A review of salvinorin analogs and their kappa-opioid receptor activity

被引：45
|
作者：
Roach, Jeremy J. [1 ]
Shenvi, Ryan A. [1 ]
机构：
[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2018年 / 28卷 / 09期
关键词：
Salvinorin; Terpenoid; Opioid; GPCR; Kappa-opioid; SALVIA-DIVINORUM; IN-VITRO; NEOCLERODANE DITERPENES; A ANALOGS; BIOLOGICAL EVALUATION; HALLUCINOGEN SALVINORIN; BIASED AGONISM; FURAN RING; POTENT; LIGANDS;
D O I：
10.1016/j.bmcl.2018.03.029
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The plant metabolite salvinorin A potently and selectively agonizes the human kappa-opioid receptor, an emerging target for next-generation analgesics. Here we review analogs of the salvinorin chemotype and their effects on selectivity, affinity and potency. Extensive peripheral modifications using isolated salvinorin A have delivered a trove of SAR information. More deep-seated changes are now possible by advances in chemical synthesis. (C) 2018 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1436 / 1445
页数：10
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