title: SR141716A, a potent and selective antagonist of the brain cannabinoid receptor.
abstract: SR141716A is the first selective and orally active antagonist of the brain cannabinoid receptor. This compound displays nanomolar affinity for the central cannabinoid receptor but is not active on the peripheral cannabinoid receptor. In vitro, SR141716A antagonises the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes. After intraperitoneal or oral administration SR141716A antagonises classical pharmacological and behavioural effects of cannabinoid receptor agonists. This compound should prove to be a powerful tool for investigating the in vivo functions of the anandamide/cannabinoid system.
authors.affiliation: Sanofi Recherche, Montpellier, France.
authors.forename: M
authors.initials: M
authors.lastname: Rinaldi-Carmona
authors.forename: F
authors.initials: F
authors.lastname: Barth
authors.forename: M
authors.initials: M
authors.lastname: Héaulme
authors.forename: D
authors.initials: D
authors.lastname: Shire
authors.forename: B
authors.initials: B
authors.lastname: Calandra
authors.forename: C
authors.initials: C
authors.lastname: Congy
authors.forename: S
authors.initials: S
authors.lastname: Martinez
authors.forename: J
authors.initials: J
authors.lastname: Maruani
authors.forename: G
authors.initials: G
authors.lastname: Néliat
authors.forename: D
authors.initials: D
authors.lastname: Caput
mesh_terms: D000818:Animals; D048588:Benzoxazines; D001667:Binding, Competitive; D001681:Biological Assay; D001921:Brain / Q000187:drug effects*; D002186:Cannabinoids / Q000494:pharmacology*; D002462:Cell Membrane / Q000378:metabolism; D003511:Cyclohexanols / Q000378:metabolism; D066298:In Vitro Techniques; D051379:Mice; D009025:Morpholines / Q000494:pharmacology; D009281:Naphthalenes / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology*; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*; D000077285:Rimonabant
chemical_list: D048588:Benzoxazines; D002186:Cannabinoids; D003511:Cyclohexanols; D009025:Morpholines; D009281:Naphthalenes; D010880:Piperidines; D011720:Pyrazoles; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; C070417:(3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone; C054649:3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-4-(3-hydroxypropyl)cyclohexanol; D000077285:Rimonabant