SR141716A, a potent and selective antagonist of the brain cannabinoid receptor
M Rinaldi-Carmona, F Barth, M Héaulme, D Shire… - FEBS letters, 1994 - Elsevier
M Rinaldi-Carmona, F Barth, M Héaulme, D Shire, B Calandra, C Congy, S Martinez…
FEBS letters, 1994•ElsevierSR141716A 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 …
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 …
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.
Elsevier
