强效阿片受体活性肽双氢埃托啡的4,4'-残基修饰及构效关系研究

Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.

作者信息

Li G, Haq W, Xiang L, Lou B S, Hughes R, De Leon I A, Davis P, Gillespie T J, Romanowski M, Zhu X, Misicka A, Lipkowski A W, Porreca F, Davis T P, Yamamura H I, O'Brien D F, Hruby V J

机构信息

Department of Chemistry, University of Arizona, Tucson 85721, USA.

出版信息

Bioorg Med Chem Lett. 1998 Mar 3;8(5):555-60. doi: 10.1016/s0960-894x(98)00065-1.

DOI:10.1016/s0960-894x(98)00065-1

PMID:9871617

Abstract

Modifications of 4,4' residues of Biphalin have resulted in greater binding selectivity and biological potency for the mu opioid receptor. A higher partition coefficient across the phospholipid bilayer membrane has been achieved by using a beta-branched unusual amino acids.

摘要

对双啡肽4,4'残基的修饰已产生了对μ阿片受体更高的结合选择性和生物活性。通过使用β-支链的非常规氨基酸，已实现了跨磷脂双分子层膜更高的分配系数。