Structure-activity relationship of endomorphins and their analogs |
| |
Authors: | Huo Xiaofeng Wu Ning Ren Weihua Wang Rui Albert S. C. Chan |
| |
Affiliation: | (1) Department of Biochemistry and Molecular Biology, School of Life Science, Lanzhou University, 730000 Lanzhou, China;(2) Department of Applied Biology and Chemical Technology, Hong Kong Polytechnic University, Hong Kong, China |
| |
Abstract: | To study the structure-activity relationship of endomorphins (EMs), the action of opioid receptor binding (AORB), analgesic activity and vasodilator effects of EMs and their eight analogs were investigated, which were prepared by rationally replacing the 2-/3-amino acid (Aa) of EMs. The results showed: i) The 2-Aa was comparatively more related to the selectivity of EMs while the 3-Aa to their affinity; ii) the analgesia and vasodilatation of EMs and their analogs were not completely dictated by their AORB (in vitro), the action of [D-Pro2]EM-2 was unusual; iii) EMs lost their analgesia in the central nervous system and their vasodilatation in the circulatory system with different mechanisms; the former was due to the degradation of some peptidase, and the latter possibly due to the feedback inhibition. |
| |
Keywords: | endomorphins structure-activity relationship action of opioid receptor binding analgesia vasodilatation mechanism of inactivation |
本文献已被 SpringerLink 等数据库收录! |
| 点击此处可从《科学通报(英文版)》浏览原始摘要信息 |
|
点击此处可从《科学通报(英文版)》下载免费的PDF全文 |