Rinaldi-Carmona M, Barth F, Héaulme M, Shire D, Calandra B, Congy C, Martinez S, Maruani J, Néliat G, Caput D
Sanofi Recherche, Montpellier, France.
FEBS Lett. 1994 Aug 22;350(2-3):240-4. doi: 10.1016/0014-5793(94)00773-x.
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.
SR141716A是首个脑大麻素受体的选择性口服活性拮抗剂。该化合物对中枢大麻素受体表现出纳摩尔级亲和力，但对外周大麻素受体无活性。在体外，SR141716A可拮抗大麻素受体激动剂对小鼠输精管收缩和大鼠脑膜中腺苷酸环化酶活性的抑制作用。腹腔注射或口服给药后，SR141716A可拮抗大麻素受体激动剂的经典药理和行为学效应。该化合物应可证明是研究花生四烯乙醇胺/大麻素系统体内功能的有力工具。
