journal. 23 (9): 3020-3029. doi:10.1096/fj.09-132142. ... "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proceedings of the National Academy of Sciences of the United ...
It binds cannabinoid receptors, acting as an inverse agonist at CB1 receptors. Longer forms of hemopressin containing 2-3 ... December 2007). "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proc. Natl. Acad. Sci. U.S.A. 104 (51): 20588 ... September 2009). "Novel endogenous peptide agonists of cannabinoid receptors". FASEB J. 23 (9): 3020-9. doi:10.1096/fj.09- ... is also an agonist at CB1 cannabinoid receptors. The original Hp peptide reduces sensitivity to painful stimuli in an ...
... is an analgesic drug that is a cannabinoid agonist. It is a highly selective agonist for the CB2 receptor, with ... "Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630". British Journal ... It produces some similar effects to other cannabinoid agonists such as analgesia, but with little or no sedative or ... This cannabinoid related article is a stub. You can help Wikipedia by expanding it.. *v ...
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum. British Journal of Pharmacology. 1999 ... An investigation into the structural determinants of cannabinoid receptor ligand efficacy. British Journal of Pharmacology. ... administered alongside a more potent CB1 agonist, but exhibits weak partial agonist effects when administered by itself. ...
... is a compound which is a cannabinoid receptor agonist. It has analgesic effects and is used in scientific research. ... Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum. British Journal of Pharmacology. 1999 ... It is an extremely potent CB1 full agonist with a Ki of 0.21nM, making it more potent than the commonly used full agonist HU- ...
It is a partial agonist at the cannabinoid receptor CB1, producing a maximal stimulation of 58.3% with a Ki of 8.45nM. Griffin ... Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum. British Journal of Pharmacology. 1999 ... An investigation into the structural determinants of cannabinoid receptor ligand efficacy. British Journal of Pharmacology. ... Structural determinants of the partial agonist-inverse agonist properties of 6'-azidohex-2'-yne-delta8-tetrahydrocannabinol at ...
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 a potent CB1 full agonist with a Ki of 1.16 nM. ...
... is an agonist for cannabinoid receptors. Affinities are: with a Ki of 0.08 nM at CB1 and 18x selectivity over CB2 with a ... is a drug that acts as a potent and selective agonist for the cannabinoid receptor CB1. It is used in scientific research for ... Regioselective F-18 radiolabeling of AM694, a CB1 cannabinoid receptor ligand. Journal of Labelled Compounds and ... AM-679 AM-1235 AM-2201 AM-2232 AM-2233 FUBIMINA JWH-018 List of AM cannabinoids List of JWH cannabinoids THJ-2201 WO patent ...
Indol-3-yl) heterocycle derivatives as agonists of the cannabinoid CB1 receptor. Patent US 7700634, priority date 5 March 2004 ... Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists. Bioorganic & Medicinal ... PTI-1 is an indole-based synthetic cannabinoid. It is one of few synthetic cannabinoids containing a thiazole group and is ...
... is an agonist for the suggested novel cannabinoid receptor GPR119. PSN-375,963 PSN-632,408 Semple G, Fioravanti B, ... "Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119". J Med Chem. 51 (17 ...
Reggio, Patricia H. (2009). "Toward the design of cannabinoid CB1 receptor inverse agonists and neutral antagonists". Drug ... 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 ... Drinabant (INN; AVE-1625) is a drug that acts as a selective CB1 receptor antagonist, which was under investigation varyingly ...
... , a potent water-soluble cannabinoid receptor agonist with antinociceptive properties. British Journal of Pharmacology. ... which gives it considerable advantages over many related cannabinoids. It has moderate affinity for both CB1 and CB2 receptors ... O-1057 is an analgesic cannabinoid derivative created by Organix Inc., Newburyport, Massachusetts, for use in scientific ... Unlike most cannabinoids discovered to date, it is water-soluble, ...
... is a full agonist for cannabinoid receptors. Affinities are: with a Ki of 1.0 nM at CB1 and 2.6 nM at CB2. The 4-methyl ... is a recreational designer drug that acts as a potent but nonselective full agonist for the cannabinoid receptor. It is part of ... "First European case of convulsions related to analytically confirmed use of the synthetic cannabinoid receptor agonist AM-2201 ... AM-2201 has an EC50 of 38 nM for human CB1 receptors, and 58 nM for human CB2 receptors. AM-2201 produces bradycardia and ...
"Differential effects of cannabinoid receptor agonists on regional brain activity using pharmacological MRI". Br. J. Pharmacol. ... that acts as a selective full agonist of the peripheral cannabinoid receptor CB2, but with much lower affinity for the ... UR-144 has high affinity for the CB2 receptor with a Ki of 1.8 nM but 83x lower affinity for the CB1 receptor with a Ki of 150 ... 2010). "Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor ...
... that acts as a reasonably selective agonist of peripheral cannabinoid receptors. It has moderate affinity for CB2 receptors ... CANNABINOID RECEPTOR MODULATORS, THEIR PROCESSES OF PREPARATION, AND USE OF CANNABINOID RECEPTOR MODULATORS IN TREATING ... January 2008). "Differential effects of cannabinoid receptor agonists on regional brain activity using pharmacological MRI". ... 2011). "Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: Design, synthesis, structure-activity ...
Agonists and silent antagonists in a series of cannabinoid sulfonamides. 12th Annual Symposium on the Cannabinoids, 2002 Martin ... O-2050 is a drug that is a classical cannabinoid derivative, which acts as an antagonist for the CB1 receptor. This gives it an ... SULFONAMIDE CANNABINOID AGONISTS AND ANTAGONISTS. US Patent 7279500, Oct 9 2007 Gardner A, Mallet PE. Suppression of feeding, ... Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist. European Journal of ...
... is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 ... January 2008). "Differential effects of cannabinoid receptor agonists on regional brain activity using pharmacological MRI". ... Poso, A.; Huffman, J. W. (2008). "Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 ... 2010). "Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor ...
Receptor. Ligands. Agonists. Adamantanes: Amantadine • Memantine • Rimantadine; Aminotetralins: 7-OH-DPAT • 8-OH-PBZI • ... CB1 Agonists (Cannabinoids). Dronabinol • Nabilone • Nonabine. D2/D3 Antagonists. Alizapride • Bromopride • Chlorpromazine • ...
Cannabinoid Receptor Agonists. Cannabinoid Receptor Modulators. Neurotransmitter Agents. Molecular Mechanisms of ... Cannabinoid Receptor (CB1) Agonist Treatment in Severe Chronic Anorexia Nervosa. The safety and scientific validity of this ... A pilot study designed to reveal the effects of Marinol / dronabinol, a CB 1 agonist. ...
Therefore, we investigated the effects of the synthetic CB1 receptor agonist JWH-133 and CB1/CB2 receptor agonist WIN-55,212-2 ... Synthetic cannabinoid receptor agonists inhibit tumor growth and metastasis of breast cancer. Zahida Qamri, Anju Preet, Mohd W. ... Synthetic Cannabinoid Receptor Agonists Inhibit Metastasis of MDA-MB 231 Cells to Lungs In vivo. Because we showed that ... Cannabinoid receptor agonist-induced apoptosis of human prostate cancer cells LNCaP proceeds through sustained activation of ...
The CB2 cannabinoid receptor-selective agonist O-3223 reduces pain and inflammation without apparent cannabinoid behavioral ... The CB2 cannabinoid receptor-selective agonist O-3223 reduces pain and inflammation without apparent cannabinoid behavioral ... The CB2 cannabinoid receptor-selective agonist O-3223 reduces pain and inflammation without apparent cannabinoid behavioral ... The CB2 cannabinoid receptor-selective agonist O-3223 reduces pain and inflammation without apparent cannabinoid behavioral ...
Its ability to displace [(3)H]CP55940 from mouse CB(1) and human CB(2) cannabinoid receptors and to inhibit electrically evoked ... that the plant cannabinoid cannabigerol is a highly potent alpha2-adrenoceptor agonist and moderately potent 5HT1A receptor ... that the plant cannabinoid cannabigerol is a highly potent α2-adrenoceptor agonist and moderately potent 5HT1A receptor ... that the plant cannabinoid cannabigerol is a highly potent α2-adrenoceptor agonist and moderately potent 5HT1A receptor ...
Thus, activation of cannabinoid receptors inhibits N- and P/Q-type Ca2+ channels. Activation of cannabinoid receptors inhibited ... The cannabinoid agonist Win55,212-2 inhibits calcium channels by receptor-mediated and direct pathways in cultured rat ... The effects of the cannabinoid receptor agonist Win55,212 on Ca2+ channels were studied in rat hippocampal neurons grown in ... Win55,212-2 inhibited whole-cell Ba2+ currents through Ca2+ channels by both CB1 receptor-mediated and direct mechanisms. The ...
A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded ... soluble cannabinoid CB1 receptor. agonists. Julia M. Adam,*a Jim Cairns,a Wilson Caulfield,a Phillip Cowley,a Iain Cumming,a ... soluble cannabinoid CB1 receptor. agonists. J. M. Adam, J. Cairns, W. Caulfield, P. Cowley, I. Cumming, M. Easson, D. Edwards, ... receptor agonist. lead series was identified using a high-throughput screening approach. The initial screen afforded a single ...
Previously we identified a series of amidoalkylindoles as potent and selective CB2 partial agonists. In the present study, we ... Introducing nitrogen atoms to amidoalkylindoles: potent and selective cannabinoid type 2 receptor agonists with improved ... Introducing nitrogen atoms to amidoalkylindoles: potent and selective cannabinoid type 2 receptor agonists with improved ... were found to be potent and selective CB2 receptor partial agonists, both with improved aqueous solubility. ...
Source: Cannabinoid receptor 2 and its agonists mediate hemato... [Blood. 2011] - PubMed - NCBI ... whereas CB₂ receptors are expressed in human and murine HSPCs. On ligand stimulation with CB₂ agonists, CB₂ receptors induced ... cannabinoid type 2 receptor knockout mice. Taken together, these results demonstrate that the endocannabinoid system is ... along with their G-coupled cannabinoid receptors (CB₁ and CB₂) and the enzymes involved in their biosynthesis and degradation. ...
Cryo-EM structure of human cannabinoid receptor 2-Gi protein in complex with agonist WIN 55,212-2. *DOI: 10.2210/pdb6PT0/pdb ... G Protein-Coupled Receptors (GPCRs). Protein: CB2-Gi cannabinoid receptor complex. ... G Protein-Coupled Receptors (GPCRs). Protein: CB2-Gi cannabinoid receptor complex. ... G Protein-Coupled Receptors (GPCRs). Protein: CB2-Gi cannabinoid receptor complex. ...
... the administration of two synthetic cannabinoid agonists of the cannabinoid brain (CB1) receptor WIN 55,212-2 mesylate (R-(+)-[ ... the GABAB receptor agonist baclofen, the NMDA receptor antagonist memantine, and the cannabinoid antagonist SR141716 (N- ... Long-Lasting Increase of Alcohol Relapse by the Cannabinoid Receptor Agonist WIN 55,212-2 during Alcohol Deprivation. José ... Basavarajappa BS, Hungund BL (1999) Down-regulation of cannabinoid receptor agonist-stimulated [35S]GTP gamma S binding in ...
PubMed journal article The cannabinoid receptor agonist WIN 55,212-2 inhibits antigen-induced plasma extravasation in guinea ... AnimalsAntigensBenzoxazinesCamphanesCannabinoid Receptor AgonistsCannabinoid Receptor AntagonistsCapillary Permeability ... Involvement of spinal cannabinoid receptors in the antipruritic effects of WIN 55,212-2, a cannabinoid receptor agonist. ... Cannabinoid receptor agonists inhibit sensory nerve activation in guinea pig airways.. *The cannabinoid antagonist SR144528 ...
... cannabinoid receptor subtype-1; CB2, cannabinoid receptor subtype-2; CCK, cholecystokinin; DAMGO, [d-Ala2, N-Me-Phe4,Gly5-ol]- ... Effects of Opioid and Cannabinoid Receptor Agonists on ERK Activation in the Normal Spinal Cord. We used a rat spinal cord ... Effects of Opioid and Cannabinoid Agonists on ERK Activation in the Spinal Cord of Nerve-Injured Rats. Although opioid receptor ... 2). These results indicate that both opioid and cannabinoid receptor agonists at optimal concentrations are effective in ...
Dual Activation and Inhibition of Adenylyl Cyclase by Cannabinoid Receptor Agonists: Evidence for Agonist-Specific Trafficking ... Dual Activation and Inhibition of Adenylyl Cyclase by Cannabinoid Receptor Agonists: Evidence for Agonist-Specific Trafficking ... Dual Activation and Inhibition of Adenylyl Cyclase by Cannabinoid Receptor Agonists: Evidence for Agonist-Specific Trafficking ... Dual Activation and Inhibition of Adenylyl Cyclase by Cannabinoid Receptor Agonists: Evidence for Agonist-Specific Trafficking ...
central cannabinoid receptor. CB2. peripheral cannabinoid receptor. CHO. Chinese hamster ovary. FCS. fetal calf serum. GPCR. G- ... Modulation of CB1 Cannabinoid Receptor Functions after a Long-Term Exposure to Agonist or Inverse Agonist in the Chinese ... Modulation of CB1 Cannabinoid Receptor Functions after a Long-Term Exposure to Agonist or Inverse Agonist in the Chinese ... Modulation of CB1 Cannabinoid Receptor Functions after a Long-Term Exposure to Agonist or Inverse Agonist in the Chinese ...
GW405833, widely accepted as a cannabinoid receptor 2 (CB2) agonist, suppresses pathologic pain in preclinical models without ... Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB ... Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of ... the unwanted central side effects of cannabinoid receptor 1 (CB1) agonists; however, recent in vitro studies have suggested ...
Effects of Cannabinoid Receptor Agonist and Antagonist Ligands on Production of Inflammatory Cytokines and Anti-Inflammatory ... Effects of Cannabinoid Receptor Agonist and Antagonist Ligands on Production of Inflammatory Cytokines and Anti-Inflammatory ... Effects of Cannabinoid Receptor Agonist and Antagonist Ligands on Production of Inflammatory Cytokines and Anti-Inflammatory ... Effects of Cannabinoid Receptor Agonist and Antagonist Ligands on Production of Inflammatory Cytokines and Anti-Inflammatory ...
... agonists have been shown to alleviate behavioral signs of inflammatory and neuropathic pain in animal models. AM1241... ... Source: A cannabinoid 2 receptor agonist attenuates bone c... [Life Sci. 2010] - PubMed result ... A cannabinoid 2 receptor agonist attenuates bone cancer-induced pain and bone loss. ... Cannabinoid CB(2) agonists have been shown to alleviate behavioral signs of inflammatory and neuropathic pain in animal models ...
Cannabinoid receptor binding and agonist activity of amides and esters of arachidonic acid.. J C Pinto, F Potié, K C Rice, D ... Cannabinoid receptor binding and agonist activity of amides and esters of arachidonic acid.. J C Pinto, F Potié, K C Rice, D ... Cannabinoid receptor binding and agonist activity of amides and esters of arachidonic acid.. J C Pinto, F Potié, K C Rice, D ... Cannabinoid receptor binding and agonist activity of amides and esters of arachidonic acid. ...
central cannabinoid receptor. CB2. peripheral cannabinoid receptor. hCB2. human type 2 cannabinoid receptor. GTPγS. guanosine-5 ... Endocannabinoid 2-Arachidonyl Glycerol Is a Full Agonist through Human Type 2 Cannabinoid Receptor: Antagonism by Anandamide. ... Endocannabinoid 2-Arachidonyl Glycerol Is a Full Agonist through Human Type 2 Cannabinoid Receptor: Antagonism by Anandamide. ... Endocannabinoid 2-Arachidonyl Glycerol Is a Full Agonist through Human Type 2 Cannabinoid Receptor: Antagonism by Anandamide. ...
The Case for Cannabinoid CB1 Receptors as a Target for Bronchodilator Therapy for β-agonist Resistant Asthma. Author(s): John C ... Title:The Case for Cannabinoid CB1 Receptors as a Target for Bronchodilator Therapy for β-agonist Resistant Asthma ... Keywords:Asthma, bronchodilation, β2-agonist, CB1 receptor, salbutamol, THC.. Abstract:Although β2-receceptor agonists are ... "The Case for Cannabinoid CB1 Receptors as a Target for Bronchodilator Therapy for β-agonist Resistant Asthma", Current Drug ...
AM-1241, a novel, racemic cannabinoid-2 receptor (CB2) ligand, is the primary experimental agonist used to characterize the ... Therapeutic modulation of cannabinoid lipid signaling: Metabolic profiling of a novel antinociceptive cannabinoid-2 receptor ...
... a highly selective cannabinoid CB1 receptor agonist) stimulates hippocampal neurogenesis in mice treated with antiepileptic ... Cannabinoid receptor agonists inhibit glutamatergic synaptic transmission in rat hippocampal cultures. Shen, M.; Piser, T.M.; ... The cannabinoid CB2 receptor agonist AM1241 enhances neurogenesis in GFAP/Gp120 transgenic mice displaying deficits in ... Effect of ACEA--a selective cannabinoid CB1 receptor agonist on the protective action of different antiepileptic drugs in the ...
The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained ... The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained ... The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained ... The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained ...
... receptor agonists WIN55,212-2 and HU-210 and the selective CB1-receptor antagonist SR141716A were tested on in vitro and in ... The effects of the cannabinoid (CB)-receptor agonists WIN55,212-2 and HU-210 and the selective CB1-receptor antagonist ... Effects of Cannabinoid Receptor Agonists on Rat Gastric Acid Secretion: Discrepancy Between In Vitro and In Vivo Data. ... Felder CC, Glass M: Cannabinoid receptors and their endogenous agonists. Annu Rev Pharmacol 38:179-200, 1998Google Scholar ...
... with the brain cannabinoid (CB(1)) receptor activates G-proteins and relays signals to regulate neuronal functions. A CB(1) ... Association of cannabimimetic compounds such as cannabinoids, aminoalkylindoles (AAIs), and arachidonylethanolamide (anandamide ... Homology Model of the CB1 Cannabinoid Receptor: Sites Critical for Nonclassical Cannabinoid Agonist Interaction Joong-Youn Shim ... Homology Model of the CB1 Cannabinoid Receptor: Sites Critical for Nonclassical Cannabinoid Agonist Interaction Joong-Youn Shim ...
  • O-1057, a potent water-soluble cannabinoid receptor agonist with antinociceptive properties. (wikipedia.org)
  • It was developed with the aim of finding a water-soluble cannabinoid agonist suitable for intravenous use as an analgesic, but did not proceed to human trials, with the related compound Org 28611 chosen instead due to its better penetration into the brain. (wikipedia.org)
  • It was developed with the aim of finding a water-soluble cannabinoid agonist suitable for intravenous use as an analgesic, and while it achieved this aim and has progressed as far as Phase II clinical trials in humans as both a sedative and an analgesic, results against the comparison drugs (midazolam and morphine respectively) were not particularly favourable in initial testing. (wikipedia.org)
  • The clonal Chinese hamster ovary (CHO)-hCB2 cell line was generated by transfection of CHO-K1 cells with hCB2 cDNA modified by placement of the hemagglutinin epitope on the N terminus cloned into the pCEP4 vector (Invitrogen, San Diego, CA). Stable clones were obtained by limiting dilution, screened with cannabinoid inhibition of cAMP, and confirmed by fluorescence-activated cell sorting analysis of cell surface hemagglutinin expression. (aspetjournals.org)
  • Tyler K, Hillard CJ, Greenwood-Van Meerveld B: Inhibition of small intestinal secretion by cannabinoids is CB 1 receptor-mediated in rats. (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)
  • To date, there has been virtually no information regarding the mechanism of CB 2 receptor-mediated inhibition of pain responses. (pnas.org)
  • RVD-Hpα also significantly potentiated the effects of CB2 receptor agonists, including the endocannabinoid 2-arachidonoyl glycerol (2-AG), for GTPγS binding and cAMP inhibition (5-10 fold). (wikipedia.org)
  • Activation of cannabinoid receptors inhibited only a fraction of the whole-cell Ca2+ channel current (17+/-2%) even though more than half of the whole-cell Ba2+ current was carried by N- and P/Q-type Ca2+ channels. (nih.gov)