Champion H C, Czapla M A, Kadowitz P J
Department of Pharmacology, Tulane University School of Medicine, New Orleans, Louisiana 70112, USA.
Peptides. 1997;18(5):729-32. doi: 10.1016/s0196-9781(97)00003-x.
The heptadecapeptide nociceptin, also known as Orphanin FQ, is a newly discovered endogenous ligand for the opioid-like G-protein coupled receptor, ORL1. In the present study, responses to intravenous injections of nociceptin were investigated in the systemic vascular bed of the rat. Nociceptin induced dose-related decreases in systemic arterial pressure and total peripheral resistance when injected in doses of 1-30 nmol/kg i.v.. Nociceptin decreased heart rate and in doses of 10 and 30 nmol/kg i.v., significantly decreased cardiac output. In terms of relative vasodilator activity, nociceptin was approximately 10-fold less potent than the beta-adrenergic receptor agonist isoproterenol. These data show that nociceptin has novel vasodilator activity in the systemic vascular bed of the rat.
十七肽孤啡肽，也被称为孤啡肽FQ，是一种新发现的类阿片G蛋白偶联受体ORL1的内源性配体。在本研究中，研究了大鼠全身血管床对静脉注射孤啡肽的反应。静脉注射剂量为1-30 nmol/kg时，孤啡肽可引起全身动脉压和总外周阻力呈剂量相关下降。孤啡肽可降低心率，静脉注射剂量为10和30 nmol/kg时，可显著降低心输出量。就相对血管舒张活性而言，孤啡肽的效力约为β-肾上腺素能受体激动剂异丙肾上腺素的十分之一。这些数据表明，孤啡肽在大鼠全身血管床具有新的血管舒张活性。
