Larua M. Bohn

O6C-20-nor-SalA is a stable and potent KOR agonist

ChemRxiv December 27, 2017 Ryan A Shenvi, Shun Hirasawa, Min Cho et al. 1 citation preprint

Salvinorin A (SalA) is a potent and selective agonist of the kappa-opioid receptor (KOR), but its instability has frustrated medicinal chemistry efforts. Treatment of SalA with weak bases like DBU leads to C8 epimerization with loss of receptor affinity and signaling potency. Here we show that replacement of C20 with H and replacement of O6 with CH2 stabilizes the SalA scaffold relative to its...