Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.
OXAZINES with a fused BENZENE ring.
Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.
Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
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.
Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS.
Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.
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.
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.
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.
A family of hexahydropyridines.
Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
GLYCEROL esterified with FATTY ACIDS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Compound isolated from Cannabis sativa extract.
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23.
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.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
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.
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.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
Drugs that bind to and activate dopamine receptors.
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.
A physiologically inactive constituent of Cannabis sativa L.
The plant genus in the Cannabaceae plant family, Urticales order, Hamamelidae subclass. The flowering tops are called many slang terms including pot, marijuana, hashish, bhang, and ganja. The stem is an important source of hemp fiber.
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 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.
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.
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.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
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)
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.
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.
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'-(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.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
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.
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
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.
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.
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
The observable response an animal makes to any situation.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
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.
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.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
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.
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.
AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
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.
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.
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.
Compounds based on benzene fused to oxole. They can be formed from methylated CATECHOLS such as EUGENOL.
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.
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
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.
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.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
Drugs that bind to and activate excitatory amino acid receptors.
The most common inhibitory neurotransmitter in the central nervous system.
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.
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.
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.
The physical activity of a human or an animal as a behavioral phenomenon.
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.
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.
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.
Six-carbon alicyclic hydrocarbons.
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)

We have demonstrated previously that mouse and human islets express ECS (endocannabinoid system) elements, and that short-term activation of islet cannabinoid CB1r and CB2r (cannabinoid type 1 and 2 receptors respectively) stimulates insulin secretion in vitro. There is evidence that the ECS is overactive in Type 2 diabetes, impairing glucose homoeostasis, but little is known about whether it is implicated in islet dysfunction. Therefore the aim of the present study was to investigate the effect of chronic exposure of isolated mouse islets to cannabinoid receptor agonists on islet gene expression and function. Quantitative RT-PCR (reverse transcription-PCR) indicated that mRNAs encoding synthesis [NAPE-PLD (N-acyl-phosphatidyl ethanolamide-hydrolysing phospholipase D)] and degradation [FAAH (fatty acid amide hydrolase)] of the endocannabinoid AEA (anandamide) were the most abundant ECS elements in mouse islets, with much lower levels of CB1r, CB2r, DAGL (diacylglycerol lipase) and MAGL ...
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 ...
Two weeks of supplementation with palmitoylethanolamide, an endocannabinoid-like molecule with potent anti-inflammatory properties, may reduce joint discomfort and improving quality of life in adults, says a new study.
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!
TY - JOUR. T1 - Pre-exposure to the cannabinoid receptor agonist CP 55,940 enhances morphine behavioral sensitization and alters morphine self-administration in Lewis rats. AU - Norwood, Christy S.. AU - Cornish, Jennifer L.. AU - Mallet, Paul E.. AU - McGregor, Iain S.. PY - 2003/3/28. Y1 - 2003/3/28. N2 - Three experiments examined the influence of pre-exposure to the cannabinoid receptor agonist CP 55,940 ((-)-cis-3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-trans-4-(3- hydroxypropyl)cyclohexanol) on the sensitization of morphine-induced locomotor hyperactivity and self-administration in Lewis rats. In Experiment 1, rats received daily injections of vehicle or CP 55,940 (0.1 mg/kg for 7 days then 0.2 mg/kg for a further 7 days). Four weeks later, the locomotor response to morphine (10 mg/kg s.c.) was tested once per day over a 3-h period for 14 consecutive days. Rats given morphine showed hypoactivity during the first hour following morphine but hyperactivity during the second and third hours. ...
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 ...
ancient herb.. 2009 - Studie ~ Cannabinoids, Endocannabinoids, and Related Analogs in Inflammation.. 2009 - Studie ~ Evaluation of Prevalent Phytocannabinoids in the Acetic Acid Model of Visceral Nociception.. 2009 - Studie ~ The putative cannabinoid receptor GPR55 affects osteoclast function in vitro and bone mass in vivo.. 2009 - Studie ~ Cannabinoids as novel anti-inflammatory drugs.. 2009 - Studie ~ Cannabidiol, a Nonpsychotropic Component of Cannabis, Inhibits Cue-Induced Heroin Seeking and Normalizes Discrete Mesolimbic Neuronal Disturbances.. 2009 - Studie ~ Cannabidiol As a Putative Novel Therapy for Diabetic Retinopathy: A Postulated Mechanism of Action as an Entry Point for Biomarker-Guided Clinical Development.. 2009 - Studie ~ Cannabidiol Attenuates Cisplatin-Induced Nephrotoxicity by Decreasing Oxidative/Nitrosative Stress, Inflammation, and Cell Death.. 2009 - Studie ~ The nonpsychotropic cannabinoid cannabidiol modulates and directly activates alpha-1 and alpha-1-Beta glycine ...
Funded by the NIH National Center for Advancing Translational Sciences through its Clinical and Translational Science Awards Program, grant number UL1TR002541 ...
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, ...
Dronabinol with NDC 0904-7144 is a a human prescription drug product labeled by Major Pharmaceuticals. The generic name of Dronabinol is dronabinol.
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
The cannabinoid receptors are cells spread throughout your body and there are at least two types of receptors that work as part of your endocannabinoid
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
TY - JOUR. T1 - Cannabinoid receptor 2 activation. T2 - A means to prevent monocyte-endothelium engagement. AU - Buch, Shilpa J.. PY - 2013/11. Y1 - 2013/11. UR - http://www.scopus.com/inward/record.url?scp=84886695905&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=84886695905&partnerID=8YFLogxK. U2 - 10.1016/j.ajpath.2013.08.003. DO - 10.1016/j.ajpath.2013.08.003. M3 - Comment/debate. C2 - 24055258. AN - SCOPUS:84886695905. VL - 183. SP - 1375. EP - 1377. JO - American Journal of Pathology. JF - American Journal of Pathology. SN - 0002-9440. IS - 5. ER - ...
Fingerprint Dive into the research topics of Cannabinoid receptor activation in the nucleus tractus solitaries produces baroreflex-like responses in the rat. Together they form a unique fingerprint. ...
A new study from the University of Texas M. D. Anderson Cancer Centre has shown that the cannabinoid cell surface receptor CB1 plays a key role in suppressing tumour growth in colorectal
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
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A detailed view of the primary molecule through which cannabinoids-the active compounds in marijuana-exert their effects on the brain could help guide the design of targeted medicines.
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 ...
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Chemicals found in cannabis or cannabinoids may be better at reducing bacteria associated with dental plaque than synthetic oral care products.
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 suggest. ...
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 ...
© 2014 The Authors. The cannabinoid receptor 2 (CB2R) has been linked with the regulation of inflammation, and selective receptor activation has been proposed as a target for the treatment of a range of inflammatory diseases such as atherosclerosis and arthritis. In order to identify selective CB2R agonists with appropriate physicochemical and ADME properties for future evaluation in vivo, we first performed a ligand-based virtual screen. Subsequent medicinal chemistry optimisation studies led to the identification of a new class of selective CB2R agonists. Several examples showed high levels of activity (EC50 <200nM) and binding affinity (K i <200nM) for the CB2R, and no detectable activity at the CB1R. The most promising example, DIAS2, also showed favourable in vitro metabolic stability and absorption properties along with a clean selectivity profile when evaluated against a panel of GPCRs and kinases.
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 ...
According to the European Monitoring Center for Drugs and Drug Addiction (EMCDDA), there were 179 different synthetic cannabinoids reported as of 2017. In the USA, 5F-MDMB-PINACA, or 5F-ADB, accounted for 28% of cannabinoid seizures 2016-2018. The synthetic cannabinoid, 5F-MDMB-PICA, is structurally …
What is Dronabinol 2.5mg Capsules ?. Dronabinol 2.5mg Capsules is used to treat nausea and vomiting caused by chemotherapy in people who have already taken other medications to treat this type of nausea and vomiting without good results.. Dronabinol 2.5mg Capsules is also used to treat loss of appetite and weight loss in people who have acquired immunodeficiency syndrome (AIDS). Dronabinol 2.5mg Capsules is in a class of medications called cannabinoids. It works by affecting the area of the brain that controls nausea, vomiting, and appetite.. How should Dronabinol be used?. Dronabinol comes as a capsule and as a solution (liquid) to take by mouth. When dronabinol capsules and solution are used to treat nausea and vomiting caused by chemotherapy, it is usually taken 1 to 3 hours before chemotherapy and then every 2 to 4 hours after chemotherapy, for a total of 4 to 6 doses a day. The first dose of the solution is usually taken on an empty stomach at least 30 minutes before eating, but the ...
Cannabinoids (CBs) implicate in a number of physiological and pathological mechanisms in the central nervous system. The cannabinoid receptor family consists of two GPCRs, cannabinoid receptor 1 (CB1) and cannabinoid…. Read More Read More. ...
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.
With a clean and minimalist style, this print depicts the names and chemical structures of 20 different cannabinoid molecules including THC, CBD, CBC, etc.
This is our resource detailing every clinical study thus far related to cannabinoid usage in dogs. Weve summarized all of these studies in as fair and impartial a way as possible, but of course, we also provide all the links to the original studies for those who want to do more research.
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 , ...
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... (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. v t e. ...
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 ...
"Cannabinoid receptors and their endogenous agonists." Annual Review of Pharmacology and toxicology 38, no. 1 (1998): 179-200. ... "Immunomodulation by cannabinoids is absent in mice deficient for the cannabinoid CB2 receptor." European Journal of ... "Concurrent stimulation of cannabinoid CB1 and dopamine D2 receptors enhances heterodimer formation: a mechanism for receptor ... "Cannabinoid receptors in the human brain: a detailed anatomical and quantitative autoradiographic study in the fetal, neonatal ...
Meyyappan C, Ford L, Vale A (February 2017). "Poisoning due to MDMB-CHMICA, a synthetic cannabinoid receptor agonist". Clinical ... September 2016). "Clinical toxicity following analytically confirmed use of the synthetic cannabinoid receptor agonist MDMB- ... is an indole-based synthetic cannabinoid that is a potent agonist of the CB1 receptor and has been sold online as a designer ... "Analysis and clinical findings of cases positive for the novel synthetic cannabinoid receptor agonist MDMB-CHMICA" (PDF). ...
... 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". FASEB Journal. 23 (9): 3020-9. doi:10.1096/fj.09-132142. PMC ... "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. Hemopressin is not an endogenous peptide but rather an extraction artefact [ ...
... produces effects typical of other cannabinoid receptor agonists in animals. It has a somewhat higher oral ... however the Δ8 and Δ9 isomers are both known to be cannabinoid receptor agonists, and Δ8-parahexyl has the code number JWH-124 ... "Manipulation of the tetrahydrocannabinol side chain delineates agonists, partial agonists, and antagonists". The Journal of ... Presumably it acts as a CB1 agonist in the same way as THC but as there has been no research published using parahexyl since ...
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... Griffin G, Wray EJ, Martin BR, Abood ME (October 1999). "Cannabinoid agonists and antagonists discriminated by receptor binding ... April 1999). "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of ... administered alongside a more potent CB1 agonist, but exhibits weak partial agonist effects when administered by itself. ...
... is a chemical compound which is a cannabinoid receptor agonist. It has analgesic effects and is used in scientific ... "Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum". British Journal of Pharmacology. 128 ... It is an extremely potent CB1 full agonist with a Ki of 0.21 nM, 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. 128 ... April 1999). "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of ... yne-delta8-tetrahydrocannabinol at cannabinoid receptors". British Journal of Pharmacology. 128 (3): 735-43. doi:10.1038/sj.bjp ...
Griffin G, Wray EJ, Martin BR, Abood ME (1999). "Cannabinoid agonists and antagonists discriminated by receptor binding in rat ... O-1125 (3-(1,1-dimethylhexyl-6-dimethylcarboxamide)-Δ8-tetrahydrocannabinol) is a research chemical which is a cannabinoid ... It is a potent CB1 full agonist with a Ki of 1.16 nM. ...
... (codenamed MK-0364) is a cannabinoid receptor type 1 (CB1) inverse agonist that was investigated as a potential ... Jun 2007). "Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3- ... 2007). "Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists". Bioorganic & Medicinal Chemistry ... Cannabinoid receptor antagonist Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, et al. ( ...
It is used in scientific research for mapping the distribution of CB1 receptors. AM-694 is an agonist for cannabinoid receptors ... is a designer drug that acts as a potent and selective agonist for the cannabinoid receptor CB1. ... AM-679 AM-1235 AM-2201 AM-2232 AM-2233 FUBIMINA JWH-018 List of AM cannabinoids List of JWH cannabinoids THJ-2201 Willis PG, ... a CB1 cannabinoid receptor ligand". Journal of Labelled Compounds and Radiopharmaceuticals. 46 (9): 799-804. doi:10.1002/jlcr. ...
March 2011). "Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists". Bioorganic & ... heterocycle derivatives as agonists of the cannabinoid CB1 receptor.", issued 20 April 2010, assigned to Organon NV US 7763732 ... PTI-1 (SGT-48) is an indole-based synthetic cannabinoid. It is one of few synthetic cannabinoids containing a thiazole group ...
It acts as a potent and selective cannabinoid receptor agonist, with high potency at both the CB1 and CB2 receptors, but low ... March 2011). "Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists". Bioorganic & ... April 2012). "Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain". Bioorganic & Medicinal ... heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate". Bioorganic & Medicinal Chemistry ...
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 ...
... 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". British Journal of ... 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 ... UR-144 was found to possess an EC50 of 421 nM for human CB1 receptors, and 72 nM for human CB2 receptors. UR-144 produces ...
Banister SD, Connor M (August 2018). The Chemistry and Pharmacology of Synthetic Cannabinoid Receptor Agonist New Psychoactive ... June 2020). "In vitro and in vivo pharmacological evaluation of the synthetic cannabinoid receptor agonist EG-018". ... EG-018 is a carbazole-based synthetic cannabinoid that has been sold online as a designer drug. It acts as a partial agonist of ... Diao X, Carlier J, Zhu M, Huestis MA (July 2018). "Metabolism of the new synthetic cannabinoid EG-018 in human hepatocytes by ...
... 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 for Treating ... January 2008). "Differential effects of cannabinoid receptor agonists on regional brain activity using pharmacological MRI". ... cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and ...
... 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 JW (January 2008). "Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 ... March 2008). "Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor ...
"An expedient atom-efficient synthesis of the cannabinoid CB1 receptor inverse agonist ibipinabant". Tetrahedron Letters. 52 (12 ... Cannabinoid receptor antagonist Lange JH, Coolen HK, van Stuivenberg HH, Dijksman JA, Herremans AH, Ronken E, et al. (January ... November 2005). "Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity". ... a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition Tasks in ...
Deutsch DG, Chin SA (September 1993). "Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist". ... a cannabinoid receptor (CB) agonist. Due to the ability of FAAH to regulate nociception, it is currently viewed as an ... which are agonists of the transient receptor potential (TRP) family of calcium channels. FAAH knockout mice display highly ... Cravatt BF, Lichtman AH (October 2004). "The endogenous cannabinoid system and its role in nociceptive behavior". Journal of ...
... is a research chemical which is a cannabinoid receptor agonist. It has analgesic effects and is used in scientific ... Griffin G, Atkinson PJ, Showalter VM, Martin BR, Abood ME (May 1998). "Evaluation of cannabinoid receptor agonists and ... "Pharmacological characterization of three novel cannabinoid receptor agonists in the mouse isolated vas deferens". European ... It is a partial agonist at CB1 receptors, with a Ki of 87 nM, making it roughly half the potency of THC. It was discovered and ...
... is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class. Rimonabant is ... Fong TM, Heymsfield SB (September 2009). "Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action ... Pi-Sunyer FX, Aronne LJ, Heshmati HM, Devin J, Rosenstock J (Feb 2006). "Effect of rimonabant, a cannabinoid-1 receptor blocker ... Cahill, K; Ussher, MH (16 March 2011). "Cannabinoid type 1 receptor antagonists for smoking cessation". The Cochrane Database ...
"Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1)". The Journal of ... ACEA is considered to be a selective cannabinoid agonist as it binds primarily to the CB1R and has low affinity to the CB2 ( ... Arachidonyl-2'-chloroethylamide (ACEA) is a synthetic agonist of the CB1 (CB1R). ...
"Cannabinoid CB1 and CB2 receptor ligand specificity and the development of CB2-selective agonists". Current Medicinal Chemistry ... is an analgesic chemical from the naphthoylindole family that acts as a cannabinoid agonist at both the CB1 and CB2 receptors. ... Poso A, Huffman JW (January 2008). "Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 ... It is the N-hexyl homolog of the more common synthetic cannabinoid compound JWH-018. Unlike the butyl homolog JWH-073, which is ...
Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first medication approved in that class. In ... Fong TM, Heymsfield SB (September 2009). "Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action ... It reduces appetite by activating a type of serotonin receptor known as the 5-HT2C receptor in a region of the brain called the ... "Off-label antiobesity treatment in patients without diabetes with GLP-1 agonists in clinical practice". Hormone and Metabolic ...
AM-251 is an inverse agonist at the CB1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are ... Discovery and development of Cannabinoid Receptor 1 Antagonists Lan R, Liu Q, Fan P, Lin S, Fernando SR, McCallion D, et al. ( ... February 1999). "Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists". Journal of ... "AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies ...
... is a synthetic agonist of the cannabinoid receptor 1 (CB1R). ACPA is considered to be a selective cannabinoid agonist as it ... 1999). "Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1)". The ... binds primarily to the CB1R and has low affinity to the cannabinoid receptor 2 (CB2R) (Ki = 2.2 nM for CB1R; Ki = 700 nM for ...
Another bile acid receptor is the cell membrane receptor known as G protein-coupled bile acid receptor 1 or TGR5. Many of their ... Obeticholic acid, 6α-ethyl-chenodeoxycholic acid, is a semi-synthetic bile acid with greater activity as FXR agonist which is ... the endogenous cannabinoid anandamide) that play important roles in several physiological pathways including stress and pain ... the farnesoid X receptor and G protein-coupled bile acid receptor/TGR5.[7][10] They bind less specifically to some other ...
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 • ...
WO application 2006069196, Pace JM, Tietje K, Dart MJ, Meyer MD, "3-Cycloalkylcarbonyl indoles as cannabinoid receptor ligands ... cannabinoid receptor activity". Journal of Medicinal Chemistry. 53 (1): 295-315. doi:10.1021/jm901214q. PMID 19921781.. .mw- ... This cannabinoid related article is a stub. You can help Wikipedia by expanding it.. *v ... XLR-12 is an indole-based synthetic cannabinoid drug that was invented by Abbott Laboratories in 2006.[1] It is an analogue of ...
Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) ... Cannabinoid receptor antagonists. *CCR5 receptor antagonists. *Neurokinin 1 receptor antagonists. *5-HT3 antagonists ... The GABAA receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ...
Cannabinoid receptor antagonist(英語:Cannabinoid receptor antagonist). *Endocannabinoid enhancer(英語:Endocannabinoid enhancer) ( ... Glutamate receptor agonist(英語:Excitatory amino acid agonist) (AMPA(英語:Ampakine)) ... Acetylcholine receptor agonist(英語:Parasympathomimetic_drug) (Muscarinic(英語:Muscarinic agonist) ... Glutamate receptor antagonist(英語:Excitatory amino acid antagonist) (NMDA(英語:NMDA receptor antagonist)) ...
The anti-obesity drugs rimonabant and taranabant are inverse agonists at the cannabinoid CB1 receptor and though they produced ... GABA receptors: GABA-A, GABA-C. GABA. Cl− , HCO−3 [11]. Glutamate receptors: NMDA receptor, AMPA receptor, and Kainate receptor ... This results in a receptor blockade, inhibiting the binding of agonists and inverse agonists. Receptor antagonists can be ... toll-like receptors (TLRs), killer activated and killer inhibitor receptors (KARs and KIRs), complement receptors, Fc receptors ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... Cannabinoid. receptor antagonists. *Drinabant§. *Ibipinabant§. *Otenabant§. *Rimonabant‡. *Rosonabant§. *Surinabant§. * ...
... is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors selective for the ... See also: Receptor/signaling modulators • Muscarinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists". Journal of Medicinal Chemistry. 50 (22): 5493-5508 ... heptane α4β2 nicotinic acetylcholine receptor selective agonist: Synthesis, analgesic efficacy and tolerability profile in ...
In populations of low cannabinoid receptor density, THC may act to antagonize endogenous agonists that possess greater receptor ... The actions of THC result from its partial agonist activity at the cannabinoid receptor CB1 (Ki = 10 nM[20]), located mainly in ... Nabilone, a novel synthetic cannabinoid analog (neocannabinoid). *HU-210, WIN 55,212-2, JWH-133, synthetic cannabinoid agonists ... The presence of these specialized cannabinoid receptors in the brain led researchers to the discovery of endocannabinoids, such ...
TNF receptor superfamily modulators. LTB (TNFβ). *Agonists: Lymphotoxin (α (TNFβ), β (TNFC)) ... TNF can bind two receptors, TNFR1 (TNF receptor type 1; CD120a; p55/60) and TNFR2 (TNF receptor type 2; CD120b; p75/80). TNFR1 ... tumor necrosis factor receptor binding. • cytokine activity. • identical protein binding. Cellular component. • membrane. • ... receptor biosynthetic process. • activation of MAPK activity. • immune response. • leukocyte tethering or rolling. • positive ...
Cannabinoid receptor modulators. Receptor. (ligands). CB1. *Agonists (abridged; see here for more): 2-AG ... Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor) ... "Identification of GPR55 as a lysophosphatidylinositol receptor". Biochemical and Biophysical Research Communications. 362 (4): ...
Cannabinoids (e.g., cannabis, dronabinol, nabilone). *NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone) ... σ receptors, IC50=145μM. Pharmacokinetics[edit]. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... Sigma receptor modulators. σ1. *Agonists: 3-PPP. *4-PPBP. *5-MeO-DMT ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ...
... beta-receptor agonists, follicle stimulating hormone, luteinising hormone, LHRH. gamolenic acid, gonadotropin release inhibitor ... cannabinoids, and 5-HT (serotonin) antagonists. ... General: β-receptor blockers ("beta blockers"), calcium channel ... Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ... Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ...
Cannabinoid receptor modulators. Receptor. (ligands). CB1. *Agonists (abridged; see here for more): 2-AG ... dependent modulation of type 1 cannabinoid receptors in nerve cells". Journal of Neuroscience Research. 81 (2): 275-283. doi: ... and as cholesterol-dependent modulation of CB1 cannabinoid receptors in nerve cells. The catalytic efficiency (i.e., the ratio ... "Regulation by cannabinoid receptors of anandamide transport across the blood-brain barrier and through other endothelial cells" ...
Benzodiazepines (GABA receptor agonists) *Midazolam (Versed) is given at the onset of anesthesia and has been shown in recent ... Some synthetic cannabinoids such as Nabilone (Cesamet) or the JWH series.. *Sativex is an oral spray containing THC and CBD. It ... 5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they ... NK1 receptor antagonist *Aprepitant (Emend) is a commercially available NK1 Receptor antagonist ...
serotonin receptors. *5-HT3 antagonists *Alosetron. *Cilansetron. *5-HT4 agonists *Mosapride ... Due to blockade of D2 receptors in the central nervous system, D2 receptor antagonists like metoclopramide can also produce a ... Domperidone is a peripherally selective dopamine D2 and D3 receptor antagonist.[7] It has no clinically significant interaction ... It blocks dopamine receptors in the anterior pituitary gland increasing release of prolactin which in turn increases lactation. ...
Ionotropic glutamate receptor modulators. AMPAR. *Agonists: Main site agonists: 5-Fluorowillardiine. *Acromelic acid ( ... Mathiesen O, Imbimbo BP, Hilsted KL, Fabbri L, Dahl JB (August 2006). "CHF3381, a N-methyl-D-aspartate receptor antagonist and ... See also: Receptor/signaling modulators • Adrenergics • Dopaminergics • Melatonergics • Serotonergics • Monoamine reuptake ... August 2003). "Antinociceptive activity of the N-methyl-D-aspartate receptor antagonist N-(2-Indanyl)-glycinamide hydrochloride ...
Drugs such as bromocriptine interact with the dopaminergic receptor sites as agonists with selectivity for D2 receptors, making ... designer cannabinoids. *4-HTMPIPO. *5F-AB-FUPPYCA. *5F-AB-PINACA. *5F-ADB ... Drugs such as bromocriptine act as a dopamine receptor agonist, stimulating the nerves that control movement.[13] Newer ... at the postsynaptic level at the D2 receptor site or an agonist of dopamine at the presynaptic level at the D1 receptor site.[ ...
Receptor. (ligands). DP (D2). DP1. *Agonists: Prostaglandin D2. *Treprostinil ...
Adenosine receptors Receptor. Gene. Mechanism [15]. Effects. Agonists. Antagonists A1 ADORA1. Gi/o → cAMP↑/↓ *Inhibition *↓ ... The adenosine receptors (or P1 receptors[1]) are a class of purinergic G protein-coupled receptors with adenosine as the ... A2A adenosine receptor[edit]. Main article: Adenosine A2A receptor. As with the A1, the A2A receptors are believed to play a ... A1 adenosine receptor[edit]. Main article: Adenosine A1 receptor. The adenosine A1 receptor has been found to be ubiquitous ...
Cannabinoids (e.g., cannabis, dronabinol, nabilone). *NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone) ... Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine). *Beta blockers (e.g., propranolol) ... Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors.[22] ... See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine ...
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 ...
... as well as inhibit the inhibitory effect of adenosine receptors on dopamine receptors,[67] however the implications for humans ... "Miscellaneous Sympathomimetic Agonists". In Brunton LL, Chabner BA, Knollmann BC (eds.). Goodman & Gilman's Pharmacological ... Kamiya T, Saitoh O, Yoshioka K, Nakata H (June 2003). "Oligomerization of adenosine A2A and dopamine D2 receptors in living ... Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ...
"Cannabinoid Receptors Couple to NMDA Receptors to Reduce the Production of NO and the Mobilization of Zinc Induced by Glutamate ... Other weak partial agonists of the glycine site of the NMDA receptor such as rapastinel (GLYX-13) and apimostinel (NRX-1074) ... The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel found in ... The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA and kainate receptors. ...
... κ-opioid receptor agonist and μ-opioid receptor antagonist.[4][5][6] ... with opioid receptors". Research Communications in Chemical Pathology and Pharmacology. 48 (2): 173-81. PMID 2992058.. ... with opioid receptors in isolated guinea pig ileum and mouse vas deferens preparations]". Nihon Yakurigaku Zasshi. Folia ...
... a selective agonist for PGE2 receptor subtype 3". Journal of Leukocyte Biology. 68 (2): 187-93. PMID 10947062.. ... "Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ... Prostaglandin E2 receptor 4 (EP4). അവലംബം[തിരുത്തുക]. *↑ 1.0 1.1 1.2 GRCh38: Ensembl release 89: ENSG00000050628 - Ensembl, May ...
D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 receptor antagonists (e.g., domperidone, ... Galanin receptor 1 (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.[5] ... "Galanin Receptors: GAL1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it. *v ...
Receptor. (ligands). DP (D2). DP1. *Agonists: Prostaglandin D2. *Treprostinil ... aspirin is combined with an ADP receptor inhibitor, such as clopidogrel, prasugrel, or ticagrelor to prevent blood clots. This ... via the action on arachidonic acid and NMDA receptors cascade.[101] ... "Salicylate induces tinnitus through activation of cochlear NMDA receptors". The Journal of Neuroscience. 23 (9): 3944-52. PMID ...
... which acts as a cannabinoid agonist at both the CB1 and CB2 receptors. It has mild selectivity for CB1 with a Ki of 2.3nM and ... Cited in: The cannabinoid receptors, Reggio PH (Ed), Humana Press. .mw-parser-output cite.citation{font-style:inherit}.mw- ... This cannabinoid related article is a stub. You can help Wikipedia by expanding it.. *v ... 19th Annual Symposium on the Cannabinoids, Burlington, Vermont, International Cannabinoid Research Society, Page 2. ...
Orexin receptor 1 (OX1R) signaling is implicated in cannabinoid receptor 1 (CB1R) modulation of feeding. Further, our studies ... A search for small-molecule agonists at orexin receptors is underway and could lead to a treatment for narcolepsy.. ... CB1 receptors formed homodimers, and they also heterodimerized with both orexin receptors. ... In conclusion, orexin receptors ... where the CB1 and orexin receptor 1 (OX1) receptors form the CB1-OX1 receptor heterodimer.[4][9][10] ...
The present invention relates to a method to identify a true antagonist and an inverse agonist of a cannabinoid receptor (CB), ... The wild-type CB receptor can be a CB1 receptor, or a variant thereof, a CB2 receptor, or a variant thereof. The CB agonist can ... The wild-type CB receptor can be a CB1 receptor, or a variant thereof, a CB2 receptor, or a variant thereof. The CB agonist can ... In a further embodiment the cannabinoid receptor is CB1 or CB2. In a further embodiment the cannabinoid receptor is CB1 wherein ...
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. ...
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 ...
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 ...
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 ...
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. ...
Cannabinoid Receptor Agonists May Be Novel Class Of Anti-Lymphoma Agents NEW YORK (Reuters Health) July 2002 - Delta-9- ... We are also investigating whether endogenous cannabinoids can exert antitumor activity.. Source: Cannabinoid receptor agonists ... Cannabinoid Receptor Agonists May Be Novel Class Of Anti-Lymphoma Agents​. NEW YORK (Reuters Health) July 2002 - Delta-9- ... Nagarkatti and her colleagues exposed murine lymphoma and mastocytoma cells to four cannabinoid receptor agonists. THC and two ...
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. ...
... 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 ...
... enhance the antinociceptive effects of μ-opioid receptor agonists, which suggests that combining cannabinoids with opioids ... Combinations with lower efficacy agonists might be preferred and could … ... Cannabinoid receptor agonists, such as Δ(9)-tetrahydrocannabinol (Δ(9)-THC), ... Cannabinoid receptor agonists increase the antinociceptive potency of higher efficacy opioid receptor agonists more than lower ...
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 ...
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 ...
Download Free Full-Text of an article THE EFFECT OF VERAPAMIL ON ANTI-SEIZURE PROPERTIES OF CANNABINOID CB1 RECEPTOR AGONIST IN ... In this research, the effects of an L-type calcium channel blocker (verapamil) and a cannabinoid CB1 receptor agonist (ACEA) on ... THE EFFECT OF VERAPAMIL ON ANTI-SEIZURE PROPERTIES OF CANNABINOID CB1 RECEPTOR AGONIST IN PENTYLENETETRAZOLE MODEL OF SEIZURE ... Cannabinoids play a role in setting the threshold of excitability of neurons through the presynaptic CB1 receptor. Calcium ...
... 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 ...
Cannabinoid receptor, drug design, docking, inverse agonist, membrane protein, GPCR.. Abstract:. Background: Cannabinoid ... Pertwee, R.G. Emerging strategies for exploiting cannabinoid receptor agonists as medicines. Br. J. Pharmacol., 2009, 156(3), ... Advances in the Understanding of the Cannabinoid Receptor 1 - Focusing on the Inverse Agonists Interactions. Author(s): Silvana ... Ibsen, M.S.; Connor, M.; Glass, M. Cannabinoid CB1 and CB2 receptor signaling and bias. Cannabis Cannabinoid Res., 2017, 2(1), ...
Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid ... Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid ... synthesis in prostate cancer cells that is not affected by androgen receptor status. ... Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid ...
Home , Papers , The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain ... 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 ... Irritant-evoked activation and calcium modulation of the TRPA1 receptor. * Quantitative differences in neuronal subpopulations ...
Low-Dose Cannabinoid Type 2 Receptor Agonist Attenuates Tolerance to Repeated Morphine Administration via Regulating μ-Opioid ... Receptor Expression in Walker 256 Tumor-Bearing Rats.. Low-Dose Cannabinoid Type 2 Receptor Agonist Attenuates Tolerance to ... Home , Papers , Low-Dose Cannabinoid Type 2 Receptor Agonist Attenuates Tolerance to Repeated Morphine Administration via ... Repeated Morphine Administration via Regulating μ-Opioid Receptor Expression in Walker 256 Tumor-Bearing Rats. ...
... , Login ... Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2. ... Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2. ... Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2 ...
Full agonist 480 nM Full agonist Endogenous Tetrahydrocannabinol 10 nM Partial agonist 24 nM Partial agonist Phytogenic [42][42 ... Cannabinoid receptor type 1 (CB1), also known as cannabinoid receptor 1, is a G protein-coupled cannabinoid receptor that in ... cannabinoid receptor 1 (brain), cannabinoid receptor 1, cannabinoid CB1 receptor gene. ... Selective CB1 agonists may be used to isolate the effects of the receptor from the CB2 receptor, as most cannabinoids and ...
What Is A Cannabinoid Drug, What Is A Cannabinoid Receptor, What Is A Cannabinoid Receptor Agonist, What Is A Cannabinoid ... What Does Cannabinoid Mean, What Does Cannabinoid Oil Do, What Does Cannabinoid Receptors Do, What Does Cannabinoid Receptors ... What Activates Cannabinoid Receptors, What Cannabinoid Receptors Do, What Cannabinoids Do, What Causes Cannabinoid Hyperemesis ... What Is Cannabinoids Thc, What Is Cannabinoids Used For, What Is Cb1 Cannabinoid Receptor, What Is Cbc Cannabinoid, What Is ...
  • The present invention relates to a method to identify a true antagonist and an inverse agonist of a cannabinoid receptor (CB), and to discriminate between them. (freepatentsonline.com)
  • These effects were blocked by pretreatment with the CB(2) receptor-selective antagonist SR144528, but not by the CB(1) receptor antagonist, rimonabant. (nih.gov)
  • Evidence that the plant cannabinoid cannabigerol is a highly potent alpha2-adrenoceptor agonist and moderately potent 5HT1A receptor antagonist. (nih.gov)
  • At 10 microM, it also behaved as a CB(1) receptor competitive antagonist. (nih.gov)
  • The 3D structure reveals the binding mode of WIN 55,212-2 and structural determinants for distinguishing CB2 agonists from antagonists, which are supported by a pair of rationally designed agonist and antagonist. (rcsb.org)
  • Pretreatment with WIN 55,212-2 (0.001, 0.01 or 0.1 mg/kg) significantly and dose-dependently reduced tracheal plasma extravasation induced by inhaling a 5% ovalbumin solution for 2 min after pretreatment with a neutral endopeptidedase inhibitor (phosphoramidon at 2.5 mg/kg i.v.). A cannabinoid CB2 receptor antagonist (SR144528) blunted the inhibitory effect of WIN 55,212-2, while a cannabinoid CB1 antagonist (SR141716A) did not. (unboundmedicine.com)
  • Pretreatment with a neurokinin-1 receptor antagonist (FK888) significantly reduced ovalbumin-induced extravasation of Evans blue dye. (unboundmedicine.com)
  • The effects of the cannabinoid (CB)-receptor agonists WIN55,212-2 and HU-210 and the selective CB 1 -receptor antagonist SR141716A were tested on in vitro and in vivo acid secretion assays from the rat. (springer.com)
  • Involvement of cannabinoid CB(2) receptor and effect of cannabinoid CB(2) receptor antagonist/inverse agonists on cutaneous inflammation were investigated. (qxmd.com)
  • These results suggest that cannabinoid CB(2) receptor is partially involved in local inflammatory responses and cannabinoid CB(2) receptor antagonist/inverse agonist has beneficial effects on ear swelling. (qxmd.com)
  • CB 2 -mediated effects in vivo were reversed by concurrent treatment with a CB 2 antagonist/inverse agonist but not with a CB 1 antagonist/inverse agonist. (elsevier.com)
  • 2 Inhibition of twitch responses and ACh release by CB agonists was reversed by the CB1-selective cannabinoid receptor antagonist, SR141716A. (elsevier.com)
  • Oral administration of Imidazole 24b blocked CP-55940-induced hypothermia, demonstrating cannabinoid CB(1) receptor antagonist efficacy in vivo. (scienceexchange.com)
  • It is a tricyclic aryl derivative that acts as a competitive antagonist at the CB2 cannabinoid receptor. (wikipedia.org)
  • In Experiment 2, rats were given morphine (10 mg/kg) once a day for 14 days in combination with either vehicle, CP 55,940 (0.1 mg/kg) or the cannabinoid CB 1 receptor antagonist SR 141716 (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H- pyrazole-3-carboxamide hydrochloride) (3 mg/kg). (edu.au)
  • Findings that the CB 1 selective antagonist/inverse agonist SR141716A produces in vivo and in vitro signs of increased motility of rodent small intestine probably reflect the presence in the enteric nervous system of a population of CB 1 receptors that are precoupled to their effector mechanisms. (bmj.com)
  • Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. (selleckchem.com)
  • 6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM. (selleckchem.com)
  • This stimulation was prevented by AM630, a CB 2 cannabinoid receptor-selective antagonist and was not observed in skin from CB 2 cannabinoid receptor-deficient mice. (pnas.org)
  • It mimics the effects of estradiol with varying agonist and antagonist effects. (drugbank.ca)
  • Propranolol is also non-specific 5-HT 1A, 5-HT 1B and 5-HT 1C serotonin receptor antagonist. (sigmaaldrich.com)
  • Metabolite of the chemotherapeutic drug tamoxifen, exhibiting more potent estrogen agonist/antagonist activity than the parent drug. (sigmaaldrich.com)
  • The invention further relates to the use of these true antagonists and inverse agonists in the treatment of CB associated disorders such as obesity, psychiatric and neurological disorders. (freepatentsonline.com)
  • These effects were reversed by CB1 and CB2 antagonists AM 251 and SR144528, respectively, suggesting involvement of CB1 and CB2 receptors. (aacrjournals.org)
  • In addition, granulocyte colony-stimulating factor -induced mobilization of HSPCs was significantly decreased by specific CB₂ antagonists and was impaired in Cnr2(-/-) cannabinoid type 2 receptor knockout mice. (420magazine.com)
  • Methods and Results- In spontaneously hypertensive rats (SHR), cannabinoid-1 receptor (CB 1 ) antagonists increase blood pressure and left ventricular contractile performance. (ahajournals.org)
  • Treatment of normotensive rats and mice with CB 1 antagonists alone does not affect blood pressure, 3,5 and baseline blood pressure is similar in CB 1 -knockout mice and their wild-type littermates, 12,13 which indicates that CB 1 receptors are not tonically active. (ahajournals.org)
  • The extent to which the effects on gastrointestinal function of cannabinoid receptor agonists or antagonists/inverse agonists can be exploited therapeutically has yet to be investigated as has the extent to which these drugs can provoke unwanted effects in the gastrointestinal tract when used for other therapeutic purposes. (bmj.com)
  • The discovery of cannabinoid receptors also instigated a quest for selective CB1 and CB2 receptor antagonists, with varying degrees of success so far. (news-medical.net)
  • therapeutic uses of agonists and antagonists of cannabinoids receptors. (booktopia.com.au)
  • Experimental findings suggesting that activation of peripheral (noncentral nervous system) CB 2 receptors is necessary and sufficient to inhibit pain responses come from site-specific injections of CB 2 receptor-selective agonists and antagonists ( 1 , 3 , 4 ). (pnas.org)
  • Here, we show that bone marrow stromal cells express endocannabinoids (anandamide and 2-arachidonylglycerol), whereas CB₂ receptors are expressed in human and murine HSPCs. (420magazine.com)
  • However, the activities of these agonists were different in the two assays with anandamide and CP-55,940 being markedly less efficacious in stimulating the accumulation of cAMP than in inhibiting its formation. (aspetjournals.org)
  • Studies examining the effects of forskolin on cannabinoid receptor mediated stimulation of adenyly cyclase also revealed differences among agonists in as much as forskolin enhanced the potency of HU-210 and CP-55,940 by ∼100-fold but, by contrast, had no effect on the potency of WIN-55212-2 or anandamide. (aspetjournals.org)
  • The endocannabinoids anandamide and 2-arachidonyl glycerol (2-AG) bind to G protein-coupled central and peripheral cannabinoid receptors CB1 and CB2, respectively. (aspetjournals.org)
  • These studies compare and contrast the potency and efficacy of anandamide, 2-AG, and the synthetic cannabinoid HU210 at hCB2. (aspetjournals.org)
  • Using [ 35 S]guanosine-5′- O -(3-thio)triphosphate (GTPγS) and radioligand bindings in insect Sf9-hCB2 membranes, we showed that both endocannabinoids bound hCB2 with similar affinity and that the cannabinoids acted as full agonists in stimulating [ 35 S]GTPγS exchange, although 2-AG was 3-fold more potent than anandamide (EC 50 = 38.9 ± 3.1 and 121 ± 29 nM, respectively). (aspetjournals.org)
  • To this end, we initiated comparative characterization of 2-AG, anandamide, and the "classical" dibenzopyran cannabinoid HU210 with human CB2 (hCB2). (aspetjournals.org)
  • Moreover, as a weak partial agonist at hCB2, anandamide attenuated 2-AG activation of hCB2. (aspetjournals.org)
  • Association of cannabimimetic compounds such as cannabinoids, aminoalkylindoles (AAIs), and arachidonylethanolamide (anandamide) with the brain cannabinoid (CB(1)) receptor activates G-proteins and relays signals to regulate neuronal functions. (nih.gov)
  • The primary endogenous agonist of the human CB 1 receptor is anandamide . (wikipedia.org)
  • 4 The endogenous cannabinoid ligands arachidonoyl ethanolamide (anandamide) and 2-arachidonoylglycerol (2-AG) also lower blood pressure and heart rate in rodents. (ahajournals.org)
  • Endogenous cannabinoids such as palmitoylethanolamide ( PEA ) and N-arachidonoylethanolamine (anandamide or AEA), were found in peripheral tissues and have been proposed to possess autacoid activity, implying that cannabinoids may downregulate mast cell activation and local inflammation . (bvsalud.org)
  • These results constitute the initial identification and characterization of a potent, high-affinity, hCB1R-selective covalent agonist with utility as a pharmacologically active, orthosteric-site probe for providing insight into structure-function correlates of ligand-induced CB1R activation and the molecular features of that activation by the native ligand, anandamide. (scripps.edu)
  • The term cannabinoids is used in this chapter to refer to a group of substances that are structurally related to THC by virtue of a tricyclic chemical structure or that bind to cannabinoid receptors, such as the natural ligand anandamide. (nap.edu)
  • Endogenous ligands for cannabinoid receptors have been identified, the most important being anandamide (arachidonylethanolamide) and 2-arachidonyl glycerol (2-AG). (bmj.com)
  • Among these endocannabinoids, arachidonoyl-ethanolamide (also known as anandamide) was among the first to be discovered, and there is compelling evidence that this ligand (as well as some of its metabolites) may also activate vanilloid VRI receptors. (news-medical.net)
  • Anandamide behaves as a partial agonist of cannabinoid receptors with slightly greater CB1 than CB2 affinity, but with much lower CB2 than CB1 efficacy . (news-medical.net)
  • cannabinoid receptor ligands also known as endocannabinoids are characterized by arachidonyl ethanolamide (anandamide, AEA) and 2-arachidonoyl glycerol (2-AG) [ 1 , 2 ] and the enzymes involved in synthesis and degradation of the endocannabinoids. (hindawi.com)
  • Compounds that bind CB2 receptors selectively induce apoptosis in these cancer cells, she said. (420magazine.com)
  • In order to investigate the effect of cannabinoid receptor -1 (CB1R) agonists on mast cell activation, AEA-derived compounds were newly synthesized and evaluated for their effect on mast cell activation. (bvsalud.org)
  • Cannabinoids are a group of terpenophenolic compounds present in Cannabis (''Cannabis sativa'') and occur naturally in the nervous and immune systems of animals. (news-medical.net)
  • Cannabinoids are naturally occurring compounds found in the Cannabis sativa plant. (news-medical.net)
  • Of over 480 different compounds present in the plant, only around 66 are termed cannabinoids. (news-medical.net)
  • Both types of compounds mimic endogenous ligands and act through distinct G-protein-coupled receptor families known as cannabinoid ( Felder and Glass, 1998 ) and opioid ( Kieffer, 1995 ) receptors. (jneurosci.org)
  • Cross-dependence between opioid and cannabinoid compounds has also been reported. (jneurosci.org)
  • The plant Cannabis sativa is the source of a set of more than 60 oxygen containing aromatic hydrocarbon compounds called cannabinoids, of which Δ 9 -tetrahydrocannabinol (Δ 9 -THC) is the main psychotropic constituent. (bmj.com)
  • Described during the late 1980s and 1990s, cannabinoid receptors (CB1R and CB2R) are G-protein-coupled receptors (GPCRs) activated by endogenous ligands and cannabinoid drug compounds, such as Δ9-THC. (drugdiscoverytoday.com)
  • Cannabinoids represent a promising class of compounds for developing novel therapeutic agents. (springer.com)
  • These compounds primarily target the cannabinoid receptors 1 (CB1) and Cannabinoid receptors 2 (CB2). (springer.com)
  • An escalating number of compounds with cannabinoid receptor activity are currently being found as ingredients of Spice, of which almost nothing is known in terms of pharmacology, toxicology, and safety. (frontiersin.org)
  • New cannabimimetic compounds are likely to be synthesized in the near future to replace banned synthetic cannabinoids, leading to a "dog chasing its tail" situation. (frontiersin.org)
  • Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS. (nih.gov)
  • Compounds that inhibit or block the activity of CANNABINOID RECEPTORS. (nih.gov)
  • Compounds and drugs that inhibit or block the activity of CCR5 RECEPTORS. (nih.gov)
  • Cannabis sativa is a herbaceous plant that represents a source of more than sixty aromatic hydrocarbon compounds known as cannabinoids, and among them delta-9-tetrahydrocannabinol (usually abbreviated as THC) is the main psychotropic constituent. (news-medical.net)
  • The number of synthetic cannabinoids, their chemical diversity and the speed of their emergence make this group of compounds particularly challenging in terms of detection, monitoring, and responding. (europa.eu)
  • Objective: Our goal here is to review the studies on CB1, starting with general aspects and focusing on the recent structural studies, with emphasis on the inverse agonists bound structures. (eurekaselect.com)
  • We also describe the molecular docking method to obtain complex structures of CB 1 with inverse agonists. (eurekaselect.com)
  • Results: Analysis of the crystallographic structure and docking results revealed the residues responsible for the specificity of the inverse agonists for CB 1. (eurekaselect.com)
  • Conclusion: Analysis of the structures involving inverse agonists and CB 1 revealed the pivotal role played by residues Phe 170 and Leu 359 in their interactions and the strong intermolecular hydrogen bonds highlighting the importance of the exploration of intermolecular interactions in the development of novel inverse agonists. (eurekaselect.com)
  • Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists. (qxmd.com)
  • These findings suggest that selective cannabinoid CB(1) receptor inverse agonists such as Imidazole 24b have potential for the treatment of obesity. (scienceexchange.com)
  • Endocannabinoids are arachidonic acid derivatives and part of a novel bioactive lipid signaling system, along with their G-coupled cannabinoid receptors (CB₁ and CB₂) and the enzymes involved in their biosynthesis and degradation. (420magazine.com)
  • Collectively, the data showed that both endocannabinoids bound hCB2 with similar affinity, but only 2-AG functioned as a full agonist. (aspetjournals.org)
  • We showed that although both endocannabinoids bound hCB2 with similar affinity, only 2-AG functioned as a full agonist in stimulating [ 35 S]guanosine-5′- O -(3-thio)triphosphate (GTPγS) exchange and inhibiting cAMP. (aspetjournals.org)
  • [13] The CB 1 receptor is activated by cannabinoids , generated naturally inside the body ( endocannabinoids ) or introduced into the body as cannabis or a related synthetic compound. (wikipedia.org)
  • The therapeutic potential of drugs that target cannabinoid receptors or modulate the tissue levels or actions of endocannabinoids. (springer.com)
  • Furthermore, the existence of endogenous ligands that bind to these receptors (termed "endocannabinoids") has also been demonstrated, pointing towards the pharmacological and physiological importance of cannabinoid receptors. (news-medical.net)
  • AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. (selleckchem.com)
  • Supplementary Fig. 1), the main active component of the hemp plant Cannabis sativa ( 6 ), exerts a wide variety of biological effects by mimicking endogenous substances-the endocannabinoids-that bind to and activate specific cannabinoid receptors ( 7 ). (aacrjournals.org)
  • These findings suggest that WIN 55,212-2 inhibits C-fiber activation via the cannabinoid CB2 receptor and thus suppresses antigen-induced inflammation in guinea pig airways. (unboundmedicine.com)
  • Fukuda H, Abe T, Yoshihara S. The cannabinoid receptor agonist WIN 55,212-2 inhibits antigen-induced plasma extravasation in guinea pig airways. (unboundmedicine.com)
  • TY - JOUR T1 - The cannabinoid receptor agonist WIN 55,212-2 inhibits antigen-induced plasma extravasation in guinea pig airways. (unboundmedicine.com)
  • Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone (SAB378), a peripherally restricted cannabinoid CB1/CB2 receptor agonist, inhibits gastrointestinal motility but has no effect on experimental colitis in mice. (qxmd.com)
  • Pharmacologically, AM3677 acts as a high-affinity, low-efficacy CB1R agonist that inhibits forskolin-stimulated cellular cAMP formation and stimulates CB1R coupling to G protein. (scripps.edu)
  • CB 2 receptor activation inhibits acute, inflammatory, and neuropathic pain responses but does not cause central nervous system (CNS) effects, consistent with the lack of CB 2 receptors in the normal CNS. (pnas.org)
  • Activation of CB 2 cannabinoid receptors inhibits nociception to thermal and mechanical stimuli ( 1 , 2 ), thermal and tactile hypersensitivity produced by peripheral inflammation ( 2 - 4 ), and tactile and thermal hypersensitivity produced in a neuropathic pain model ( 5 ). (pnas.org)
  • Cannabinoid WIN-55,212-2 mesylate inhibits interleukin-1β induced matrix metalloproteinase and tissue inhibitor of matrix metalloproteinase expression in human chondrocytes. (soft-tox.org)
  • Buprenorphine is a partial agonist of the μ-opioid receptor, and tramadol is a serotonin norepinephrine reuptake inhibitor (SNRI) with weak μ-opioid receptor agonist properties. (wikipedia.org)
  • Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. (selleckchem.com)
  • Science, 2000, Vol. 289, pp. 739-745) in the conformation most likely to represent the "high-affinity" state for agonist binding to G-protein coupled receptors (GPCRs). (nih.gov)
  • The cannabinoid 1 receptor (CB1R) is one of the most abundant G protein-coupled receptors (GPCRs) in the central nervous system. (scripps.edu)
  • It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. (selleckchem.com)
  • Following agonist activation, G-protein-coupled receptors (GPCRs) recruit β-arrestin, which desensitizes heterotrimeric G-protein signalling and promotes receptor endocytosis1. (stanford.edu)
  • GABAB belongs to the Family C of G protein-coupled receptors (GPCRs), which operate as dimers to relay synaptic neurotransmitter signals into a cellular response through the binding and activation of heterotrimeric G proteins2,3. (stanford.edu)
  • In biochemical studies, chronic alcohol treatment increased the levels of the endogenous ligands for cannabinoid receptors arachidonoylethanolamide and 2-arachidonoyl-glycerol ( Basavarajappa and Hungund, 2002 ). (jneurosci.org)
  • Both the receptors and their endogenous ligands comprise the endocannabinoid system . (news-medical.net)
  • The endogenous ligands of cannabinoid receptors CB1 and CB2, mainly metabolized by the fatty acid amide hydrolase and the monoacylglycerol lipase, induce antinociceptive effects [ 2 , 3 ]. (mdpi.com)
  • On ligand stimulation with CB₂ agonists, CB₂ receptors induced chemotaxis, migration, and enhanced colony formation of bone marrow cells, which were mediated via ERK, PI3-kinase, and Gαi-Rac1 pathways. (420magazine.com)
  • Further structural analyses with computational docking results uncover the differences between CB2 and CB1 in receptor activation, ligand recognition, and G i coupling. (rcsb.org)
  • We evaluated two alternative binding conformations, C3-in and C3-out, denoting the directionality of the ligand C3 side chain within the receptor with respect to the inside or the outside of the cell. (nih.gov)
  • Assuming both the C3-in or C3-out conformation, the calculated ligand-receptor binding energy (DeltaE(bind)) was correlated with the experimentally observed binding affinity (K(i)) for a series of nonclassical cannabinoid agonists. (nih.gov)
  • Adopting the C3-in conformation due to the greater number of receptor interactions with known pharmacophoric elements of the ligand, key residues were identified comprising the presumed hydrophobic pocket that interacts with the C3 side chain of cannabinoid agonists. (nih.gov)
  • In summary, the present study represents one of the first attempts to construct a homology model of the CB(1) cannabinoid receptor based upon the published bovine rhodopsin x-ray crystal structure and to elucidate the putative ligand binding site for nonclassical cannabinoid agonists. (nih.gov)
  • We postulated sites of the CB(1) receptor critical for the ligand interaction, including the hydrophobic pocket interacting with the key pharmacophoric moiety, the C3 side chain. (nih.gov)
  • The present study provides a consistent framework for further investigation of the CB(1) receptor-ligand interaction and for the study of CB(1) receptor activation. (nih.gov)
  • Why do cannabinoid receptors have more than one endogenous ligand? (royalsocietypublishing.org)
  • 2008. Crystal structure of the ligand-free G-protein-coupled receptor opsin. (springer.com)
  • The receptor for bigLEN is GPR171, which was an orphan G protein-coupled receptor (GPCR) until this ligand was identified. (sciencemag.org)
  • These two ligand-receptor pairs altered each other's pharmacological properties. (sciencemag.org)
  • Knowing the ligand for GPR83 will enable the investigation of how GPR83, GPR171, and other receptors interact to control body weight, which has implications for treating metabolic disorders associated with being underweight or overweight. (sciencemag.org)
  • Lasofoxifene mediates an agonist effect on estrogen receptors expressed on bone to mimic the positive effects of estrogen to reduce the production and lifespan of osteoclasts via altering the NF-kappaB ligand (RANKL)/RANK/osteoprotegerin system, stimulation of osteoblast (the bone forming cells) activity and additional effects on calcium homeostasis [ 4 ] . (drugbank.ca)
  • The activation of the CB 1 and CB 2 receptors causes the numerous intracellular effects which may be cell type and ligand specific and involve the inhibition of various voltage gated Ca +2 channels and adenylate cyclase activity and the activation of K + channels, resulting in lower levels of cAMP along with activation of MAPK pathways [ 5 ]. (hindawi.com)
  • Liu, Z.J. Crystal structures of agonist-bound human cannabinoid receptor CB1. (eurekaselect.com)
  • The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB 1 receptor stably expressed in Chinese hamster ovary (CHO) cells. (elsevier.com)
  • Yamamura, Henry I. / AM630 is an inverse agonist at the human cannabinoid CB 1 receptor . (elsevier.com)
  • To further investigate the inhibitory effects of CB1R agonist in vivo, an oxazolone -induced atopic dermatitis mouse model was exploited. (bvsalud.org)
  • We found that CB1R inhibited the release of inflammatory mediators without causing cytotoxicity in RBL-2H3 cells and that CB1R agonists markedly and dose -dependently suppressed mast cell proliferation indicating that CB1R plays an important role in modulating antigen -dependent immunoglobulin E ( IgE )-mediated mast cell activation. (bvsalud.org)
  • We also found that topical application of CB1R agonists suppressed the recruitment of mast cells into the skin and reduced the level of blood histamine . (bvsalud.org)
  • Our results indicate that CB1R agonists down-regulate mast cell activation and may be used for relieving inflammatory symptoms mediated by mast cell activation, such as atopic dermatitis , psoriasis , and contact dermatitis . (bvsalud.org)
  • Methods Firstly, the antitumor activity was tested for the combination of cannabinoid receptor 1 (CB1R) receptor agonist WIN55212-2 with each of 25 antitumor drugs using three tumor cell lines with high CB1R, HepG2, DU145 and HCT-8, by highthroughput assay. (bvsalud.org)
  • AM3677 also induces CB1R endocytosis and irreversible receptor internalization. (scripps.edu)
  • Whereas CB1R has a role in the regulation of neurotransmission in different brain regions and mainly mediates the psychoactive effects of cannabinoids, CB2R is found predominantly in the cells and tissues of the immune system and mediates anti-inflammatory and immunomodulatory processes. (drugdiscoverytoday.com)
  • In addition, we analyzed the diurnal variation of the expression of the cannabinoid receptors CB1R and CB2R in the cerebral cortex of both control rats and rats subjected to TBI. (mdpi.com)
  • Although Δ(9)-tetrahydrocannabinol (THC) and other mixed CB(1)/CB(2) receptor agonists are well established to elicit antinociceptive effects, their psychomimetic actions and potential for abuse have dampened enthusiasm for their therapeutic development. (nih.gov)
  • Cannabinoid receptor agonists, such as Δ(9)-tetrahydrocannabinol (Δ(9)-THC), enhance the antinociceptive effects of μ-opioid receptor agonists, which suggests that combining cannabinoids with opioids would improve pain treatment. (nih.gov)
  • The antinociceptive effects of μ-opioid receptor agonists alone and in combination with cannabinoid receptor agonists were studied in rhesus monkeys (n = 4) using a warm water tail withdrawal procedure. (nih.gov)
  • The antinociceptive effects of the CB 2 receptor-selective agonist AM1241 were prevented in rats when naloxone or antiserum to β-endorphin was injected in the hindpaw where the noxious thermal stimulus was applied, suggesting that β-endorphin is necessary for CB 2 receptor-mediated antinociception. (pnas.org)
  • One type of cells that might mediate the actions of CB 2 receptor-selective agonists is keratinocytes, which have been reported to express CB 2 receptors ( 11 ) and to contain endogenous opioid peptides ( 12 - 14 ) and which are found in abundance in skin, where nociceptive stimuli have been applied when testing the antinociceptive effects of CB 2 receptor-selective agonists. (pnas.org)
  • Whereas cannabinoids are consistently shown to attenuate neuropathic pain, the efficacy of opioids is highly controversial. (aspetjournals.org)
  • These results indicate that, after nerve injury, opioids lose their capability to suppress C-fiber-induced spinal neuron activation in the injured L 5 but not in the intact L 4 spinal segment, whereas cannabinoids still maintain their efficacy. (aspetjournals.org)
  • however, it is unclear whether interactions between opioids and cannabinoids vary across drugs with different efficacy. (nih.gov)
  • The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained efficacy and attenuates morphine tolerance and dependence. (painresearchforum.org)
  • 3,5 However, an increase in the hypotensive efficacy of cannabinoids has been noted in spontaneously hypertensive rats (SHR). (ahajournals.org)
  • Several studies have shown that these phytocannabinoids show affinity, potency, selectivity, and efficacy towards cannabinoid receptors and inhibit endocannabinoid metabolizing enzymes, thus reducing hyperactivity of endocannabinoid systems. (hindawi.com)
  • Taken together, these results demonstrate that the endocannabinoid system is involved in hematopoiesis and that CB₂/CB₂ agonist axis mediates repopulation of hematopoiesis and mobilization of HSPCs. (420magazine.com)
  • Antiinflammatory action of endocannabinoid palmitoylethanolamide and the synthetic cannabinoid nabilone in a model of acute inflammation in the rat. (qxmd.com)
  • Endocannabinoid precursors are present in the fat molecules in the cell membrane and are released upon demand, when the endocannabinoid receptors are activated. (medicinenet.com)
  • Endocannabinoid receptors are concentrated in the brain, but are also present in nerve tissues all over the body. (medicinenet.com)
  • Two of them, tetrahydrocannabinol (THC) and cannabidiol (CBD), bind to the human endocannabinoid receptors CB1-R and CB2-R. Both THC and CBD have medical benefits, but only THC produces euphoric effects. (medicinenet.com)
  • The cannabis plant contains other minor cannabinoids that interact with the human endocannabinoid system, but their effects are far weaker and they are present in lower concentrations. (medicinenet.com)
  • This entry was posted in Endocannabinoid System , Stroke , THC (Delta-9-Tetrahydrocannabinol) and tagged agonists , anti-inflammatory , cannabinoid , cannabinoid receptors , Cannabinoids , CB2 by David . (thctotalhealthcare.com)
  • The 21st century will witness the unprecedented marketing of therapeutic drugs developed from cannabinoids and the endocannabinoid system. (booktopia.com.au)
  • Moreover, this compound can serve as a template to develop new CB(2) receptor agonists with increased receptor selectivity and increased potency in treating inflammatory and neuropathic pain. (nih.gov)
  • These conflicting data may result from differences in the type of nerve injury, route of drug administration, potency and receptor selectivity of the particular opioid agonist, and the methods of measuring neuropathic pain. (aspetjournals.org)
  • Following on from the promising activity of a series of 4-oxo-1,4-dihydroquinoline-3-carboxamide, we developed constrained analogues based on a 2H-pyrazolo[4,3-c]quinolin-3(5H)-one scaffold, with improved affinity for the hCB2 receptor and had very high selectivity over the hCB1 receptor. (uclouvain.be)
  • Selectivity of cannabinor for human and rat CB receptors was evaluated. (elsevier.com)
  • Cannabinor exhibited similar binding at human and rat CB2 receptors and a 321-fold functional selectivity for the CB2 receptor versus the CB1 receptor. (elsevier.com)
  • The cannabinoid receptor agonists that have been used extensively in pharmacological experiments show equal binding affinity for both CB1 and CB2 receptors, or show merely marginal CB1 or CB2 selectivity. (news-medical.net)
  • AM-1241 is a selective cannabinoid CB2 receptor agonist with K i of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. (selleckchem.com)
  • BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with K i of 435 nM, with 50-fold selectivity over CB1 receptor. (selleckchem.com)
  • Abood, M.E. Cannabinoid receptors: nomenclature and pharmacological principles. (eurekaselect.com)
  • Surprisingly, neither pharmacological inhibition nor genetic ablation of CB2 had any effect on CB2 agonist-induced macrophage chemotaxis. (ox.ac.uk)
  • The future of medical marijuana lies in classical pharmacological drug development, and indeed there has been a resurgence of scientific, as well as public, interest in the therapeutic applications of cannabinoids. (nap.edu)
  • Of the other plant cannabinoids, those which have been most investigated are Δ 8 -THC which has similar pharmacological properties to Δ 9 -THC, cannabinol, which has much weaker psychotropic properties than Δ 9 -THC, and cannabidiol, which lacks psychotropic activity. (bmj.com)
  • Since cannabinoids are characterized by low water and high lipid solubility, their pharmacological properties were classically ascribed to the perturbation of biological membranes and their phospholipid components. (news-medical.net)
  • In any case, the above-mentioned distribution pattern of CB1 receptors accounts for several notable pharmacological properties of their agonists, e.g. their tendency to impair memory and cognition, as well as to alter the motor function control. (news-medical.net)
  • The aim of this study was to evaluate the impact of ACEA (arachidonyl-2′-chloroethylamide-a highly selective cannabinoid CB1 receptor agonist) combined with a classical antiepileptic drug sodium valproate (VPA) on neural precursor cells׳ proliferation and differentiation in the mouse brain. (deepdyve.com)
  • Additionally, chronic alcohol exposure induced a decrease in the number of CB 1 receptors and a desensitization of the cannabinoid-activated signal transduction ( Basavarajappa and Hungund, 2002 ). (jneurosci.org)
  • This compound is featured on the Cannabinoid Receptors page of the Handbook of Receptor Classification and Signal Transduction. (sigmaaldrich.com)
  • Experimental evidence has shown that cannabinoids inhibit the growth of tumor xenograft in mice ( 8 , 11 - 14 ). (aacrjournals.org)
  • In this research, the effects of an L-type calcium channel blocker (verapamil) and a cannabinoid CB1 receptor agonist (ACEA) on pentylenetetrazole-induced seizure model in mice were studied. (sid.ir)
  • Mice ears topically exposed to an ether-linked analogue of 2-arachidonoylglycerol (2-AG-E) or selective cannabinoid CB(2) receptor agonist, {4-[4-(1,1-dimethylheptyl)-2,6-dimethoxy-phenyl]-6.6-dimethyl-bicyclo[3.1.1]hept-2-en-2-yl}-methanol (HU-308), had early and late ear swelling (0--24 h and 1--8 days after exposure, respectively). (qxmd.com)
  • Involvement of cannabinoid CB2 receptors in the IgE-mediated triphasic cutaneous reaction in mice. (qxmd.com)
  • The cannabinoid CB2 receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis. (qxmd.com)
  • 11 Cannabinoids fail to lower blood pressure after selective blockade of CB 1 5 or in CB 1 -knockout mice, 12,13 which implicates CB 1 in this effect. (ahajournals.org)
  • The specific CB2 cannabinoid receptor agonist JWH-133 induced cognitive improvement in double AβPP/PS1 transgenic mice, a genetic model of Alzheimer's disease. (scicombinator.com)
  • Administration had no effect in cannabinoid CB(1) receptor-deficient mice. (scienceexchange.com)
  • To investigate the molecular basis for cannabinoid dependence and its possible relationship with the endogenous opioid system, we explored Δ9-tetrahydrocannabinol (THC) activity in mice lacking μ-, δ- or κ-opioid receptor genes. (jneurosci.org)
  • Further, AM1241 did not inhibit nociception in μ-opioid receptor-deficient mice. (pnas.org)
  • The present study evaluated the actions and ability of these small-molecule agonists to counteract experimental diabetes in mice. (springer.com)
  • Mechanism of action of agonists was assessed in acute studies using incretin-receptor-knockout mice. (springer.com)
  • Acute studies in Gipr - and Glp1r -knockout mice revealed an important role for the glucagon-like peptide 1 (GLP-1) receptor in the actions of both agonists, with the glucose-lowering effects of Abn-CBD also partly mediated through the glucose-dependent insulinotropic peptide (GIP) receptor. (springer.com)
  • Thus, cannabinoid administration curbs the growth of several types of tumor xenografts in rats and mice ( 11, 12 ) including gliomas ( 13-16 ). (aacrjournals.org)
  • Cannabidiol analogues which bind cannabinoid receptors but exert peripheral activity only. (qxmd.com)
  • Abnormal cannabidiol (Abn-CBD) and AS-1269574 are potent selective agonists for GPR55 and GPR119, respectively. (springer.com)
  • 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)
  • The results showed that inhibition of L-type calcium channel by verapamil did not affect the anti-seizure properties of cannabinoid CB1 receptor agonist. (sid.ir)
  • 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)
  • Orally administered JTE-907 (0.1-10 mg/kg) and SR 144528 (1 mg/kg) also produced significant inhibition of dinitrofluorobenzene-induced ear swelling, with increased cannabinoid CB(2) receptor mRNA expression observed in the inflamed ear. (qxmd.com)
  • 1 The dose-related inhibition of the twitch responses of the myenteric plexus-longitudinal muscle preparation of the guinea-pig small intestine by cannabinoid (CB) agonists, (+)-WIN 55212 and CP 55940 during stimulation at 0.1 Hz with supramaximal voltage was confirmed. (elsevier.com)
  • Coutts, AA & Pertwee, RG 1997, ' Inhibition by cannabinoid receptor agonists of acetylcholine release from the guinea-pig myenteric plexus ', British Journal of Pharmacology , vol. 121, no. 8, pp. 1557-1566. (elsevier.com)
  • To date, there has been virtually no information regarding the mechanism of CB 2 receptor-mediated inhibition of pain responses. (pnas.org)
  • However, enthusiasm for this therapeutic approach has been tempered by the lack of information regarding the mechanism underlying the inhibition of nociceptive responses by CB 2 receptor activation. (pnas.org)
  • GABA (γ-aminobutyric acid) stimulation of the metabotropic GABAB receptor results in prolonged inhibition of neurotransmission that is central to brain physiology1. (stanford.edu)
  • have shown that opioids [especially μ-opioid receptor (MOR) agonists] can be effective in treating neuropathic pain. (aspetjournals.org)
  • Low-Dose Cannabinoid Type 2 Receptor Agonist Attenuates Tolerance to Repeated Morphine Administration via Regulating μ-Opioid Receptor Expression in Walker 256 Tumor-Bearing Rats. (painresearchforum.org)
  • Morphine , the archetypal opioid , and other opioids (e.g., codeine , oxycodone , hydrocodone , dihydromorphine , pethidine ) all exert a similar influence on the cerebral opioid receptor system. (wikipedia.org)
  • This investigation addressed the question of whether the little-studied phytocannabinoid, cannabigerol, can activate or block any G protein-coupled receptor. (nih.gov)
  • The [(35)S]GTPgammaS binding assay, performed with mouse brain membranes, was used to test the ability of cannabigerol to produce G protein-coupled receptor activation or blockade. (nih.gov)
  • 2000. Crystal structure of rhodopsin: A G protein-coupled receptor. (springer.com)
  • Our current main focus is the exploration of the mechanisms responsible for transmembrane signal instigation in cytokine receptors and G protein coupled receptor (GPCR) complexes. (stanford.edu)
  • Not much is known, however, about the effects and mechanism of action of synthetic nonpsychotic cannabinoids on breast cancer growth and metastasis. (aacrjournals.org)
  • Although these studies point to the potential application of cannabinoids as antitumor agents in various human cancer cells, not much is known about the molecular mechanism of cannabinoid-mediated antimetastatic and tumurogenic effects. (aacrjournals.org)
  • The influence of a cannabinoid receptor agonist, WIN 55,212-2, on C-fiber activation in guinea pig airways was investigated, as was the mechanism by which cannabinoids regulate antigen-induced airway inflammation. (unboundmedicine.com)
  • This study is to investigate a potential role and mechanism of JWH133, a selected cannabinoid receptor type2 (CB2R) agonist, on protecting blood-brain barrier integrity after ICH. (thctotalhealthcare.com)
  • Gastric acid secretion is also inhibited in response to CB 1 receptor activation, although the detailed underlying mechanism has yet to be elucidated. (bmj.com)
  • They can be divided into "specific" agents, e.g., affecting an identifiable molecular mechanism unique to target cells bearing receptors for that agent, and "nonspecific" agents, those producing effects on different target cells and acting by diverse molecular mechanisms. (nih.gov)
  • This mechanism allows for the local release of β-endorphin, where CB 2 receptors are present, leading to anatomical specificity of opioid effects. (pnas.org)
  • another plant-derived cannabinoid that also induces glioma cell death through a mechanism of action different from that of THC) remarkably reduces the growth of glioma xenografts. (aacrjournals.org)
  • In this study, we examined whether opioids and cannabinoids can affect C-fiber-induced ERK phosphorylation (pERK) in dorsal horn neurons in spinal cord slices from normal and spinal nerve-ligated rats. (aspetjournals.org)
  • The lack of effect of CB-receptor ligands in vitro cannot be ascribed to the use of immature rats, since HU-210 inhibited stimulated acid secretion in vivo, irrespective of the animal age. (springer.com)
  • Izzo AA, Mascolo N, Pinto L, Capasso R, Capasso F: The role of cannabinoid receptors in intestinal motility, defaecation and diarrhoea in rats. (springer.com)
  • CB 1 agonists lower blood pressure much more in SHR than in normotensive Wistar-Kyoto rats, and the expression of CB 1 is increased in heart and aortic endothelium of SHR compared with Wistar-Kyoto rats. (ahajournals.org)
  • Using ex vivo autoradiography, Imidazole 24b resulted in dose-dependent increases in brain cannabinoid CB(1) receptor occupancy (RO) at 2h post-dosing in rats, indicating that approximately 50% receptor occupancy is sufficient for attenuation of receptor agonist-induced hypothermia. (scienceexchange.com)
  • Collectively these results show that prenatal exposure to the cannabinoid CB1 receptor agonist WIN increases expression and functional activity of GLT1 and EAAC1 glutamate transporters (GluTs) associated to a decrease of cortical glutamate outflow, in adolescent rats. (unifg.it)
  • Three experiments examined the influence of pre-exposure to the cannabinoid receptor agonist CP 55,940 ((-)-cis-3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-trans-4-(3- hydroxypropyl)cyclohexanol) on the sensitization of morphine-induced locomotor hyperactivity and self-administration in Lewis rats. (edu.au)
  • Overall, these results suggest that cannabinoid pre-exposure can lead to an exaggeration of morphine-induced hyperactivity and may alter the reinforcing effects of morphine in Lewis rats. (edu.au)
  • A cannabinoid receptor 2 agonist reduces blood-brain barrier damage via induction of MKP-1 after intracerebral hemorrhage in rats. (thctotalhealthcare.com)
  • Leelamine hydrochloride suppresses transcriptional activity of androgen receptor , which is known to regulate fatty acid synthesis [2,3] . (medchemexpress.com)
  • CB 2 agonists produce analgesia in both inflammatory and neuropathic pain models. (elsevier.com)
  • Cannabinoid pretreatment induces tolerance to the inhibitory effects of cannabinoid receptor agonists on gastrointestinal motility. (bmj.com)
  • Similarly, the activation of the lipase by exogenous ligands of cannabinoid receptors, particularly CB1, induces antinociception in various acute pain tests in rodents [ 2 , 4 , 5 ], but also in several animal models of chronic pain [ 6 ]. (mdpi.com)
  • Org 27569 is an allosteric modulator of cannabinoid CB1 receptor , induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity. (selleckchem.com)
  • Therapeutic aspects of cannabis and cannabinoids. (springer.com)
  • Guy G, Whittle BA, Robson PJ: Medicinal Uses of Cannabis and Cannabinoids. (aerzteblatt.de)
  • After an initial burst of scientific activity in the 1970s, today's renewed interest has been fueled by major scientific discoveries discussed in previous chapters: the identification and cloning of endogenous cannabinoid receptors, the discovery of endogenous substances that bind to these receptors, and the emergence of synthetic cannabinoids that also bind to cannabinoid receptors. (nap.edu)
  • A pilot study designed to reveal the effects of Marinol / dronabinol, a CB 1 agonist. (clinicaltrials.gov)
  • In addition, the proposal seeks to assess whether the cannabinoid agonist dronabinol, when given to patients with SCZ and CUD, will also ameliorate this BRC deficit, and, thus, whether dronabinol could be considered as a potential adjunctive treatment (given with an antipsychotic medication) to decrease their cannabis use. (clinicaltrials.gov)
  • dronabinol (tetrahydrocannabinol, or THC, in sesame oil), the only approved cannabinoid in the United States. (nap.edu)
  • Currently, there are numerous cannabinoid based synthetic drugs used in clinical practice like the popular ones such as nabilone, dronabinol, and Δ 9 -tetrahydrocannabinol mediates its action through CB 1 /CB 2 receptors. (hindawi.com)
  • Δ 9 -Tetrahydrocannabinol (THC), the major active ingredient of marijuana, and other cannabinoid receptor agonists inhibit tumor growth in animal models of cancer, including glioma, an effect that relies, at least in part, on the stimulation of autophagy-mediated apoptosis in tumor cells. (aacrjournals.org)
  • Thus, CB₂ agonists may be therapeutically applied in clinical conditions, such as bone marrow transplantation. (420magazine.com)
  • Efficient synthetic approaches for therapeutically interesting cannabinoid analogues have been developed to further facilitate the drug discovery process. (springer.com)
  • Altogether, our findings support that the combined administration of TMZ and cannabinoids could be therapeutically exploited for the management of GBM. (aacrjournals.org)
  • Nevertheless, this changed in the late 1980s when specific cannabinoid receptors were discovered. (news-medical.net)
  • The cannabinoid receptor in brain (CB1) specifically binds delta 9-tetrahydrocannabinol, the predominant central nervous system-active component of marijuana. (aspetjournals.org)
  • Mechoulam R: Cannabinoids as Therapeutics. (aerzteblatt.de)
  • The present review provides an overview of therapeutic potential of ligands and plants modulating cannabinoid receptors that may be of interest to pharmaceutical industry in search of new and safer drug discovery and development for future therapeutics. (hindawi.com)
  • It is not clear whether spinal neurons have different sensitivity to cannabinoids and opioids after nerve injury. (aspetjournals.org)
  • Cannabinoids play a role in setting the threshold of excitability of neurons through the presynaptic CB1 receptor. (sid.ir)
  • Calcium channels, both in the cell membrane and inside the cytoplasm of neurons, are affected by cannabinoid receptors. (sid.ir)
  • When modified using a process known as epoxidation, two naturally occurring lipids are converted into potent agents that target multiple cannabinoid receptors in neurons, interrupting pathways that promote pain and inflammation, researchers report. (news-medical.net)
  • Therefore, a common property of CB1 and CB2 receptors is the ability to modulate the continuous release of diverse chemical messengers - CB1 receptors from neurons and CB2 receptors from immune cells. (news-medical.net)
  • THC, like other cannabinoids that contain a phenol group, possess mild antioxidant activity, sufficient to protect neurons against oxidative stress, such as that produced by glutamate-induced excitotoxicity [ 8 ]. (mdpi.com)
  • Here, we test the hypothesis that CB 2 receptor activation stimulates release from keratinocytes of the endogenous opioid β-endorphin, which then acts at opioid receptors on primary afferent neurons to inhibit nociception. (pnas.org)
  • CB 2 cannabinoid receptors have not been found in the CNS or on peripheral neurons, suggesting that activation of CB 2 receptors produces antinociception indirectly, by causing the release from nonneuronal cells of mediators that alter the responsiveness of primary afferent neurons to noxious stimuli. (pnas.org)
  • Therefore, we tested the hypothesis that activation of keratinocyte CB 2 receptors results in the release of the endogenous opioid peptide β-endorphin, which then acts on primary afferent neurons to inhibit nociception. (pnas.org)
  • In this article we review the evidence for the bronchodilator effects of the cannabinoid CB1 receptor tetrahydrocannabinol (THC) and suggest that the mechanisms of action for these effects are sufficiently independent of the mechanisms of standard bronchodilators to warrant clinical investigation. (eurekaselect.com)
  • Thus the human receptors are named after the psychoactive principles in marijuana. (erowid.org)
  • Since the isolation and identification of the major psychoactive component Δ 9 -THC in Cannabis sativa in the 1960s, numerous analogues of the classical plant cannabinoids have been synthesized and tested for their biological activity. (springer.com)
  • Synthetic cannabinoids are functionally similar to delta9-tetrahydrocannabinol (THC), the psychoactive principle of cannabis, and bind to the same cannabinoid receptors in the brain and peripheral organs. (frontiersin.org)
  • Synthetic cannabinoid receptor agonists (commonly referred to as 'synthetic cannabinoids') are a group of substances that mimic the effects of (-)- trans -Δ9-tetrahydrocannabinol (THC), which is the substance that is primarily responsible for the major psychoactive effects of cannabis. (europa.eu)
  • Synthetic cannabinoids (SC), cannabinoid 1 and cannabinoid 2 receptors agonists, are the psychoactive substances. (hindawi.com)
  • Due to the relatively high expression of the CB2 isotype on peripheral immune cells, it has been hypothesized that this receptor mediates the immunosuppressive effects of cannabinoids. (aspetjournals.org)
  • CB1 is expressed primarily in the central nervous system and mediates many, if not all of the psychotropic and analgesic effects classically associated with cannabinoid agonists. (aspetjournals.org)
  • Previously we identified a series of amidoalkylindoles as potent and selective CB 2 partial agonists. (rsc.org)
  • Benzimidazole 43 (EC 50,CB 1 = NA, EC 50,CB 2 = 0.067 μM) and azaindole 24 (EC 50,CB 1 = NA, EC 50,CB 2 = 0.048 μM) were found to be potent and selective CB 2 receptor partial agonists, both with improved aqueous solubility. (rsc.org)
  • WIN 54,461 (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2. (wikipedia.org)
  • Cannabinoid receptor type 1 ( CB 1 ), also known as cannabinoid receptor 1 , is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene . (wikipedia.org)
  • Humans have endogenous (naturally occuring) cannabinoid receptors throughout our bodies and brains, which were discovered after those in the plant. (erowid.org)
  • The implications for 'gateway' theories of cannabinoid effects in humans are discussed. (edu.au)
  • The enteric nervous system of several species, including the mouse, rat, guinea pig and humans, contains cannabinoid CB 1 receptors that depress gastrointestinal motility, mainly by inhibiting ongoing contractile transmitter release. (bmj.com)
  • Cannabinoid receptor agonists delay gastric emptying in humans as well as in rodents and probably also inhibit human gastric acid secretion. (bmj.com)
  • It also accounts for the ability of these agonists to induce analgesia in humans. (news-medical.net)
  • In vivo, the CB₂ agonist AM1241 induced mobilization of murine HSPCs with short- and long-term repopulating abilities. (420magazine.com)
  • In vitro and in vivo data indicate that CB 1 receptors are not located on parietal cells but, rather, on vagal pathways (possibly at preganglionic sites) supplying the gastric mucosa. (springer.com)
  • In the present study, we tested the possible effect of a CB1 cannabinoid receptor agonist on L-DOPA-stimulated abnormal behavioral and signaling responses in vivo. (scienceopen.com)
  • These sections serve as a road map to determine whether the therapeutic potential of cannabinoids is likely to be exploited commercially to meet patient needs. (nap.edu)
  • 2007. Cannabinoid-1 receptor blockade in cardiometabolic risk reduction: Safety, tolerability, and therapeutic potential. (springer.com)
  • 7 SR141716A alone produced a significant increase in ACh release in both the absence and presence of exogenous cannabinoid drugs, hence we conclude that it has a presynaptic site of action. (elsevier.com)
  • We also conclude that SR141716A acts either by antagonizing the effect of an endogenous CB1 receptor agonist or by having an inverse agonist effect at these receptors. (elsevier.com)
  • SR141716A has been reported not to behave in this manner in the myenteric plexus-longitudinal muscle preparation (MPLM) of human ileum unless this has first been rendered cannabinoid tolerant. (bmj.com)
  • and measuring the activity of the constitutively active CB receptor following contact with the inhibitory agent, wherein a decrease in the activity in the constitutively active CB receptor, compared to the activity of the constitutively active CB receptor in the absence of the inhibitory agent, indicates that the agent is an inverse agonist. (freepatentsonline.com)
  • The inhibitory effects of cannabinoid receptor agonists on gastric emptying and intestinal transit are mediated to some extent by CB 1 receptors in the brain as well as by enteric CB 1 receptors. (bmj.com)
  • Its ability to displace [(3)H]CP55940 from mouse CB(1) and human CB(2) cannabinoid receptors and to inhibit electrically evoked contractions of the mouse isolated vas deferens was also investigated. (nih.gov)
  • A molecular docking approach that combined Monte Carlo and molecular dynamics simulations was used to identify the putative binding conformations of nonclassical cannabinoid agonists, including AC-bicyclic CP47497 and CP55940, and ACD-tricyclic CP55244. (nih.gov)
  • These are the classical cannabinoids (THC and HU-210), as well as the non-classical cannabinoid (CP55940) and certain aminoalkylindoles. (news-medical.net)
  • During April 2-May 3, 2015, MPCC received reports of 721 suspected cases, including nine deaths associated with synthetic cannabinoid use. (cdc.gov)
  • Acute kidney injury associated with synthetic cannabinoid use--multiple states, 2012. (soft-tox.org)
  • We are also investigating whether endogenous cannabinoids can exert antitumor activity. (420magazine.com)
  • Additionally, cannabigerol inhibited evoked contractions of the vas deferens in a manner that appeared to be alpha(2)-adrenoceptor-mediated (EC(50)= 72.8 nM) and displayed significant affinity for mouse CB(1) and human CB(2) receptors. (nih.gov)
  • The in vitro binding affinity of Imidazole 24b for recombinant human and rat CB(1) receptor is 4 and 10 nM, respectively. (scienceexchange.com)
  • Lasofoxifene is a non-steroidal 3rd generation selective estrogen receptor modulator (SERM) that selectively binds to both ERα and ERβ with high affinity. (drugbank.ca)
  • 4-Hydroxytamoxifen (4-HT) is the active metabolite of tamoxifen which binds estrogen receptors (ER) and estrogen-related receptors (ERR) with estrogenic and anti-estrogenic effects. (sigmaaldrich.com)
  • This investigation has provided the first evidence that cannabigerol can activate alpha(2)-adrenoceptors, bind to cannabinoid CB(1) and CB(2) receptors and block CB(1) and 5-HT(1A) receptors. (nih.gov)
  • One of the most active areas of research in the cannabinoid field is the study of the potential application of cannabinoids in the treatment of different pathologies ( 9, 10 ). (aacrjournals.org)
  • These data provide evidence for the active involvement of CB1 cannabinoid receptors in the regulation of L-DOPA action during PD therapy. (scienceopen.com)
  • 4 - 6 Moreover, the American Medical Association reviewed the evidence in 2009 and recommended rescheduling cannabinoid-based medicines to allow their legal prescription in the United States. (mja.com.au)
  • Furthermore, we have shown that the CB2 synthetic agonist JWH-133 and the CB1 and CB2 agonist WIN-55,212-2 inhibit cell proliferation and migration under in vitro conditions. (aacrjournals.org)
  • Cannabinoids have been reported to possess antitumorogenic activity. (aacrjournals.org)
  • To test whether there is specificity among cannabinoid receptor agonists in activating G s - or G i -coupled pathways, the potency and intrinsic activity of various cannabinoid receptor ligands in stimulating or inhibiting cAMP accumulation were quantified. (aspetjournals.org)
  • Cannabinoid receptor binding and agonist activity of amides and esters of arachidonic acid. (aspetjournals.org)
  • Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor. (aalto.fi)
  • These drugs are used to suppress cannabinoid receptor activity (for example, rimonabant). (medicinenet.com)
  • Cannabinoids are a class of chemicals, with structure or activity similar to those found naturally in the cannabis plant. (erowid.org)
  • Thus, an opposing activity of μ- and κ-opioid receptors in modulating reward pathways forms the basis for the dual euphoric-dysphoric activity of THC. (jneurosci.org)
  • Removal of the serotonin afferents, or dampening of serotonin neuron activity by 5-HT1A and 5-HT1B agonist drugs, resulted in a near-complete block of the L-DOPA-induced dyskinesias, suggesting that dysregulated dopamine release from serotonin terminals is the prime trigger of dyskinesia in the rat Parkinson's disease model. (scienceopen.com)
  • GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. (selleckchem.com)
  • A study also suggests that lasofoxifene may also act as an inverse agonist at CB2 cannabinoid receptor which is expressed in bone to inhibit osteoclast formation and resorptive activity. (drugbank.ca)
  • Despite the lack of crystal structures for CB1, protein-based homology modeling approaches and molecular docking methods can be used in the design and discovery of cannabinoid analogues. (springer.com)
  • This led to the discovery of Org 28611, a potent, water soluble CB1 receptor agonist , which was selected for clinical evaluation as a potential intravenous analgesic agent. (rsc.org)
  • Molecular mechanisms underlying analgesic effects of opioids and cannabinoids are not fully understood. (aspetjournals.org)
  • O-3223 mediated stimulation of [ 35 S]GTPγS binding in membranes from HEK cells stably expressing the human CB 1 or CB 2 receptor. (nih.gov)
  • In conclusion, the present study lends support to the idea that stimulation of CB2 receptors ameliorates several altered parameters in Alzheimer's disease such as impaired memory and learning, neuroinflammation, oxidative stress damage and oxidative stress responses, selected tau kinases, and tau hyperphosphorylation around plaques. (scicombinator.com)
  • Adrenergic agonists that release tissue stores of epinephrine, causing subsequent alpha- and/or beta-adrenergic stimulation, have provided benefits to patients with obesity. (medscape.com)

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