BAN-ORL-24-(hydrochloride)

BAN ORL 24 is an antagonist of the nociceptin (NOP) receptor (Ki = 0.24 nM in a radioligand binding assay using CHO cell membranes expressing the human receptor). It is selective for NOP receptors over μ-, δ-, and κ-opioid receptors (Kis = 0.19, 0.34, and >1 µM, respectively). BAN ORL 24 reduces NOP-induced GTPγS binding (pA2 = 9.98) and calcium mobilization (KB = 0.93 nM) in CHO cells. It inhibits electrically induced twitches in isolated mouse and rat vas deferens, as well as isolated guinea pig ileum, when used at a concentration of 100 nM. BAN ORL 24 (10 mg/kg) reverses thermal and mechanical...