J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.
J-113397 (0-500 nM) inhibits NociceptinNociceptin/orphanin FQ -stimulated [35S]GTPγS binding to CHO cells expressing ORL1 (CHO-ORL1) but had no effect on [35S]GTPγS binding by itself[1].
J-113397 (0-30 mg/kg; subcutaneously (s.c.); once) dose-dependently inhibits hyperalgesia elicited by intracerebroventricular (i.c.v.) administration of NociceptinNociceptin/orphanin FQ in a tail-flick test with mice[1].
















