Giuliani S, Maggi C A
Pharmacology Department, Menarini Ricerche, Florence, Italy.
Br J Pharmacol. 1996 Aug;118(7):1567-9. doi: 10.1111/j.1476-5381.1996.tb15576.x.
The novel heptadecapeptide opioid, nociceptin, produced a concentration-dependent (EC50 28 nM) suppression of the inotropic response of the guinea-pig isolated renal pelvis to electrical stimulation, a response mediated by release of tachykinins from sensory nerves. Nociceptin did not affect the response to neurokinin A, indicating a prejunctional site of action on tachykininergic nerves. The effect of nociceptin was unchanged in the presence of the mu, delta and kappa opioid receptor antagonists, naloxone, naltrindole and nor-binaltorphimine.
新型十七肽阿片样物质——孤啡肽,对豚鼠离体肾盂对电刺激的变力反应产生浓度依赖性(半数有效浓度为28 nM)抑制作用,该反应由感觉神经释放速激肽介导。孤啡肽不影响对神经激肽A的反应,表明其作用于速激肽能神经的节前位点。在μ、δ和κ阿片受体拮抗剂纳洛酮、纳曲吲哚和去甲双丙戊酰吗啡存在的情况下,孤啡肽的作用不变。