Structure-activity Study of Endomorphins Analogs with C-terminal Substitution

doi:10.1016/j.proenv.2011.10.085

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	Structure-activity Study of Endomorphins Analogs with C-terminal Substitution
	Gong, P; Chen, FX; Wang, R; Wang, R (reprint author), Lanzhou Univ, Sch Basic Med Sci, Lanzhou 730000, Peoples R China.
	2011
会议日期	NOV 25-27, 2011
会议地点	Male, MALDIVES
关键词	Endomorphins Opioid Receptor 1 Phenylalanine 2 3 4-tet-rahydroisoquinoline-3-carboxylic Acid
卷号	8
DOI	10.1016/j.proenv.2011.10.085
页码	549-553
英文摘要	Aims: To further wonder the influence of C-terminal residues on the pharmacological activities. Methods: The in vitro and in vivo opioid activities of C-terminal substitution analogs [L-Tic 4] EM1 and [L-Tic 4] EM2 were investigated using radioligand binding assay, guinea pig ileum (GPI) assay, mouse vas deferens (MVD) assay, systemic arterial pressure (SAP) assay and tail-flick test. Results: Our data showed that the analogs produced a higher delta-opioid affinity but low mu-opioid affinity, dose-dependent but reduced analgesic activities and cardiovascular effect comparing with those of EMs. Moreover, these effects induced by the analogs can be inhibited by naloxone, indicating an opioid mechanism. Conclusion: These results provided suggestive evidences that the substitution of C-terminal residue may play an important role in the regulation of opioid affinities and pharmacological activities. (C) 2011 Published by Elsevier Ltd. Selection and/or peer-review under responsibility of the Asia-Pacific Chemical, Biological & Environmental Engineering Society (APCBEES)
会议录	2011 INTERNATIONAL CONFERENCE ON ENVIRONMENT SCIENCE AND BIOTECHNOLOGY (ICESB 2011)
会议录出版地	AMSTERDAM
学科主题	Biotechnology & Applied Microbiology ; Environmental Sciences & Ecology
语种	英语
ISSN号	1878-0296
WOS记录号	WOS:000312366100083
内容类型	会议论文
源URL	[http://ir.lzu.edu.cn/handle/262010/183009]
专题	基础医学院_会议论文
通讯作者	Wang, R (reprint author), Lanzhou Univ, Sch Basic Med Sci, Lanzhou 730000, Peoples R China.
推荐引用方式 GB/T 7714	Gong, P,Chen, FX,Wang, R,et al. Structure-activity Study of Endomorphins Analogs with C-terminal Substitution[C]. 见:. Male, MALDIVES. NOV 25-27, 2011.