期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 9, 页码 1436-1445出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.03.029
关键词
Salvinorin; Terpenoid; Opioid; GPCR; Kappa-opioid
资金
- NIH [R35 GM122606]
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.
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