Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues

被引：30

作者：

Lee, DYW

He, MS

Kondaveti, L

Liu-Chen, LY

Ma, ZZ

Wang, YL

Chen, Y

Li, JG

Beguin, C

Carlezon, WA

Cohen, B

机构：

[1] Harvard Univ, McLean Hosp, Mol Pharmacol Lab, Belmont, MA 02478 USA

[2] Harvard Univ, McLean Hosp, Sch Med, Bioorgan & Nat Prod Lab, Belmont, MA 02478 USA

[3] Temple Univ, Sch Med, Dept Pharmacol, Philadelphia, PA 19140 USA

[4] Harvard Univ, McLean Hosp, Sch Med, Behav Genet Lab, Belmont, MA 02478 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 19期

关键词：

in vitro; salvinorin A; kappa-opioid receptor; agonist; neoclerodane diterpene;

D O I：

10.1016/j.bmcl.2005.06.092

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Salvinorin A is the most potent naturally occurring opioid agonist with a high selectivity and affinity for kappa-opioid receptor. To explore its structure-activity relationships, modifications at the C(4) position have been studied and a series of salvinorin A derivatives were prepared. These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human kappa-opioid receptor and several potent new agonists have been identified. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：4169 / 4173

页数：5

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