新克罗烷二萜类化合物作为μ阿片受体配体的新型骨架。

Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.

作者信息

Harding Wayne W, Tidgewell Kevin, Byrd Nathan, Cobb Howard, Dersch Christina M, Butelman Eduardo R, Rothman Richard B, Prisinzano Thomas E

机构信息

Division of Medicinal & Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA.

出版信息

J Med Chem. 2005 Jul 28;48(15):4765-71. doi: 10.1021/jm048963m.

DOI:10.1021/jm048963m

PMID:16033256

Abstract

Structural modification of salvinorin A, the active component of Salvia divinorum, has resulted in the synthesis of novel neoclerodane diterpenes with opioid receptor affinity and activity. We report in this study a nonnitrogenous neoclerodane diterpene with mu opioid receptor affinity (13) that is an agonist at mu opioid receptors. This represents the identification of a novel structural class of mu opioid receptor agonists.

摘要

鼠尾草属植物（Salvia divinorum）的活性成分二萜内酯（salvinorin A）的结构修饰，已导致合成出具有阿片受体亲和力和活性的新型新克罗烷二萜。我们在本研究中报告了一种具有μ阿片受体亲和力的非含氮新克罗烷二萜（13），它是μ阿片受体的激动剂。这代表了一种新型μ阿片受体激动剂结构类别的鉴定。