Central administration of [Phe1psi(CH2-NH)Gly2]nociceptin(1-13)-NH2 and orphanin FQ/nociceptin (OFQ/N) produce similar cardiovascular and renal responses in conscious rats.

摘要: In vitro studies have shown that [Phe 1 Ψ(CH 2 -NH)Gly ]OFQ/N(1–13)-NH (referred to as [FG]OFQ/N(1–13)-NH ) is the first selective antagonist prevent binding of endogenous ligand orphanin FQ/Nociceptin (OFQ/N) at orphan opioid-like receptor. present study, we examined potential changes in cardiovascular and renal function produced by i.c.v. injection conscious Sprague-Dawley rats. rats, a marked sustained decrease heart rate, mean arterial pressure, urinary sodium excretion profound increase urine flow rate (i.e., water diuresis). The excretory responses were dose dependent similar pattern but longer duration than evoked OFQ/N. other animals, OFQ/N(1–13)-NH , metabolite comparable those . contrast, OFQ/N(2–17), fragment OFQ/N [OFQ/N(1–17)], was inactive when administered centrally. Finally, performed determine whether may be an receptor centrally alone inactive. these studies, pretreatment animals with low-dose failed response Although reported vitro, findings indicate this compound has agonist activity vivo.