Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/33144
Title: Structure-activity relationship of endomorphins and their analogs
Authors: Huo, X
Wu, N
Ren, W
Wang, R
Chan, ASC
Keywords: Action of opioid receptor binding
Analgesia
Endomorphins
Mechanism of inactivation
Structure-activity relationship
Vasodilatation
Issue Date: 2001
Publisher: Chinese Academy of Sciences
Source: Chinese science bulletin (科學通報. 英文版), v. 46, no. 13, p. 1096-1100 How to cite?
Journal: Chinese science bulletin (科學通報. 英文版) 
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-Pro 2]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.
URI: http://hdl.handle.net/10397/33144
ISSN: 1001-6538
EISSN: 1861-9541
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