Endomorphin analogues with balanced affinity for bothμ- andδ-opioid receptors  

作　　者：Liang Zhang Lei Chang Lei Lei Yu Jin Chun Liu Jia Jia Chen Xiao Wen Li Lawrence H. Lazarus Ting You Li 

机构地区：[1]School of Pharmacy, Nanjing Medical University, Nanjing 210029, China [2]Medicinal Chemistry Group, Laboratory of Toxicology and Pharmacology, National Institute of Environmental Health Sciences, Research Triangle Park, NC 27709, USA

出　　处：《Chinese Chemical Letters》2011年第8期907-910,共4页中国化学快报（英文版）

基　　金：was supported by grants 08KJB350002 and 08NMUZ028;in part by the Intramural Research Program of the NIH and NIEHS

摘　　要：Analogues of endomorphin and tripeptidcs modified at positions 4 and 3,respectively,with various phenylalanine analogues were synthesized and their affinities for opioid receptors were evaluated.Most of the peptides exhibited potentμ-receptor affinity and selectivity,among them,compound 7（Dmt-Pro-Tmp-Tmp-NH_2） exhibited potent affinity for bothμ-andδ-receptors （K_iμ= 0.47 nmol/L,K_iδ= 1.63 nmol/L）.Analogues of endomorphin and tripeptidcs modified at positions 4 and 3,respectively,with various phenylalanine analogues were synthesized and their affinities for opioid receptors were evaluated.Most of the peptides exhibited potentμ-receptor affinity and selectivity,among them,compound 7（Dmt-Pro-Tmp-Tmp-NH_2） exhibited potent affinity for bothμ-andδ-receptors （K_iμ= 0.47 nmol/L,K_iδ= 1.63 nmol/L）.

关 键 词：ENDOMORPHIN OPIOID ANALGESICS 

分 类 号：Q432[生物学—生理学] Q426