Premium
SR141716A, a potent and selective antagonist of the brain cannabinoid receptor
Author(s) -
Rinaldi-Carmona Murielle,
Barth Francis,
Héaulme Michel,
Shire David,
Calandra Bernard,
Congy Christian,
Martinez Serge,
Maruani Jeanne,
Néliat Gervais,
Caput Daniel,
Ferrara Pascual,
Soubrié Philippe,
Brelière Jean Claude,
Le Fur Gérard
Publication year - 1994
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(94)00773-x
Subject(s) - cannabinoid , cannabinoid receptor , gpr18 , pharmacology , cannabinoid receptor antagonist , chemistry , cannabinoid receptor type 2 , anandamide , depolarization induced suppression of inhibition , rimonabant , antagonist , competitive antagonist , receptor , biology , biochemistry
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.