Loading...
*  Cannabinoid receptor type 2
Cannabinoid receptor agonists reduce gut motility in IBS patients. Application of CB2-specific antagonists has found that these ... The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that ... Cannabinoid receptor Cannabinoid receptor type 1 (CB1) GRCh38: Ensembl release 89: ENSG00000188822 - Ensembl, May 2017 GRCm38: ... The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB1 ...
*  Cannabinoid receptor antagonist
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: ...
*  WIN 54,461
"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 ...
*  Otenabant
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 ...
*  WIN 56,098
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". ...
*  Ibipinabant
... 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 ...
*  AM-251 (drug)
... 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: ...
*  Surinabant
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 ...
*  Drinabant
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 ...
*  Rosonabant
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 ...
*  Endocannabinoid enhancer
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 ...
*  NESS-0327
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 ...
*  O-2050
... 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 ...
*  SR-144,528
"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 ...
*  Cannabinoid receptor type 1
Discovery and development of Cannabinoid Receptor 1 Antagonists Cannabinoid receptor Cannabinoid receptor type 2 (CB2) GRCh38: ... The cannabinoid type 1 receptor, often abbreviated as CB1, is a G protein-coupled cannabinoid receptor located primarily in the ... "Evidence that the plant cannabinoid Δ9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist". British ... 2015-01-01). "CB1 and CB2 cannabinoid receptor antagonists prevent minocycline-induced neuroprotection following traumatic ...
*  Tetrahydrocannabivarin
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 ...
*  Endocannabinoid system
Santucci V, Storme JJ, Soubrié P, Le Fur G (1996). "Arousal-enhancing properties of the CB1 cannabinoid receptor antagonist SR ... "CB1 cannabinoid receptor activity is modulated by the cannabinoid receptor interacting protein CRIP 1a". Mol. Pharmacol. 72 (6 ... which are endogenous lipid-based retrograde neurotransmitters that bind to cannabinoid receptors, and cannabinoid receptor ... All effects were abolished by the CB1 antagonist AM251, supporting the conclusion that these effects were cannabinoid-receptor ...
*  Taranabant
Cannabinoid receptor antagonist Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, et al. "Substituted acyclic ... Taranabant (codenamed MK-0364) is a cannabinoid receptor type 1 inverse agonist that was investigated as a potential treatment ... "Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1- ... sulfonamides as human cannabinoid-1 receptor inverse agonists." Bioorganic & Medicinal Chemistry Letters. 2007 Apr 15;17(8): ...
*  Fingolimod
... has been reported to be a cannabinoid receptor antagonist, a cPLA2 inhibitor and a ceramide synthase inhibitor. It ... interact with the CB1 cannabinoid receptor". Mol. Pharmacol. 70 (1): 41-50. doi:10.1124/mol.105.020552. PMID 16571654. Payne SG ... Hla T, Lee MJ, Ancellin N, Paik JH, Kluk MJ (2001). "Lysophospholipids--receptor revelations". Science. 294 (5548): 1875-8. doi ... Fingolimod is a sphingosine-1-phosphate receptor modulator, which sequesters lymphocytes in lymph nodes, preventing them from ...
*  TM-38837
... is among the first of a new generation of cannabinoid receptor antagonist designed to avoid the central nervous system ... TM-38837 is a small molecule inverse agonist/antagonist of the CB1 cannabinoid receptor, with peripheral selectivity. It is ... 1H-pyrazole-3-carboxamide as a Potential Peripheral Cannabinoid-1 Receptor Inverse Agonist". ChemMedChem. 5 (9): 1439-1443. doi ... liabilities of the first generation CB1 receptor antagonists such as rimonabant. AM-6545 https://web.archive.org/web/ ...
*  Tetrahydrocannabinol-C4
... 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 ...
*  PSB-SB-487
... a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists. Journal of ... PSB-SB-487 is a coumarin derivative which is an antagonist at the former orphan receptor GPR55. Unlike older GPR55 antagonists ... However it has poorer selectivity over other related receptors, acting as a weak antagonist at CB1 with a Ki of 1170nM, and a ... "Antagonists for the orphan G protein-coupled receptor GPR55 based on a coumarin scaffold". Journal of Medicinal Chemistry. 56 ( ...
*  VCHSR
... is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It is derived ... 2006). "Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28( ... so that VCHSR instead acts as a neutral antagonist, blocking the receptor but producing no physiological effect of its own. ... is crucial for its inverse agonism at the cannabinoid CB1 receptor". Molecular Pharmacology. 62 (6): 1274-87. doi:10.1124/mol. ...
*  PSB-SB-1202
... a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists. Journal of ... PSB-SB-1202 is a coumarin derivative which is an agonist at the cannabinoid receptors CB1 and CB2, with a CB1 Ki of 32nM and a ... It is also a weak antagonist at the related receptor GPR55, with an IC50 of 6350nM, but has no significant affinity for GPR18. ... "Antagonists for the orphan G protein-coupled receptor GPR55 based on a coumarin scaffold". Journal of Medicinal Chemistry. 56 ( ...
*  LY-320,135
... a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. Journal ... LY-320,135 is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It was ... Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sciences. 2005 Feb 4;76(12):1307-24. PMID 15670612. ... and at higher doses it also binds to a range of non-cannabinoid receptors. However LY-320,135 is still fairly widely used in ...
*  Single Convention on Narcotic Drugs
In particular, the discovery of the cannabinoid receptor system in the late 1980s revolutionized scientific understanding of ... agonist-antagonist opioid) butorphanol (agonist-antagonist opioid) There are of course many opioid designer drugs, not used in ... Semisynthetic agonist-antagonist opioids: buprenorphine Synthetic agonist-antagonist opioids - benzomorphans: pentazocine ... Cannabinoids (natural and synthetic) and opioids (synthetic and semisynthetic) are scheduled by Convention on Psychotropic ...
*  CP 55,940
... cannabinoid receptor antagonist, in rodent brain". Life Sciences. 58 (15): 1239-1247. doi:10.1016/0024-3205(96)00085-9. PMID ... "Cannabinoid receptor agonists upregulate and enhance serotonin 2A (5-HT2A) receptor activity via ERK1/2 signaling". Synapse. 67 ... Tomiyama, K.; Funada, M. (2011). "Cytotoxicity of synthetic cannabinoids found in 'Spice' products: The role of cannabinoid ... but is an antagonist at GPR55, the putative "CB3" receptor. CP 55,940 showed protective effects on rat brain mitochondria upon ...