Champion H C, Wang R, Hellstrom W J, Kadowitz P J
Department of Pharmacology, Tulane University School of Medicine, New Orleans, Louisiana 70112, USA.
Am J Physiol. 1997 Jul;273(1 Pt 1):E214-9. doi: 10.1152/ajpendo.1997.273.1.E214.
The heptadecapeptide nociceptin, also known as orphanin FQ, is a newly discovered endogenous ligand for the opioid-like G protein-coupled receptor ORL1. The present study was undertaken to investigate the effects of intracavernosal injections of nociceptin on penile erection in anesthetized cats. Responses to nociception were compared with erectile responses elicited by intracavernosal injection of vasoactive intestinal polypeptide (VIP), adrenomedullin (ADM), the novel nitric oxide donor diethylaminenitric oxide complex sodium (DEA/NO), and the control triple-drug combination (papaverine, phentolamine, and prostaglandin E1). The order of potency was VIP > ADM > nociceptin > DEA/NO. Intracavernosal injections of nociceptin in doses of 0.3-30 nmol elicited dose-related increases in cavernosal pressure and penile length that were comparable to those induced by the triple-drug combination, which is used in the treatment of erectile dysfunction. The response to nociceptin was rapid in onset, and the duration of the peak pressure increase and total response was significantly shorter than the response to the control triple-drug combination but longer in duration than responses to VIP and ADM. Intracavernosal injection of the triple-drug combination resulted in a greater decrease in mean systemic arterial blood pressure than did nociceptin. These data demonstrate that intracavernosal injection of this novel endogenous ligand for the ORL1 receptor induces a potent and relatively long-lasting erectile response in the cat.
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。本研究旨在探讨海绵体内注射孤啡肽对麻醉猫阴茎勃起的影响。将对伤害性刺激的反应与海绵体内注射血管活性肠肽（VIP）、肾上腺髓质素（ADM）、新型一氧化氮供体二乙胺一氧化氮复合物钠（DEA/NO）以及对照三联药物组合（罂粟碱、酚妥拉明和前列腺素E1）所引发的勃起反应进行比较。效力顺序为VIP > ADM > 孤啡肽 > DEA/NO。海绵体内注射剂量为0.3 - 30 nmol的孤啡肽会引起海绵体压力和阴茎长度与剂量相关的增加，这与用于治疗勃起功能障碍的三联药物组合所诱导的增加相当。对孤啡肽的反应起效迅速，峰值压力增加和总反应的持续时间明显短于对对照三联药物组合的反应，但长于对VIP和ADM的反应。海绵体内注射三联药物组合导致的平均体循环动脉血压下降幅度大于孤啡肽。这些数据表明，海绵体内注射这种针对ORL1受体的新型内源性配体可在猫体内诱导出强效且相对持久的勃起反应。
