Salvadori S, Picone D, Tancredi T, Guerrini R, Spadaccini R, Lazarus L H, Regoli D, Temussi P A
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
Biochem Biophys Res Commun. 1997 Apr 28;233(3):640-3. doi: 10.1006/bbrc.1997.6285.
Nociceptin, a novel heptadecapeptide, interacts with ORL1 a G protein-coupled receptor whose sequence is closely related to that of the kappa opioid receptor but has no opioid activity. We have investigated the conformational preferences of Nociceptin also in comparison to Dynorphin A. The N-terminal part of Nociceptin has the same conformational preferences of the message of endogenous opioids but the C-terminal part of the sequence is more flexible than the corresponding address of Dynorphin A. [Tyr1]-Nociceptin, while retaining nociceptive activity, has also an opioid activity comparable to that of enkephalins.
痛敏肽是一种新型十七肽，它与孤儿受体1（ORL1）相互作用，ORL1是一种G蛋白偶联受体，其序列与κ阿片受体密切相关，但无阿片样活性。我们还与强啡肽A比较研究了痛敏肽的构象偏好。痛敏肽的N端部分具有与内源性阿片样物质信息相同的构象偏好，但该序列的C端部分比强啡肽A的相应区域更具灵活性。[酪氨酸1] - 痛敏肽在保留伤害感受活性的同时，还具有与脑啡肽相当的阿片样活性。
