Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues.
Journal of medicinal chemistry December 26, 2014 Andrew P Riley, Chad E Groer, David Young et al. 115 citations
Salvinorin A, a compound from the leaves of Salvia divinorum, activates κ-opioid receptors and could be a basis for treating substance abuse. Researchers synthesized several derivatives with modified furan rings to better understand how this part of the molecule binds to the receptor. Functional assays showed that smaller substitutions are preferred, indicating the furan ring fits into a tight part of the binding pocket. The most potent analogue reduced drug-seeking behavior in an animal model of relapse without causing sedation, a common side effect of other κ-opioid agonists.