Receptors, Cannabinoid: A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES.Cannabinoid Receptor Antagonists: Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Receptor, Cannabinoid, CB2: A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Pyrazoles: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.Cannabinoid Receptor Modulators: Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS.Piperidines: A family of hexahydropyridines.Energy Intake: Total number of calories taken in daily whether ingested or by parenteral routes.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Endocannabinoids: 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.Cerumen: The yellow or brown waxy secretions produced by vestigial apocrine sweat glands in the external ear canal.Health Services: Services for the diagnosis and treatment of disease and the maintenance of health.BooksFatty Liver: Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.Choline Deficiency: A condition produced by a deficiency of CHOLINE in animals. Choline is known as a lipotropic agent because it has been shown to promote the transport of excess fat from the liver under certain conditions in laboratory animals. Combined deficiency of choline (included in the B vitamin complex) and all other methyl group donors causes liver cirrhosis in some animals. Unlike compounds normally considered as vitamins, choline does not serve as a cofactor in enzymatic reactions. (From Saunders Dictionary & Encyclopedia of Laboratory Medicine and Technology, 1984)Keratin-18: A type I keratin found associated with KERATIN-8 in simple, or predominately single layered, internal epithelia.Hepatitis: INFLAMMATION of the LIVER.Liver: A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.Internet: A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.Liver Cirrhosis: Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.Conducted Energy Weapon Injuries: The injuries caused by conducted energy weapons such as stun guns, shock batons, and cattle prods.Computer Storage Devices: Devices capable of receiving data, retaining data for an indefinite or finite period of time, and supplying data upon demand.Security Measures: Regulations to assure protection of property and equipment.Optical Storage Devices: A computer disk read by a laser beam, containing data prerecorded by a vendor. The buyer cannot enter or modify data in any way but the advantages lie in the speed of accessibility, relative immunity to damage, and relatively low cost of purchase.Wireless Technology: Techniques using energy such as radio frequency, infrared light, laser light, visible light, or acoustic energy to transfer information without the use of wires, over both short and long distances.Computer Communication Networks: A system containing any combination of computers, computer terminals, printers, audio or visual display devices, or telephones interconnected by telecommunications equipment or cables: used to transmit or receive information. (Random House Unabridged Dictionary, 2d ed)Local Area Networks: Communications networks connecting various hardware devices together within or between buildings by means of a continuous cable or voice data telephone system.Intra-Abdominal Fat: Fatty tissue inside the ABDOMINAL CAVITY, including visceral fat and retroperitoneal fat. It is the most metabolically active fat in the body and easily accessible for LIPOLYSIS. Increased visceral fat is associated with metabolic complications of OBESITY.Diet, Fat-Restricted: A diet that contains limited amounts of fat with less than 30% of calories from all fats and less than 10% from saturated fat. Such a diet is used in control of HYPERLIPIDEMIAS. (From Bondy et al, Metabolic Control and Disease, 8th ed, pp468-70; Dorland, 27th ed)Dietary Fats: Fats present in food, especially in animal products such as meat, meat products, butter, ghee. They are present in lower amounts in nuts, seeds, and avocados.Tomography, X-Ray Computed: Tomography using x-ray transmission and a computer algorithm to reconstruct the image.Physician-Patient Relations: The interactions between physician and patient.Research Personnel: Those individuals engaged in research.Bees: Insect members of the superfamily Apoidea, found almost everywhere, particularly on flowers. About 3500 species occur in North America. They differ from most WASPS in that their young are fed honey and pollen rather than animal food.Honey: A sweet viscous liquid food, produced in the honey sacs of various bees from nectar collected from flowers. The nectar is ripened into honey by inversion of its sucrose sugar into fructose and glucose. It is somewhat acidic and has mild antiseptic properties, being sometimes used in the treatment of burns and lacerations.IcelandGenome, Insect: The genetic complement of an insect (INSECTS) as represented in its DNA.Social Behavior: Any behavior caused by or affecting another individual, usually of the same species.Models, Biological: Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.Neurobiology: The study of the structure, growth, activities, and functions of NEURONS and the NERVOUS SYSTEM.Calcium Carbonate: Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Carbonates: Salts or ions of the theoretical carbonic acid, containing the radical CO2(3-). Carbonates are readily decomposed by acids. The carbonates of the alkali metals are water-soluble; all others are insoluble. (From Grant & Hackh's Chemical Dictionary, 5th ed)Hyperlipidemia, Familial Combined: A type of familial lipid metabolism disorder characterized by a variable pattern of elevated plasma CHOLESTEROL and/or TRIGLYCERIDES. Multiple genes on different chromosomes may be involved, such as the major late transcription factor (UPSTREAM STIMULATORY FACTORS) on CHROMOSOME 1.Foramen Ovale, Patent: A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.Chemistry, Pharmaceutical: Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.Search Engine: Software used to locate data or information stored in machine-readable form locally or at a distance such as an INTERNET site.Glucagon-Like Peptide 1: A peptide of 36 or 37 amino acids that is derived from PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. GLP-1(1-37 or 1-36) is further N-terminally truncated resulting in GLP-1(7-37) or GLP-1-(7-36) which can be amidated. These GLP-1 peptides are known to enhance glucose-dependent INSULIN release, suppress GLUCAGON release and gastric emptying, lower BLOOD GLUCOSE, and reduce food intake.Whistleblowing: The reporting of observed or suspected PROFESSIONAL MISCONDUCT or incompetence to appropriate authorities or to the public.Public Health: Branch of medicine concerned with the prevention and control of disease and disability, and the promotion of physical and mental health of the population on the international, national, state, or municipal level.Receptors, Glucagon: Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.Glucagon-Like Peptides: Peptides derived from proglucagon which is also the precursor of pancreatic GLUCAGON. Despite expression of proglucagon in multiple tissues, the major production site of glucagon-like peptides (GLPs) is the INTESTINAL L CELLS. GLPs include glucagon-like peptide 1, glucagon-like peptide 2, and the various truncated forms.Glucagon-Like Peptide 2: A 33-amino acid peptide derived from the C-terminal of PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. It stimulates intestinal mucosal growth and decreased apoptosis of ENTEROCYTES. GLP-2 enhances gastrointestinal function and plays an important role in nutrient homeostasis.Gastrointestinal Agents: Drugs used for their effects on the gastrointestinal system, as to control gastric acidity, regulate gastrointestinal motility and water flow, and improve digestion.
CB(1) cannabinoid receptor antagonism promotes remodeling and cannabinoid treatment prevents endothelial dysfunction and hypotension in rats with myocardial infarction. (1/155)1. To study the long-term effects of altered cannabinoid receptor activity on myocardial and vascular function, Wistar rats were treated with the selective CB(1) antagonist AM-251 (0.5 mg kg(-1) d(-1)), the potent synthetic cannabinoid HU-210 (50 micro g kg(-1) d(-1)) or vehicle for 12 weeks after coronary artery ligation or sham operation. 2. AM-251 further reduced the pressure-generating capacity, shifted the pressure volume curve to the right (P<0.05) and increased the left-ventricular operating volume (AM-251: 930+/-40 micro l vs control: 820+/-40 micro l vs HU-210: 790+/-50 micro l; P<0.05) in rats with large myocardial infarction (MI). 3. Left-ventricular CB(1) immunoactivity in rats 12 weeks after large MI was unaltered as compared with noninfarcted hearts. 4. Cannabinoid receptor activation through HU-210, a cannabinoid that alters cardiovascular parameters via CB(1) receptors, increased the left-ventricular end-diastolic pressure (LVEDP, P<0.05). However, it prevented the drop in left-ventricular systolic pressure (HU-210: 142+/-5 mm Hg; P<0.05 vs control: 124+/-3 mm Hg; and P<0.001 vs AM-251: 114+/-3 mm Hg) and prevented endothelial dysfunction (ED) in aortic rings of rats with large MI (P<0.05). 5. Compared with AM-251, HU-210 prevented the decline in the maximal rate of rise of left-ventricular pressure and the maximum pressure-generating ability (P<0.05). In rats with small MI, HU-210 increased cardiac index (P<0.01) and lowered the total peripheral resistance (P<0.05). 6. The study shows that during the development of congestive heart failure post-large MI, cannabinoid treatment increases LVEDP and prevents hypotension and ED. Presumed CB(1) antagonism promotes remodeling despite unchanged myocardial CB(1) expression. (+info)
Vasodilator actions of abnormal-cannabidiol in rat isolated small mesenteric artery. (2/155)1. The nonpsychoactive cannabinoid abnormal-cannabidiol (trans-4-[3-methyl-6-(1-methylethenyl)-2-cyclohexen-1-yl]-5-pentyl-1,3-benzenedio l) (abn-cbd) produced concentration-dependent relaxation of methoxamine-precontracted rat small mesenteric artery. Endothelial removal reduced abn-cbd potency six-fold without affecting the maximum relaxation. 2. In endothelium-intact vessels, abn-cbd was less potent under 60 mM KCl-induced tone and inhibited by combination of L-N(G)-nitroarginine methyl ester (L-NAME) (nitric oxide synthase inhibitor; 300 micro M), apamin (small conductance Ca(2+)-activated K(+) channels inhibitor; 50 nM) and charybdotoxin (inhibitor of intermediate conductance Ca(2+)-activated K(+) channels and large conductance Ca(2+)-activated K(+) channels BK(Ca); 50 nM). L-NAME alone or in combination with either toxin alone had little effect. 3. In intact vessels, relaxations to abn-cbd were inhibited by SR 141716A (cannabinoid receptor antagonist; 1 or 3 micro M). Concomitant addition of L-NAME, apamin and charybdotoxin had no further effect. Other cannabinoid receptor antagonists either had little (SR 144528; 1 micro M and AM 251; 1 micro M) or no effect (AM 630; 10 micro M and AM 281; 1 micro M). Inhibition of gap junctions, G(i/o) protein coupling and protein kinase A also had no effect. 4. Endothelium-independent relaxation to abn-cbd was unaffected by L-NAME, apamin plus charybdotoxin or capsaicin (10 micro M). Abn-cbd inhibited CaCl(2)-induced contractions in vessels with depleted intracellular Ca(2+) stores and stimulated with methoxamine or KCl. This was insensitive to SR 141716A (3 micro M) but greatly reduced in vessels stimulated with ionomycin (Ca(2+) ionophore; 1 micro M). 5. We conclude that abn-cbd relaxes the rat small mesenteric artery by endothelium-dependent activation of K(+) channels via SR 141716A-sensitive pathways, which do not involve CB(1) and CB(2) receptors. It also causes endothelium-independent, SR 141716A-insensitive, relaxation by inhibiting Ca(2+) entry through voltage-gated Ca(2+) channels. (+info)
Cannabinoid receptor-mediated regulation of intracellular calcium by delta(9)-tetrahydrocannabinol in resting T cells. (3/155)Cannabinoids exhibit broad immune modulating activity by targeting many cell types within the immune system, including T cells, which exhibit sensitivity, as evidenced by altered activation, proliferation, and cytokine expression. As a result of the critical role calcium plays in T cell function coupled with previous findings demonstrating disruption of the calcium-regulated transcription factor, nuclear factor of activated T cells, by cannabinoid treatment, the objective of the present investigation was to perform an initial characterization of the role of the cannabinoid receptors in the regulation of the intracellular calcium concentration ([Ca(2+)](i)) by delta(9)-tetrahydrocannabinol (delta(9)-THC) in T lymphocytes. Here, we demonstrate that delta(9)-THC robustly elevates [Ca(2+)](i) in purified murine splenic T cells and in the human peripheral blood acute lymphoid leukemia (HPB-ALL) human T cell line but only minimally elevates [Ca(2+)](i) in Jurkat E6-1 (dysfunctional cannabinoid receptor 2-expressing) human T cells. Removal of extracellular calcium severely attenuated the delta(9)-THC-mediated rise in [Ca(2+)](i) in murine splenic T cells and HPB-ALL cells. Pretreatment with cannabinoid receptor antagonists, SR144528 and/or SR141716A, led to an attenuation of delta(9)-THC-mediated elevation in [Ca(2+)](i) in splenic T cells and HPB-ALL cells but not in Jurkat E6-1 cells. Furthermore, pretreatment of HPB-ALL cells with SR144528 antagonized the small rise in [Ca(2+)](i) elicited by delta(9)-THC in the absence of extracellular calcium. These findings suggest that delta(9)-THC induces an influx of extracellular calcium in resting T cells in a cannabinoid receptor-dependent manner. (+info)
Endocannabinoid system modulates relapse to methamphetamine seeking: possible mediation by the arachidonic acid cascade. (4/155)We clarified the modulating action of the endocannabinoid system, and its possible mediation by the arachidonic acid cascade, on the reinstatement of methamphetamine (METH)-seeking behavior, using the intravenous self-administration paradigm in rats. Following 12 days of self-administration of METH, the replacement of METH with saline resulted in a gradual decrease in lever press responses (extinction). Under extinction conditions, METH-priming or re-exposure to cues previously paired with METH infusion markedly increased the responses (reinstatement of drug-seeking). The cannabinoid CB1 receptor antagonist, SR141716A, blocked this behavior. Although the cannabinoid agonist, Delta8-tetrahydrocannabinol (THC), had no effects by itself, coadministration of the agonist and METH at small doses reinstated the drug-seeking behavior. THC attenuated the effects of the reinstatement-inducing dose of METH, but enhanced the effect of cues. Either given repeatedly during the extinction or singly, 24 h before the first METH-priming or cues challenge, THC suppressed the reinstatement. In another set of experiments, we found that diclofenac, a cyclooxygenase inhibitor, also attenuated the reinstatement induced by exposure to cues or drug-priming. These results suggest that the endocannabinoid system, through possible mediation by the arachidonic acid cascade, serves as a modulator of the reinstating effects of METH-priming and cues. Extending the current view on the treatment of drug dependence, these results indicate that endocannabinoid-activating substances as well as cyclooxygenase inhibitors may be promising as antirelapse agents. (+info)
Central effects of the cannabinoid receptor agonist WIN55212-2 on respiratory and cardiovascular regulation in anaesthetised rats. (5/155)1 The primary aim was to study the central respiratory effects of cannabinoids (CB). To this end, the cannabinoid receptor agonist WIN55212-2 was injected into the cisterna magna of urethane-anaesthetised rats and changes in respiratory parameters were observed. The secondary aim was to observe the centrally elicited cardiovascular actions of WIN55212-2. Involvement of opioid mechanisms in the central effects of WIN55212-2 was also studied. 2 Intracisternal (i.c.) application of WIN55212-2 (1, 3, 10 and 30 microg kg(-1)) dose-dependently decreased the respiratory rate and minute volume. Tidal volume was slightly increased, whereas peak inspiratory flow remained unchanged. In addition, WIN55212-2 increased mean arterial pressure and the plasma noradrenaline concentration and decreased heart rate. 3 I.c. injection of WIN55212-3 (1, 3, 10 and 30 microg kg(-1)), an enantiomer of WIN55212-2 lacking affinity for cannabinoid receptors, elicited no effects. All effects of WIN55212-2 were prevented by the CB1 receptor antagonist SR141716 (2 mg kg(-1) i.v.). I.c. administration of the opioid receptor agonist DAMGO (0.1, 0.3, 1 and 3 microg kg(-1)) markedly lowered the respiratory rate, tidal volume, minute volume and peak inspiratory flow. These effects were attenuated by the opioid receptor antagonist naloxone (0.2 mg kg(-1) i.v.). In contrast, naloxone did not affect the respiratory and cardiovascular effects of i.c. administered WIN55212-2. 4 Our results show that activation of CB1 cannabinoid receptors in the brain stem depresses respiration and enhances sympathetic tone and cardiac vagal tone. Opioid mechanisms are not involved in these central cannabinoid effects. (+info)
The cannabinomimetic arachidonyl-2-chloroethylamide (ACEA) acts on capsaicin-sensitive TRPV1 receptors but not cannabinoid receptors in rat joints. (6/155)The vasoactive effects of the synthetic cannabinoid (CB) arachidonyl-2-chloroethylamide (ACEA) was tested in the knee joints of urethane-anaesthetised rats. Experiments were also performed to determine whether these vasomotor responses could be blocked by the selective CB(1) receptor antagonists AM251 (N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole- 3-carboxamide) (10(-9) mol) and AM281 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-c arboxamide) (10(-8) mol), as well as the selective CB(2) receptor antagonist AM630 (6-iodo-2-methyl-1-[2-4(morpholinyl)ethyl]-[1H-indol-3-yl](4-methoxyphenyl)methan one) (10(-8) mol). Peripheral application of ACEA (10(-14)-10(-9) mol) onto the exposed surface of the knee joint capsule caused a dose-dependent increase in synovial blood flow. The dilator action of the CB occurred within 1 min after drug administration and rapidly returned to control levels shortly thereafter. The maximal vasodilator effect of ACEA corresponded to a 30% increase in articular perfusion compared to control levels. The hyperaemic action of ACEA was not significantly altered by coadministration of AM251, AM281 or AM630 (P>0.05; two-way ANOVA). The transient receptor potential channel vanilloid receptor 1 (TRPV(1)) antagonist capsazepine (10(-6) mol) significantly reduced the vasodilator effect of ACEA on joint blood vessels (P=0.002). Furthermore, destruction of unmyelinated and thinly myelinated joint sensory nerves by capsaicin (8-methyl-N-vanillyl-6-nonenamide) treatment also attenuated ACEA responses (P<0.0005). These data clearly demonstrate a vasodilator effect of the cannabinomimetic ACEA on knee joint perfusion. Rather than a classic CB receptor pathway, ACEA exerts its vasomotor influence by acting via TRPV(1) receptors located on the terminal branches of capsaicin-sensitive afferent nerves innervating the joint. (+info)
Anandamide-induced cell death in primary neuronal cultures: role of calpain and caspase pathways. (7/155)Anandamide (arachidonoylethanolamide or AEA) is an endocannabinoid that acts at vanilloid (VR1) as well as at cannabinoid (CB1/CB2) and NMDA receptors. Here, we show that AEA, in a dose-dependent manner, causes cell death in cultured rat cortical neurons and cerebellar granule cells. Inhibition of CB1, CB2, VR1 or NMDA receptors by selective antagonists did not reduce AEA neurotoxicity. Anandamide-induced neuronal cell loss was associated with increased intracellular Ca(2+), nuclear condensation and fragmentation, decreases in mitochondrial membrane potential, translocation of cytochrome c, and upregulation of caspase-3-like activity. However, caspase-3, caspase-8 or caspase-9 inhibitors, or blockade of protein synthesis by cycloheximide did not alter anandamide-related cell death. Moreover, AEA caused cell death in caspase-3-deficient MCF-7 cell line and showed similar cytotoxic effects in caspase-9 dominant-negative, caspase-8 dominant-negative or mock-transfected SH-SY5Y neuroblastoma cells. Anandamide upregulated calpain activity in cortical neurons, as revealed by alpha-spectrin cleavage, which was attenuated by the calpain inhibitor calpastatin. Calpain inhibition significantly limited anandamide-induced neuronal loss and associated cytochrome c release. These data indicate that AEA neurotoxicity appears not to be mediated by CB1, CB2, VR1 or NMDA receptors and suggest that calpain activation, rather than intrinsic or extrinsic caspase pathways, may play a critical role in anandamide-induced cell death. (+info)
2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand, induces rapid actin polymerization in HL-60 cells differentiated into macrophage-like cells. (8/155)Delta9-Tetrahydrocannabinol, a major psychoactive constituent of marijuana, interacts with specific receptors, i.e. the cannabinoid receptors, thereby eliciting a variety of pharmacological responses. To date, two types of cannabinoid receptors have been identified: the CB1 receptor, which is abundantly expressed in the nervous system, and the CB2 receptor, which is predominantly expressed in the immune system. Previously, we investigated in detail the structure-activity relationship of various cannabinoid receptor ligands and found that 2-AG (2-arachidonoylglycerol) is the most efficacious agonist. We have proposed that 2-AG is the true natural ligand for both the CB1 and CB2 receptors. Despite the potential physiological importance of 2-AG, not much information is available concerning its biological activities towards mammalian tissues and cells. In the present study, we examined the effect of 2-AG on morphology as well as the actin filament system in differentiated HL-60 cells, which express the CB2 receptor. We found that 2-AG induces rapid morphological changes such as the extension of pseudopods. We also found that it provokes a rapid actin polymerization in these cells. Actin polymerization induced by 2-AG was abolished when cells were treated with SR144528, a CB2 receptor antagonist, and pertussis toxin, suggesting that the response was mediated by the CB2 receptor and G(i/o). A phosphoinositide 3-kinase, Rho family small G-proteins and a tyrosine kinase were also suggested to be involved. Reorganization of the actin filament system is known to be indispensable for a variety of cellular events; it is possible that 2-AG plays physiologically essential roles in various inflammatory cells and immune-competent cells by inducing a rapid actin rearrangement. (+info)
"Cannabinoid Receptor Agonists and Antagonists". Current Pharmaceutical Design. 1 (3): 343-352. ... WIN 54,461 (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2 ...
Cannabinoid receptor antagonist Kim, M.; et al. (2008), "Design, chemical synthesis, and biological evaluation of novel ... a cannabinoid-1 receptor inverse agonist" (PDF), Tetrahedron, 64 (48): 10802-10809, doi:10.1016/j.tet.2008.09.057 Woods SC. The ... Otenabant (CP-945,598) is a drug which acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the ...
It is a tricyclic aryl derivative that acts as a competitive antagonist at the CB2 cannabinoid receptor. Its activity at CB1 ... WIN 55,212-2 WIN 55,225 Howlett AC, Berglund B, Melvin LS (October 1995). "Cannabinoid Receptor Agonists and Antagonists". ...
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... "Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum". British Journal of Pharmacology. 128 ... "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of Pharmacology. ... This cannabinoid related article is a stub. You can help Wikipedia by expanding it.. *v ...
... it is additionally a μ-opioid receptor antagonist. Discovery and development of Cannabinoid Receptor 1 Antagonists Lan, R; Liu ... AM-251 is structurally very close to SR141716A (rimonabant); both are biarylpyrazole cannabinoid receptor antagonists. In AM- ... "AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies ... "Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists". J Med Chem. 42: 769-76. doi: ...
This article is about the metabotropic glutamate receptor antagonist. For the cannabinoid drug, see APICA (synthetic ... It is a selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), and has been useful in the study of ... Synthesis of (S)-alphaM4CPG, (S)-MPPG, (S)-AIDA, and (S)-APICA, the Antagonists of Metabotropic Glutamate Receptors. Journal of ... Synthesis and biological activity of cyclic analogues of MPPG and MCPG as metabotropic glutamate receptor antagonists. ...
Cahill, K; Ussher, MH (16 March 2011). "Cannabinoid type 1 receptor antagonists for smoking cessation". The Cochrane Database ... Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class. Rimonabant is ... Pi-Sunyer FX, Aronne LJ, Heshmati HM, Devin J, Rosenstock J (Feb 2006). "Effect of rimonabant, a cannabinoid-1 receptor blocker ... Fong TM, Heymsfield SB (September 2009). "Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action ...
... especially structure-activity relationship studies into novel CB1 antagonists. Cannabinoid receptor antagonist Lange, JH; ... cannabinoid receptor antagonists". Journal of Medicinal Chemistry. 47 (3): 627-43. doi:10.1021/jm031019q. PMID 14736243. Need, ... 4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity". Bioorganic & Medicinal Chemistry ... vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists ...
Cannabinoid receptor antagonist Lange JH, Kruse CG (2008). "Cannabinoid CB1 receptor antagonists in therapeutic and structural ... Lee HK, Choi EB, Pak CS (2009). "The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as ... Reggio, Patricia H. (2009). "Toward the design of cannabinoid CB1 receptor inverse agonists and neutral antagonists". Drug ... Drinabant (INN; AVE-1625) is a drug that acts as a selective CB1 receptor antagonist, which was under investigation varyingly ...
Cannabinoid receptor Synthetic cannabinoid Cannabinoid receptor antagonist George I. Papakostas; Maurizio Fava (2010). ... 323-. ISBN 978-981-4287-59-3. Bambico, Francis Rodriguez; Gobbi, Gabriella (2008). "The cannabinoid CB1 receptor and the ...
Cannabinoid receptor antagonist Janero DR, Makriyannis A (March 2009). "Cannabinoid receptor antagonists: pharmacological ... Lee HK, Choi EB, Pak CS (2009). "The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as ... Rosonabant (INN; E-6776) is a drug acting as a CB1 receptor antagonist/inverse agonist that was under investigation by Esteve ... Development of the drug for clinical use was apparently halted shortly after the related CB1 antagonist rimonabant was ...
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum. British Journal of Pharmacology. 1999 ... An investigation into the structural determinants of cannabinoid receptor ligand efficacy. British Journal of Pharmacology. ... Agonist-antagonist characterization of 6'-cyanohex-2'-yne-delta 8-tetrahydrocannabinol in two isolated tissue preparations. ...
Discovery and development of Cannabinoid Receptor 1 Antagonists NESS-040C5 Ruiu, S; Pinna, GA; Marchese, G; Mussinu, JM; Saba, ... a novel putative antagonist of the CB1 cannabinoid receptor". Journal of Pharmacology and Experimental Therapeutics. 306 (1): ... Synthesis and Biological Activity of Rigid Cannabinoid CB1 Receptor Antagonists". Chem. Pharm. Bull. 50 (8): 1109-1113. doi: ... It is much more potent an antagonist, and more selective for the CB1 receptor over CB2, than the more commonly used ligand ...
Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum. British Journal of Pharmacology. 1999 ... CP 55,244 is a compound which is a cannabinoid receptor agonist. It has analgesic effects and is used in scientific research. ...
Cannabinoid agonists and antagonists discriminated by receptor binding in rat cerebellum. British Journal of Pharmacology. 1999 ... It is a partial agonist at the cannabinoid receptor CB1, producing a maximal stimulation of 58.3% with a Ki of 8.45nM. Griffin ... An investigation into the structural determinants of cannabinoid receptor ligand efficacy. British Journal of Pharmacology. ... yne-delta8-tetrahydrocannabinol at cannabinoid receptors. British Journal of Pharmacology. 1999 Oct;128(3):735-43. PMID ...
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 ...
Cannabinoid receptor antagonist O-1269 Rinaldi-Carmona, M; Barth, F; Congy, C; Martinez, S; Oustric, D; Pério, A; Poncelet, M; ... Surinabant (SR147778) is a cannabinoid receptor type 1 antagonist developed by Sanofi-Aventis. It is being investigated as a ... Gessa, GL; Serra, S; Vacca, G; Carai, MA; Colombo, G (2005). "Suppressing effect of the cannabinoid CB1 receptor antagonist, ... Lallemand, F; De Witte, P (Jul 2006). "SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in ...
... is a drug that is a classical cannabinoid derivative, which acts as an antagonist for the CB1 receptor. This gives it an ... Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist. European Journal of ... Suppression of feeding, drinking, and locomotion by a putative cannabinoid receptor 'silent antagonist'. European Journal of ... Agonists and silent antagonists in a series of cannabinoid sulfonamides. 12th Annual Symposium on the Cannabinoids, 2002 Martin ...
Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N (2007). "NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked ... JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. This was the fourth opioid ... "Small-molecule agonists and antagonists of the opioid receptor-like receptor (ORL1, NOP): Ligand-based analysis of structural ... and cannabinoids. JTC-801 is an orally active drug that blocks the nociceptin receptor and produces analgesic effects in a ...
Investigational medications include cannabinoids and the 5-HT3 receptor antagonist tropisetron. Low quality evidence found an ... A systematic review found most cytokines levels were similar in patients and controls, except for IL-1 receptor antagonist, IL- ... Späth, M (May 2002). "Current experience with 5-HT3 receptor antagonists in fibromyalgia". Rheumatic diseases clinics of North ... Decreased binding of μ-opioid receptor have been observed; however, it is unknown if this is a result of increased endogenous ...
... or antagonist at the cannabinoid receptors. The propyl analog, THCV, is a cannabinoid receptor type 1 and cannabinoid receptor ... "Evidence that the plant cannabinoid Δ9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist". British ... Cannabis Cannabinoid Parahexyl Thomas, Adèle; Stevenson, Lesley A; Wease, Kerrie N; Price, Martin R; Baillie, Gemma; Ross, Ruth ... type 2 antagonist, while THC is a CB1 agonist. THC-C4 has rarely been isolated from cannabis samples, but appears to be less ...
Effects of the cannabinoid CB1 receptor antagonist rimonabant in models of emotional reactivity in rodents. Biological ... Activation of corticotropin-releasing factor receptors from the basolateral or central amygdala increases the tonic immobility ...
THCV is a cannabinoid receptor type 1 antagonist and cannabinoid receptor type 2 partial agonist. Δ8-THCV has also been shown ... Cannabinoids Rimonabant (synthetic CB1 antagonist) Tetrahydrocannabinol-C4 Cannabivarin Parahexyl Cannabis Medical cannabis SC ... Pertwee, Roger G (September 2007). "The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: Δ9- ... At lower doses, THCV may act as a CB1 antagonist. At higher doses, however, it can switch, behaving as a CB1 agonist, much like ...
"CB2 cannabinoid receptor antagonist SR144528 decreases μ-opioid receptor expression and activation in mouse brainstem: Role of ... an Antagonist for the Peripheral Cannabinoid Receptor that Behaves as an Inverse Agonist". Journal of Pharmacology and ... "Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB2 receptor". ... the First Potent and Selective Antagonist of the CB2 Cannabinoid Receptor". Journal of Pharmacology and Experimental ...
2010). "Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor ... antagonists/inverse. agonists/antibodies). *AM-251. *AM-281. *AM-630. *AM-1387 ... This cannabinoid related article is a stub. You can help Wikipedia by expanding it.. *v ... "3-Cycloalkylcarbonyl indoles as cannabinoid receptor ligands", published 2006-06-29, assigned to Abbott Laboratories ...
Kiefer F, Jahn H, Tarnasker T, Helwig H, Briken P, Holbach R, Kampf P, Stracke R, Baehr M, Naber D et al. (2003) Comparing and combining naltrexone and acamprosate in relapse prevention of alcoholism. A double-blind, placebo-controlled study. Arch Gen Psychiatry 60: 92-99PubMedCrossRefGoogle Scholar ...
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Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. Lifestyle, diabetes, and...
Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. Lifestyle, diabetes, and cardiovascular risk factors 10 years after bariatric surgery
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Not too long ago, a drug called rimonabant seemed to be just such a magic bullet. Rimonabant blocked the receptors in the body that are sensitive to cannabinoids like THC. There are two known varieties of cannabinoid receptors, by the way, CB1 and CB2, though they stand among other multi-purpose receptors that are sensitive to…
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Coconut Shrimp and Broccoli with Macadamia nuts Recipe. "What do you mean you dont see it? Its right there!" Christina shouted through the phone. I was driving along the crunchy, iced-over roads. The cars in front of me rolled along slowly, a quiet steam pouring from their tailpipes into the crisp, blue morning. I frantically scanned the horizon. A gentle sloping hill covered with naked, wiry trees obscured my view to the North. To the West the road was littered with condos, houses, and the occasional strip mall. To the South was a river, topped by bridges, which were lit up like runway strips that sloped upwards. To the East was our towering city, the one we had just left behind.. We had parted ways in the elevator, briefcases in hand, freshly dressed in business attire. The phone call in the car was to continue a conversation which had been interrupted when a couple of residents two floors down, dressed in pajamas and winter coats, entered the elevator.. "Beautiful dog" Christina said, to ...
In a well-publicized article in the February 23, 2005 issue of the Journal of Neuroscience, researchers from Spain describe changes in cannabinoid receptors in the brains of AD patients, as well as animal behavioral and in-vitro data suggesting that cannabinoid agonists can protect neurons by reducing microglial activation.. The headlines on this study were predictably tantalizing (see, for example, Marijuana May Block Alzheimers), but also misleading. The mass media stories barely dug beyond the papers stated implication that marijuanas active ingredients could stem the progression of neurodegeneration. In reality, however, the story is more complicated and still unfolding. To begin with, two cannabinoid receptors have been identified. CB1 is the major type in brain, expressed by all types of nervous system cells, and apparently responsible for the psychoactive effects of the drug. CB2 is mainly expressed in immune system cells, but also in microglia (Benito et al., 2003), and may mediate ...
Just How Cannabinoid Receptors Unlock Relief Of Pain and much more Youve heard the narrative that is well-worn Cannabis and cannabinoids are bad for you
References for Abcams Cannabinoid Receptor I peptide (320-334) (ab45820). Please let us know if you have used this product in your publication
This unit describes the use of cannabinoid radioligands in competitive binding assays for determining affinity parameters (IC50, Ki) of unlabeled compounds at transfected CB1 and CB2 receptors expressed in cell lines
This unit describes the use of cannabinoid radioligands in competitive binding assays for determining affinity parameters (IC50, Ki) of unlabeled compounds at transfected CB1 and CB2 receptors expressed in cell lines
Pharmaxis in Australia was actively engaged in a research programme focused on developing orally-available, synthetic selective cannabinoid receptor ligands,
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Frontiers | Cold Side-Effect Effect: Affect Does Not Mediate the Influence of Moral Considerations in Intentionality Judgments ...
Research has consistently shown that people consider harmful side effects of an action more intentional than helpful side effects. This phenomenon is known as the side-effect effect (SEE), which refers to the influence of moral considerations in judgments of intentionality and other non-moral concepts. There is an ongoing debate about how to explain this asymmetric pattern of judgment and the psychological factors involved in it. It has been posited that affective reactions to agents that bring about harmful side-effects could bias intentionality attributions in these cases, explaining the asymmetric pattern of intentionality judgments that we observe in the SEE. We call this the affective bias hypothesis (ABH). Evidence for the ABH is mixed, with some findings suggesting a role for affective processes, while others suggesting that affective processes play no role in the SEE. A possible explanation for these apparently contradictory results points to affective processes involved in the SEE being
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What we need is 100% enthusiastic support for scientific progress, combined with a clear understanding of what progress would be and a firm grip on what is done. Do we want to lose our jobs, and to have a large part of our population unable to earn a living? If not, then robotics might not be progress. Do we want to increase the rate of cancer and obesity? If not, then a diet based overwhelmingly on processed food might not be progress.. There is no possibility of making good ethical choices today, because there is no shared ethic. Communitarianism presupposes such an ethic, and we are far from having one.. Meanwhile, a co-worker today handed me a small tract called, "Dare the School Build a New Social Order?" Stay tuned!. ...
The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene. It is closely related to the cannabinoid receptor type 1, which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol, the active agent in cannabis, and other phytocannabinoids (plant cannabinoids). The principal endogenous ligand for the CB2 receptor is 2-arachidonoylglycerol (2-AG). CB2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol. The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the immune system. ...
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis. - Mechanism of Action & Protocol.
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Rimonabant: A Cannabinoid Receptor Type 1 Blocker for Management of Multiple Cardiometabolic Risk Factors | JACC: Journal of...
Cannabinoids have long been known to have potent psychotropic actions, but their wide-ranging effects on the cardiovascular system are just beginning to be unraveled.. In anesthetized rat models, intravenously administered anandamide produces a triphasic hemodynamic response (28): a brief period of vagally mediated bradycardia and hypotension, followed by a transitory pressor reaction, and a relatively prolonged vasodepressor response. The latter is the dominant effect of anandamide in animal models, and it results from CB1-mediated inhibition of norepinephrine release from presynaptic nerve terminals (29). In humans, acute administration of the cannabinoids produces vasodilation and tachycardia with a variable net effect on systemic blood pressure (30), but long-term use of THC results in CB1-mediated hypotension and bradycardia (31,32).. Although CB1receptors are mostly expressed on the neuronal terminals, there is evidence showing that other cell types express these receptors and participate ...
Rimonabant is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. It is an inverse agonist for the cannabinoid receptor CB1. Its main avenue of effect is reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States. This decision was made after a U.S. advisory panel recommended the medicine not be approved because it may increase suicidal thinking and depression.
Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB(2) Cannabinoid Receptor Activity -...
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 …
The digestive, nervous, circulatory and respiratory system are some of the well-known systems in the body, but theres a lesser known yet still important system most people havent heard of, the endocannabinoid system. This recently discovered system plays a major role in many of the our bodily functions, and is only b
Cannabinoid/Terpene Profile. Cannabinoid profiling during the growing stage enables the identification of plants that might have unique cannabinoid profiles of interest. These plants can provide growers with differentiated products and a competitive advantage in the market. Performing an analysis of compounds like cannabidiolic acid (CBDA) while a plant is still growing provides useful information for the optimization of growing conditions. Terpene profiling is also important as terpenes are primarily responsible for the taste and smell of cannabis. A terpene profile will provide further data in developing differentiated strains or products with optimum organoleptic qualities.. ...
Fenofibrate, a common treatment for high cholesterol, may stimulate the same receptors as cannabinoids, which could lead to a new class of drugs.
Ischemia-reperfusion injury (IRI) is a common cause of acute kidney injury (AKI), which is an increasing problem in the clinic and has been associated with increased rates of mortality. Currently, therapies to treat AKI are not available, so identification of new targets which, upon diagnosis of AKI, can be modulated to ameliorate renal damage is essential. In this study, a novel cannabinoid receptor 2 (CB2) agonist, SMM-295, was designed, synthesized, and tested in vitro and in silico. In vivo testing of the CB2 agonist was performed using a mouse model of bilateral IRI, which is a common model to mimic human AKI. Molecular docking of SMM-295 into a CB2 active-state homology model showed that SMM-295 interacts well with key amino acids to stabilize the active-state. In HEK-293 cells, SMM-295 was capable of reducing cAMP production with a 66-fold selectivity for the CB2 versus the cannabinoid receptor 1 (CB1), and dose-dependently increased MAPK and Akt phosphorylation. In mice, SMM-295 was ...
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The aim of this research project is to develop peripherally restricted cannabinoid receptor 1 (CB1R) antagonists for alcoholic steatosis. Alcohol abuse has detr...
NEW YORK, September 13, 2017 /PRNewswire/ -- Biosynthesis Technology Could Transform Cannabinoid Production. NetworkNewsWire Editorial Coverage.
Cannabinoids affect the receptor sites that comprise the endocannabinoid system, helping to body to achieve homeostasis in certain conditions.
In a well-publicized article in the February 23, 2005 issue of the Journal of Neuroscience, researchers from Spain describe changes in cannabinoid receptors in the brains of AD patients, as well as animal behavioral and in-vitro data suggest. ...
Our endocannabinoid system regulates balance in vital aspects of our biology. When our endocannabinoid system isnt signally and functioning optimally we can suffer from what is called Clinical Endocannabinoid Deficiency (CED).
Scientists are beginning to understand the role nutrition plays in keeping your endocannabinoid system healthy. SOL*CBD outlines ways to nurture ECS with diet!
Researchers report the love hormone, oxytocin, could enhance the pleasure of social interactions be stimulating the production of anandamide.... Read More... ...
The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details ...
A pentacyclic hybrid cannabinoid (4) has been synthesized, which combines structural elements of traditional cannabinoids and cannabmimetic indoles. Cannabinoid 4 contains a 1-pentylindole structure fused to the 2,3-positions of the partially reduced hydroxydibenzopyran system of THC. The successful approach to 4 employed 9-benzoyl-5,7-dimethoxy-1,2,3,4-tetrahydrocarbazole (17) as the starting material.
On these proscar warnings terminals, CB1 and CB2 cannabinoid receptors have been reported to inhibit nociceptive transmission, and both receptors seem to be acti- vated by an endogenous cannabinoid tone (37,51в53). T.
The present review synthetically describes the currently advanced hypotheses for a neurobiological basis of depression, ranging from the classical monoaminergic to the more recent neurotrophic hypothesis. Moreover, the Authors review the available preclinical and clinical evidence suggesting a possible role for the endocannabinoid system in the physiopathology of depression. Indeed, in spite of the reporting of conflicting results, the pharmacological enhancement of endocannabinoid activity at the CB1 cannabinoid receptor level appears to exert an antidepressant-like effect in some animal models of depression. On the contrary, a reduced activity of the endogenous cannabinoid system seems to be associated with the animal model of depression, namely the chronic mild stress model. Moreover, a few studies have reported an interaction of antidepressants with the endocannabinoid system. With regard to clinical studies, several authors have reported an alteration of endocannabinoid serum levels in ...
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 ...
Latest Progress in the Identification of Novel Synthetic Ligands for the Cannabinoid CB2 Receptor | BenthamScience
Title:Latest Progress in the Identification of Novel Synthetic Ligands for the Cannabinoid CB2 Receptor. VOLUME: 14 ISSUE: 5. Author(s):Shuang Han, Jiong-Jiong Chen and Jian-Zhong Chen. Affiliation:College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Rd, Hangzhou 310058, Zhejiang, P. R. China.. Keywords:Cannabinoid receptors, CB2, GPCRs, selective ligand, structure-activity relationship.. Abstract:Cannabinoid receptors, belonging to the superfamily of G-protein coupled receptors, play a major role in pathophysiology of a wide range of disparate diseases. Cannabinoid CB2 receptor, which mainly locates in peripheral tissues, represents as a promising drug target for the treatment of pain, osteoporosis, liver disorders, and so on without serious CNS side effects. In the past decades, the identification and optimization of selective ligands for the CB2 receptor has been a major objective in drug discovery. In the present review, we describe recent advances in the development of ...
Healthy wealth: Medical Studies that Prove Cannabis Can Cure Brain Cancer (3): Cellular/Molecular: Neuroprotection...
Excitotoxicity is a paradigm used to explain the biochemical events in both acute neuronal damage and in slowly progressive, neurodegenerative diseases. Here, we show in a longitudinal magnetic resonance imaging study that Δ9-tetrahydrocannabinol (Δ9-THC), the main active compound in marijuana, reduces neuronal injury in neonatal rats injected intracerebrally with the Na+/K+-ATPase inhibitor ouabain to elicit excitotoxicity. In the acute phase Δ9-THC reduced the volume of cytotoxic edema by 22%. After 7 d, 36% less neuronal damage was observed in treated rats compared with control animals. Coadministration of the CB1 cannabinoid receptor antagonist SR141716 prevented the neuroprotective actions of Δ9-THC, indicating that Δ9-THC afforded protection to neurons via the CB1 receptor. In Δ9-THC-treated rats the volume of astrogliotic tissue was 36% smaller. The CB1 receptor antagonist did not block this effect. These results provide evidence that the cannabinoid system can serve to protect the ...
Chronic treatment with a synthetic cannabinoid CP-55,940 alters G-protein expression in the rat central nervous system. |...
Prolonged exposure of rats to the synthetic cannabinoid receptor ligand, CP-55,940 (0.4 mg/kg, i.p. for 11 days), induced tolerance to analgesia, to the reduction in spontaneous locomotor activity and the incidence of splayed hind limbs. One hour after the last injection on day 11, the rats were killed and in situ hybridization was used to investigate the effect of treatment on G-protein alpha-subunit expression throughout the brain. Chronic cannabinoid exposure markedly reduced G alpha(s), G alpha(i) and G alpha(o) mRNA levels. The message for the alpha(s)-subunit was decreased in all the brain areas containing the basal autoradiographic signal; the decrease ranging from 25% in the thalamus to 45% in the mesencephalon. Also the basal G alpha(i) expression was reduced in tolerant rats showing the greatest decrease in the forebrain (63%) in the cerebellum (58%) and in the mesencephalon (38%). The reduction in G alpha(o) expression (25%) was more localized, being present only in the rostral portion of the
Thats Natural! is excited about the discoveries being made about cannabidiol (CBD) and the inherent endocannabinoid system that exists in each of our bodies. We hope you will do research for yourself, here are some links to places to start: Arthritis & Anti-Inflammatory 1- The nonpsychoactive cannabis constituent cannabidiol is an oral anti-arthritic therapeutic in murine collagen-induced…
Basal Ganglia. CB1 receptors are expressed throughout the basal ganglia and have well established effects on movement in rodents. As in the hippocampus, these receptors inhibit the release of glutamate or GABA transmitter, resulting in decreased excitation or reduced inhibition based on the cell they are expressed in. Consistent with the variable expression of both excitatory glutamate and inhibitory GABA interneurons in both the basal ganglias direct and indirect motor loops, synthetic cannabinoids are known to influence this system in a dose-dependent triphasic pattern. Decreased locomotor activity is seen at both higher and lower concentrations of applied cannabinoids, while an enhancement of movement may occur upon moderate dosages. However, these dose-dependent effects have been studied predominately in rodents and the physiological basis for this triphasic pattern warrants future research in humans. Effects may vary based on the site of cannabinoid application, input from higher cortical ...
Positive Allosteric Modulation of Cannabinoid Receptor Type 1 Suppresses Pathological Pain Without Producing Tolerance or...
PRF readers can get free access to a selected Journal of Pain paper each month, thanks to the American Pain Society. Get the free full text of the selection from the December 2017 issue here.. ...
LL: Do you see a place for both THC-containing cannabis and CBD-only cannabis in healthcare?. RM: Both compounds are of extreme interest, but not for the same diseases. In some disease states, the THC is more important than CBD, and there are other disease states where CBD is more important. For example, in autoimmune diseases, in which the body attacks itself for various reasons, CBD seems to be much better than THC. For example, in diabetes type 1, in which the body attacks the cells that produce insulin, CBD is much more important than THC. In other disease states like trauma, apparently, THC is more important. LL: What do you think about cannabis for up-regulating the endocannabinoid system for health and wellness, not just for treating diseases?. RM: The endocannabinoid system is of extreme importance. On the health side, there was just a review recently by senior people at NIH. They wrote that the endocannabinoid system is involved in essentially all human diseases. So obviously, its of ...
THC, it generally does not feature psychoactive (or narcotic) properties. Due to this (lack of) a function, its probable to utilize therapeutic attributes of Pot without getting high. The explanation for this big difference between the two ingredients is the fact, while THC immediately interacts with the CB1 and CB2 receptors in the body, CBD uses a rather oblique method towards the receptors.. Sensations in your brain and human anatomy are now being controlled by cannabinoid receptors, which are made to talk with Cannabinoids in plants which in turn are created by the mind for use in the torso according to necessity. A some of the frequent feelings which are underneath the get a handle on of cannabinoid receptors contain appetite, temper, pain, experience and memory.. While made to talk with the natural Endocannabinoids which are obviously created by the brain within the individual body. There are occasions that the human body needs additional security against the sounds (appetite, mood, ...
CB 2 agonists demonstrate remarkable anti inflammatory properties but , your , idea of receptor attraction has some merit, at least with respect to the , CB , 1 receptor. I recall an old study wherein they found that cannabis , tolerance , was proportional to the level of receptor retraction from the cell , surface. I wonder if, as with mu opioid tolerance, this effect is mediated by a PKC. Would inhibiting that PKC result in elevation of cannabinoid receptor levels? Also, B-cell proliferation appears to be partly under the regulation of a CB, although the research hasnt clarified it well yet. Ive always wondered if the way loss of gut bacteria knocks out the mu opioid and cannabinoid receptors of the gut wasnt also kicking antibody/B-cell production into needless overdrive (hence the use of B-cell depletion agents in autoimmune condition). , This does raise some worrying questions with respect to the chronic , ingestion of the same but the studies tend to find little ill effects. , ...
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Deletion Of CB2 Cannabinoid Receptor Induces Schizophrenia-Related Behaviors In Mice | 420 Magazine ®
Abstract The possible role of the CB2 receptor (CB2r) in psychiatric disorders has been considered. Several animal models use knockout (KO) mice that...
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New study provides insight on the mechanisms behind the development of kidney damage due to obesity, points to a potential target for protecting the kidney health of individuals with obesity
The cannabinoid receptor agonist WIN 55,212-2 reduces the initial cerebral damage after hypoxic-ischemic injury in fetal lambs. Alonso-Alconada D,
Dr. Saoirse OSullivan is a leading researcher in the field of cannabinoid research. Awarded the title of International Cannabinoid Research Society Young Investigator of the Year in 2016, Dr OSullivan has published numerous papers on the role of cannabinoid receptors in health and disease. SelectScience spoke to Dr OSullivan to find out more about her work.
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Cannabinoid receptor antagonists: a perspective | SpringerLink
Serra S, Brunetti G, Pani M, Vacca G, Carai MAM, Gessa GL, Colombo G (2002) Blockade by the cannabinoid CB1 receptor antagonist ... Serra S, Carai MAM, Brunetti G, Gomez R, Melis S, Vacca G, Colombo G, Gessa GL (2001) The cannabinoid receptor antagonist SR ... Carai M.A., Lobina C., Gessa G.L., Colombo G. (2005) Cannabinoid receptor antagonists: a perspective. In: Spanagel R., Mann K.F ... Colombo G, Vacca G, Serra S, Carai MAM, Gessa GL (2004) Suppressing effect of the cannabinoid CB1 receptor antagonist, SR ...https://link.springer.com/chapter/10.1007%2F3-7643-7305-9_17
Cannabinoid receptor antagonist - Wikipedia
A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of ... cannabinoid receptor 1 (CB1) and 2 (CB2). Both receptors are 7-transmembrane G-protein coupled receptors (GPCRs) which inhibit ... 1994), "SR141716A, a potent and selective antagonist of the brain cannabinoid receptor", FEBS Letters, 350 (2-3): 240-244, doi: ... This revived the research on cannabinoid receptor antagonists which were expected to help answer these questions. The use ...https://en.m.wikipedia.org/wiki/Discovery_and_development_of_Cannabinoid_Receptor_1_Antagonists
Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists. - PubMed - NCBI
Cannabinoid Receptor Antagonists. *N-(1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)-4-phenylpiperidin-4-yl) ... Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists.. Fulp A1, Bortoff K, Zhang Y, ... Cannabinoid receptor 1 (CB1) antagonists are potentially useful for the treatment of several diseases. However, clinical ... Even though otenabant penetrates the CNS, it is unique among CB1 antagonists that have been clinically tested because it has ...https://www.ncbi.nlm.nih.gov/pubmed/23098108
Cannabinoid receptor antagonist - Wikipedia
A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of ... cannabinoid receptor 1 (CB1) and 2 (CB2). Both receptors are 7-transmembrane G-protein coupled receptors (GPCRs) which inhibit ... This revived the research on cannabinoid receptor antagonists which were expected to help answer these questions. The use of ... 1994), "SR141716A, a potent and selective antagonist of the brain cannabinoid receptor", FEBS Letters, 350 (2-3): 240-244, doi: ...https://en.wikipedia.org/wiki/Cannabinoid_receptor_antagonist
Inhibition of alcoholic steatosis by a type 1 cannabinoid receptor antagonist | RTI
However, neutral antagonists or CNS-sparing peripherally restricted antagonists of CB1R may be useful for ALD as these ... Past reports suggest that antagonism of the CB1 receptor (CB1R) is an emerging strategy to alcoholic liver disease. ... Inhibition of alcoholic steatosis by a type 1 cannabinoid receptor antagonist ESBRA 2015 Meeting Abstract P-16. ... Inhibition of alcoholic steatosis by a type 1 cannabinoid receptor antagonist: ESBRA 2015 Meeting Abstract P-16. Alcohol and ...https://www.rti.org/publication/inhibition-alcoholic-steatosis-type-1-cannabinoid-receptor-antagonist-0
Effects of the cannabinoid CB1 receptor antagonist SR141716A on the behavior of pigeons and rats | SpringerLink
... a pyrazole derivative with high affinity for rat and human CB1 cannabinoid receptors, has recently been reported to reverse ... Effects of the cannabinoid CB1 receptor antagonist SR141716A on the behavior of pigeons and rats. ... a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 350:240-244Google Scholar ... Physical withdrawal in rats tolerant to Δ9-tetrahydrocannabinol precipitated by a cannabinoid receptor antagonist. Eur J ...https://link.springer.com/article/10.1007%2FBF02247436
Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist. - PubMed - NCBI
Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist.. Hirst RA1, ... CB1 receptor - data and references - Guide to Pharmacology. *Cannabinoid receptors - overview and references - Guide to ... Cannabinoid receptor agonists displaced [3H]SR141716A in a dose-dependent manner, (pKi) nabilone (8.29 +/- 0.08), WIN 55,212-2 ... We describe the use of SR141716A, a central cannabinoid antagonist, in radioligand binding and adenylyl cyclase (AC) inhibition ...https://www.ncbi.nlm.nih.gov/pubmed/8981483?dopt=Abstract
Pruritus Therapeutics Market (Antihistamines, Topical Corticosteroids, Opioid Receptor Antagonists, Topical Immunomodulators,...
Cannabinoid Receptors Global Pruritus Therapeutics Market: Regional Analysis. North America. U.S.. Europe. U.K.. Germany. ... Opioid Receptor Antagonists. Topical Immunomodulators. Antidepressants. Immunosuppressants. Topical Local Anesthetics. ... Pruritus Therapeutics Market (Antihistamines, Topical Corticosteroids, Opioid Receptor Antagonists, Topical Immunomodulators, ... cannabinoid receptors and others. This report also includes the current and forecast demand for the region of North America, ...https://www.medgadget.com/2017/06/pruritus-therapeutics-market-antihistamines-topical-corticosteroids-opioid-receptor-antagonists-topical-immunomodulators-antidepressants-immunosuppressants-topical-local-anesthetics-cannabinoi.html
Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4...
Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- ... Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- ...https://www.rti.org/publication/synthesis-long-chain-amide-analogs-cannabinoid-cb1-receptor-antagonist-n-piperidinyl-5-4
The neutral cannabinoid CB₁ receptor antagonist AM4113 regulates body weight through changes in energy intake in the rat.
The aim of this study was to determine if the neutral cannabinoid CB₁ receptor antagonist, AM4113, regulates body weight in the ... The aim of this study was to determine if the neutral cannabinoid CB₁ receptor antagonist, AM4113, regulates body weight in the ... We confirmed that the AM4113-induced reduction in food intake is mediated by CB₁ receptors using CB₁ receptor knockout mice. In ... These data suggest that blockade of an endocannabinoid tone acting at CB₁ receptors induces an initial, transient reduction in ...http://www.biomedsearch.com/nih/neutral-cannabinoid-CB1-receptor-antagonist/21056053.html
Effects of Cannabinoid Receptor Agonist and Antagonist Ligands on Production of Inflammatory Cytokines and Anti-Inflammatory...
1995) Novel antagonist implicates the CB1 cannabinoid receptor in the hypotensive action of anadamide. Eur J Pharmacol 278:279- ... 1998) SR1442528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J Pharmacol Exp Ther 284:644-650. ... a highly selective CB1 receptor antagonist, but not by SR144528, a highly selective CB2 receptor antagonist. Thus, the results ... 1997) SR141716A, a cannabinoid receptor antagonist produces hyperalgesia in untreated mice. Eur J Pharmacol 319:R3-R4. ...http://jpet.aspetjournals.org/content/293/1/136
LY320135, a Novel Cannabinoid CB1 Receptor Antagonist, Unmasks Coupling of the CB1 Receptor to Stimulation of cAMP Accumulation...
Use of antagonists in studies of cannabinoid receptor biology will be useful in separating receptor-dependent from receptor- ... or pyrazole cannabinoid receptor antagonists and may provide a novel approach to cannabinoid receptor antagonist development. ... LY320135, a Novel Cannabinoid CB1 Receptor Antagonist, Unmasks Coupling of the CB1 Receptor to Stimulation of cAMP Accumulation ... LY320135, a Novel Cannabinoid CB1 Receptor Antagonist, Unmasks Coupling of the CB1 Receptor to Stimulation of cAMP Accumulation ...http://jpet.aspetjournals.org/content/284/1/291?ijkey=01d39d72ee3d76806ade0909dca6359a5526e789&keytype2=tf_ipsecsha
Cannabinoid Type 1 Receptor Antagonists Modulate Transport Activity of Multidrug Resistance-Associated Proteins MRP1, MRP2,...
2009) Cannabinoid receptor CB1 antagonists: state of the art and challenges. Vitam Horm 81:159-189. ... Cannabinoid type 1 (CB1) receptor antagonists have been developed for the treatment of obesity, but a major disadvantage is ... 4-diarylpyrazoline CB1 receptor antagonists (Fig. 1) (Lange et al., 2005) and the prototypic CB1 receptor antagonist rimonabant ... Cannabinoid Type 1 Receptor Antagonists Modulate Transport Activity of Multidrug Resistance-Associated Proteins MRP1, MRP2, ...http://dmd.aspetjournals.org/content/39/7/1294?ijkey=0ab466caaf3197c805f2b6da02658ec479116c8f&keytype2=tf_ipsecsha
The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in...
The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ... The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ... The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ... The Cannabinoid CB1 Receptor Antagonist SR141716 Increases Acrp30 mRNA Expression in Adipose Tissue of Obese fa/fa Rats and in ...http://molpharm.aspetjournals.org/content/63/4/908
Cannabinoid CB1 receptor antagonists
Cannabinoid receptor subtypes. Cannabinoids and the zebra finch. Cannabinoid CB1 receptor and emotion. CB1 cannabinoid receptor ... CB1 cannabinoid receptor agonism isnt rewarding 01 02 03 04 05 06 07 08 09 10 11 12 13 14 15. HOME. Refs. HedWeb. Future ... This review examines the development of cannabinoid CB1 receptor antagonists as a new class of therapeutic agents for drug ... CANNABINOID CB1 ANTAGONISTS AS PROMISING NEW MEDICATIONS FOR DRUG DEPENDENCE by. Le Foll B, Goldberg SR. NIDA. J Pharmacol Exp ...https://www.cannabis-marijuana.com/cb1/antagonists.html
GPR55 is a cannabinoid receptor that increases intracellular calcium and inhibits M current | PNAS
The CB1 antagonist SR141716A, but not the CB2 antagonist SR144528, is a GPR55 antagonist. (A) Summary calcium responses in ... The effects of cannabinoid compounds are largely mediated by cannabinoid receptors. CB1, cloned in 1990 (1), is widely and ... 2007) The orphan receptor GPR55 is a novel cannabinoid receptor. Br J Pharmacol 152:1092-1101.. ... Here, we provide further evidence that GPR55, a G protein-coupled receptor, is a cannabinoid receptor. GPR55 is highly ...https://www.pnas.org/content/105/7/2699
Crystal Structure of the Human Cannabinoid Receptor CB2
Two of the cannabinoid receptors, CB1 and CB2 are the key targets of this endocannabinoid system. ... The authors also compare this conformation to the structure of antagonist (AM6538)-bound CB1 receptor. While both AM10257 and ... Two of the cannabinoid receptors, CB1 and CB2 are the key targets of this endocannabinoid system. While CB1 is widely present ... 2019, August 29). Crystal Structure of the Human Cannabinoid Receptor CB2. News-Medical. Retrieved on September 19, 2019 from ...https://www.news-medical.net/life-sciences/Crystal-Structure-of-the-Human-Cannabinoid-Receptor-CB2.aspx
Cannabinoid receptor type 2 - Wikipedia
"CB1 and CB2 cannabinoid receptor antagonists prevent minocycline-induced neuroprotection following traumatic brain injury in ... The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that ... CNR2, CB-2, CB2, CX5, Cannabinoid receptor type 2, cannabinoid receptor 2. ... G-protein coupled receptor activity. • signal transducer activity. • cannabinoid receptor activity. Cellular component. • ...https://en.wikipedia.org/wiki/CB2_receptor
Δ-9-Tetrahydrocannabinol Inhibits Antitumor Immunity by a CB2 Receptor-Mediated, Cytokine-Dependent Pathway | The Journal of...
SR144528, an antagonist of the CB2 cannabinoid receptor, blocks the THC-mediated increase in tumor growth in vivo. BALB/c mice ... CB2 cannabinoid receptor antagonist prevents the THC-mediated increase in tumor growth in vivo. Based on previous studies, we ... CB2 cannabinoid receptor antagonist studies. To determine whether the THC effect on tumorigenicity in vivo is mediated through ... SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J. Pharmacol. Exp. Ther. 284: 644. ...http://www.jimmunol.org/content/165/1/373?ijkey=5da9c5eba731e31f556d80c33bd029ea2ef71218&keytype2=tf_ipsecsha
Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-...
Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-( ... Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-( ... Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-( ... T1 - Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist ...https://abdn.pure.elsevier.com/en/publications/synthesis-and-structure-activity-relationships-of-amide-and-hydra
Heart Disease - Alair Castro - Studies: Rimonabant: A novel selective cannabinoid-1 receptor antagonist
Summary. Discovery of the cannabinoid receptors has led to the development of rimonabant, a cannabinoid-1 (CB1) antagonist. ... Rimonabant: A novel selective cannabinoid-1 receptor antagonist for treatment of obesity. American Journal of Health-System ... Selective blockade of this receptor has been shown to lead to decreased appetite and food intake in animal models. Clinical ... Conclusion. Rimonabant, a selective CB1 antagonist, is a novel treatment option for obese and overweight individuals. ...http://heartdisease-alaircastro.blogspot.com/2007/05/rimonabant-novel-selective-cannabinoid.html
Cannabinoid receptor type 1 - Wikipedia
"Evidence that the plant cannabinoid Δ9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist". British ... 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. ... "Entrez Gene: CNR1 cannabinoid receptor 1 (brain)".. *^ Demuth DG, Molleman A (January 2006). "Cannabinoid signalling". Life ...https://en.m.wikipedia.org/wiki/Cannabinoid_receptor_type_1
Obesity Treatment & Management: Approach Considerations, Patient Screening, Assessment, and Expectations, Weight-Loss Goals
Cannabinoid-receptor antagonists. The central cannabinoid system has an increasingly recognized role in appetite and feeding ... Cannabinoid receptor antagonists and obesity. Curr Opin Investig Drugs. 2004 Apr. 5(4):389-94. [Medline]. ... Rimonabant, the most-developed CB1-receptor antagonist, caused a mean weight loss of 3-6 kg over a 1-year follow-up at doses of ... Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight ...https://emedicine.medscape.com/article/123702-treatment
STUDY: Evidence that the plant cannabinoid Δ9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist
Cannabinoid - Δ9-tetrahydrocannabivarin (THCV) displaced [3H]CP55940 from specific binding sites on mouse brain and CHO-hCB2 ... STUDY: Evidence that the plant cannabinoid Δ9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist. Written ... CB1 receptor antagonist, CB2 receptor antagonist, CP55940, methanandamide, mouse vas deferens, R-(+)-WIN55212, Δ9- ... THCV behaves as a competitive CB1 and CB2 receptor antagonist. In the vas deferens, it antagonized several cannabinoids more ...https://www.thecannabisadvisory.com/clinical-studies/health_condition/study-evidence-that-the-plant-cannabinoid-%CE%B49-tetrahydrocannabivarin-is-a-cannabinoid-cb1-and-cb2-receptor-antagonist/
SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in chronically alcoholized Wistar rats. | DIAL...
SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in chronically alcoholized Wistar rats.. In: ... SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in chronically alcoholized Wistar rats. Primary ... Home» SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in chronically alcoholized Wistar rats. ... This study investigated the effect of the new CB1 cannabinoid receptor antagonist, SR147778, on ethanol preference in ...https://dial.uclouvain.be/pr/boreal/object/boreal:10786
Agonists and antagonists1990BlockadeCentral cannabinoidAlcoholpreferring ratsPotentModulateSR141716AAnandamideKnockout miceSelective CB1 antagonist1995AnalogsAdenylyl cyclaseBehavioral effectsAngiotensin receptor blockersEthanol preferencePharmacologyPeripherally selectiveCannabidiolPsychoactiveMediatesTreatment of obesityAffinityPharmacological propertiesBindsRegulatesIntakePeripheral tissuesTherapeuticMetabolic factorsCannabimimeticTetrahydrocannabinolObeseEffectsIntracellularDopamineResponsesPeripheryPrimarilyPredominantly
- CB 1 , cloned in 1990 ( 1 ), is widely and highly expressed in the CNS, where it likely mediates the majority of the psychotropic and behavioral effects of cannabinoids. (pnas.org)
- The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB 1 ) receptor, discovered in 1990. (wikipedia.org)
- Lallemand F, Soubrié PH, De Witte PH (2001) Effects of CB1 cannabinoid receptor blockade on ethanol preference after chronic ethanol administration. (springer.com)
- And Δ9-tetrahydrocannabivarin (THCV), a naturally occurring cannabinoid, modulate the effects of THC via direct blockade of cannabinoid CB1 receptors, thus behaving like first-generation CB1 receptor inverse agonists, such as rimonabant. (wikipedia.org)
- These data suggest that blockade of an endocannabinoid tone acting at CB₁ receptors induces an initial, transient reduction in food intake which results in long-term reduction of body weight gain. (biomedsearch.com)
- Blockade of CB1 receptor activity by genetic invalidation also decreases rewarding effects of opiates and alcohol in animals. (cannabis-marijuana.com)
- Although CB1 receptor blockade is generally ineffective in reducing the self-administration of cocaine in rodents and primates, it reduces the reinstatement of extinguished cocaine-seeking behavior produced by cocaine-associated conditioned stimuli and cocaine priming injections. (cannabis-marijuana.com)
- Similarly, CB1 receptor blockade is effective in reducing nicotine-seeking behavior induced by re-exposure to nicotine-associated stimuli. (cannabis-marijuana.com)
- Selective blockade of this receptor has been shown to lead to decreased appetite and food intake in animal models. (blogspot.com)
- Arnone M, Maruani J, Chaperon F, Thiébot M-E, Poncelet M, Soubrié P, Le Fur G (1997) Selective inhibition of sucrose and alcohol intake by SR 141716, an antagonist of central cannabinoid (CB1) receptors. (springer.com)
- Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist. (nih.gov)
- We describe the use of SR141716A, a central cannabinoid antagonist, in radioligand binding and adenylyl cyclase (AC) inhibition studies in rat cerebella membranes. (nih.gov)
- CBD is a very low-affinity CB1 ligand, that can nevertheless affect CB1 receptor activity in vivo in an indirect manner, while THCV is a high-affinity CB1 receptor ligand and potent antagonist in vitro and yet only occasionally produces effects in vivo resulting from CB1 receptor antagonism. (wikipedia.org)
- Our efforts have resulted in an orally absorbed compound that is a potent and selective CB1 antagonist with limited penetration into the CNS. (nih.gov)
- One of the major advances in CB research has been the development of a potent and selective antagonist of the CB1 receptor, SR 141716A [ N -(piperdin-1-yl)-5-(4-chloropheny)-1-(2,4-dichloropheny)-4-methyl-1 H -pyrazole-3-carboxamide hydrochloride]. (aspetjournals.org)
- LY320135 is a promising lead compound for the further development of novel, potent and selective cannabinoid antagonists of novel structure. (aspetjournals.org)
- SR141716A was found to be selective and potent at the CB1 receptor and blocked WIN 55212-2-mediated behavioral responses. (aspetjournals.org)
- In the vas deferens, it antagonized several cannabinoids more potently than THC and was also more potent against CP55940 and R -(+)-WIN55212 in this tissue than in brain membranes. (thecannabisadvisory.com)
- Cannabinoid CB1 receptors are expressed in this brain reward circuit and modulate the dopamine-releasing effects of Delta(9)-THC and nicotine. (cannabis-marijuana.com)
- it is not surprising that cannabinoids modulate emotional responses and emotional states, as well as cognitive and memory processes. (frontiersin.org)
- SR141716A (Sanofi Recherche), a pyrazole derivative with high affinity for rat and human CB1 cannabinoid receptors, has recently been reported to reverse biochemical, physiological and behavioral effects induced by cannabinoid agonists. (springer.com)
- Cannabinoid receptor agonists displaced [3H]SR141716A in a dose-dependent manner, (pKi) nabilone (8.29 +/- 0.08), WIN 55,212-2 (7.75 +/- 0.15), delta 9-tetrahydrocannabinol (7.29 +/- 0.21), delta 8-tetrahydrocannabinol (6.53 +/- 0.09) and anandamide (5.92 +/- 0.04). (nih.gov)
- In addition, studies with SR141716A have provided evidence for the presence of CB1 receptors in peripheral tissues as well as in the central nervous system (CNS). (aspetjournals.org)
- In the first step, the authors created crystals of CB2 antagonist AM10257 which was obtained by optimizing the first known antagonist of CB1, SR141716A. (news-medical.net)
- LY320135 functionally reversed anandamide-mediated adenylate cyclase inhibition in Chinese hamster ovary (CHO) cells stably expressing the CB1 receptor. (aspetjournals.org)
- Pertussis toxin treatment of CHO cells expressing the CB1 receptor attenuated the anandamide-mediated inhibition of adenylate cyclase and unmasked a stimulatory effect of anandamide on adenylate cyclase. (aspetjournals.org)
- These discoveries have led to a growing interest in determining the physiological role of anandamide, other fatty acid amides and cannabinoid receptors. (aspetjournals.org)
- GPR55 is highly expressed in large dorsal root ganglion neurons and, upon activation by various cannabinoids (Δ 9 THC, the anandamide analog methanandamide, and JWH015) increases intracellular calcium in these neurons. (pnas.org)
- Naassila M, Pierrefiche O, Ledent C, Daoust M (2004) Decreased alcohol self-administration and increased alcohol sensitivity and withdrawal in CB1 receptor knockout mice. (springer.com)
- We confirmed that the AM4113-induced reduction in food intake is mediated by CB₁ receptors using CB₁ receptor knockout mice. (biomedsearch.com)
- In addition, in adipose tissue of CB 1 -receptor knockout mice, SR141716 had no effect on Acrp30 mRNA expression, demonstrating a CB 1 receptor mediating effect. (aspetjournals.org)
- Compton DR, Johnson MR, Melvin LS, Martin BR (1992) Pharmacological profile of a series of bicyclic cannabinoid analogs: classification as cannabimimetic agents. (springer.com)
- Among the different factors involved, of particular interest is the binding affinity of endocannabinoids, and their analogs, for other receptor families beyond cannabinoid receptors, such as the peroxisome proliferator-activated receptors (PPARs), and the transient receptor potential cation channel subfamily V member 1 (TRPV1). (frontiersin.org)
- CB1 receptors are coupled through Gi/o proteins and inhibit adenylyl cyclase and activate mitogen-activated protein (MAP) kinase. (wikipedia.org)
- Like the CB 1 receptors, CB 2 receptors inhibit the activity of adenylyl cyclase through their Gi/Go α subunits. (wikipedia.org)
- Like noladin, the synthetic ligand CP-55,940 has also been shown to preferentially inhibit adenylyl cyclase in CB 2 receptors. (wikipedia.org)
- Wang L, Liu J, Harvey-White J, Zimmer A, Kunos G (2003) Endocannabinoid signaling via cannabinoid receptor 1 is involved in ethanol preference and its age-dependent decline in mice. (springer.com)
- SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in chronically alcoholized Wistar rats. (uclouvain.be)
- This study investigated the effect of the new CB1 cannabinoid receptor antagonist, SR147778, on ethanol preference in chronically alcoholized Wistar rats. (uclouvain.be)
- Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists. (nih.gov)
- Even though otenabant penetrates the CNS, it is unique among CB1 antagonists that have been clinically tested because it has properties that are normally associated with peripherally selective compounds. (nih.gov)
- In summary, RTI-13329-173B and other such peripherally selective CB1R antagonists should be further developed and investigated for alcoholic liver disease. (rti.org)
- These results suggest that SR is an effective antagonist of the psychoactive effects of cannabinoids. (springer.com)
- Psychoactive cannabinoids (CBs) have a variety of pharmacological effects that are evoked through interactions with central or peripheral CB receptors. (aspetjournals.org)
- The CB 1 cannabinoid receptor mediates many of the psychoactive effects of Δ 9 THC, the principal active component of cannabis. (pnas.org)
- It is closely related to the cannabinoid receptor type 1 , which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol , the active agent in cannabis , and other phytocannabinoids (plant cannabinoids). (wikipedia.org)
- LY320135 is a selective antagonist for the brain CB1 receptor, having greater than 70-fold higher affinity for the CB1 than the peripheral CB2 receptor. (aspetjournals.org)
- Few other modifications, such as the addition of an amide group along with the 1-adamantyl group at C-3 position and stabilization of the ligand-CB2 receptor increased the affinity of the antagonist for CB2 and also promoted CB2 crystals. (news-medical.net)
- The corresponding amide analogues were compared to the hydrazides to determine the effect of the second nitrogen on receptor binding affinity. (elsevier.com)
- 2) or the antagonist [H-, 14 exhibited the highest CB, affinity. (elsevier.com)
- In general, increasing the length and bulk of the substituent was associated with increased receptor affinity and efficacy (as measured in a guanosine 5'-triphosphate-gamma-[S-assay). (elsevier.com)
- However, in most instances, receptor affinity and efficacy increases were no longer observed after a certain chain length was reached. (elsevier.com)
- CB 2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol . (wikipedia.org)
- We tested two cannabinoid compounds with different pharmacological properties in the inhibitory avoidance task, and evaluated whether the observed effects are mediated by cannabinoid, PPARα or TRPV1 receptor activation. (frontiersin.org)
- Colombo G, Serra S, Brunetti G, Gomez R, Melis S, Vacca G, Carai MAM, Gessa GL (2002) Stimulation of voluntary ethanol intake by cannabinoid receptor agonists in ethanol-preferring sP rats. (springer.com)
- Colombo G, Agabio R, Fà M, Guano L, Lobina C, Loche A, Reali R, Gessa GL (1998) Reduction of voluntary ethanol intake in ethanol-preferring sP rats by the cannabinoid antagonist SR 141716. (springer.com)
- These results reinforce the hypothesis that the cannabinoid CB1 receptor is part of the neural substrate mediating alcohol intake and the motivational properties of alcohol. (uclouvain.be)
- Therefore, peripheral CB1 receptor antagonists might have therapeutic potential for improving metabolic risk in obese patients without causing psychiatric side effects. (aspetjournals.org)
- T his review examines the development of cannabinoid CB1 receptor antagonists as a new class of therapeutic agents for drug addiction. (cannabis-marijuana.com)
- However, ample evidence suggests that additional receptors may contribute to the behavioral, vascular, and immunological actions of Δ 9 tetrahydrocannabinol (THC) and endogenous cannabinoids ( 3 ). (pnas.org)
- Marijuana smoke produces its psychotropic effects by delivering milligram quantities of cannabinoids, including primarily Δ-9-tetrahydrocannabinol (THC), 3 to the lung ( 1 ). (jimmunol.org)
- Two types of cannabinoid receptors, CB1 and CB2, responsible for the effects of THC were discovered and cloned in the early 1990s. (wikipedia.org)
- However, clinical development of several CB1 antagonists was halted due to central nervous system (CNS)-related side effects including depression and suicidal ideation in some users. (nih.gov)
- However, neutral antagonists or CNS-sparing peripherally restricted antagonists of CB1R may be useful for ALD as these compounds should have limited adverse effects. (rti.org)
- CB1 receptors are present at high densities in the forebrain and cerebellum consistent with the observed effects of CBs on cognition and movement. (aspetjournals.org)
- The CB2 receptor may mediate some of the peripheral effects of THC, such as immunosuppression ( Martin, 1986 ). (aspetjournals.org)
- Selective targeting of peripheral CB1 receptors might be an option to circumvent these side effects. (aspetjournals.org)
- The effects of cannabinoid compounds are largely mediated by cannabinoid receptors. (pnas.org)
- The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the immune system. (wikipedia.org)
- In vivo administration of a specific antagonist of the CB2 cannabinoid receptor also blocked the effects of THC. (jimmunol.org)
- The recent documentation of specific cannabinoid receptor expression by leukocytes has generated increased interest in the immunomodulatory effects of THC ( 7 , 12 ). (jimmunol.org)
- WIN55,212-22 effects on memory consolidation were predominantly mediated by CB1 receptor activation but CB2 receptors were involved as well. (frontiersin.org)
- Our findings drive beyond the classical hypothesis centered on the unique role of CB1 receptor activation for cannabinoid effects on memory, and reveal new insights in the neural mechanisms of memory consolidation. (frontiersin.org)
- Activation of GPR55 by Cannabinoids Increases Intracellular Calcium. (pnas.org)
- As is commonly seen in G protein-coupled receptors, the CB 2 receptor has seven transmembrane spanning domains, a glycosylated N-terminus , and an intracellular C-terminus . (wikipedia.org)
- These interactions induce a conformational change in the receptor structure, which triggers the activation of various intracellular signaling pathways. (wikipedia.org)
- CB1 receptors are present in highest concentration in the brain but can also be found in the periphery. (wikipedia.org)
- Recently, studies have indicated that selective regulation of CB1 receptors in the periphery is a viable strategy for treating several important disorders. (nih.gov)
- CB1 antagonists that are reported to be selective for the periphery. (nih.gov)