| Literature DB >> 29615341 |
Jeremy J Roach1, Ryan A Shenvi2.
Abstract
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.Entities:
Keywords: GPCR; Kappa-opioid; Opioid; Salvinorin; Terpenoid
Mesh:
Substances:
Year: 2018 PMID: 29615341 PMCID: PMC5912166 DOI: 10.1016/j.bmcl.2018.03.029
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823