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

页码：1436 / 1445

页数：10

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