Pharmacology and anti-addiction effects of the novel κ opioid receptor agonist Mesyl Sal B, a potent and long-acting analogue of salvinorin A.
British journal of pharmacology January 1, 2015 B Simonson, A S Morani, A W M Ewald et al.
A synthetic version of salvinorin A, Mesyl Sal B, activates κ opioid receptors and shows potential as an anticocaine agent with fewer adverse effects than classic κ agonists. In rats, Mesyl Sal B had a longer duration of action than salvinorin A, reduced cocaine-seeking behavior, and increased dopamine transporter function in vitro through a κ opioid receptor- and ERK1/2-dependent mechanism. Unlike salvinorin A, Mesyl Sal B raised the maximum rate of dopamine uptake without increasing transporter cell-surface expression. The findings suggest that salvinorin-based compounds like Mesyl Sal B warrant further study as treatments for cocaine addiction, though their side-effect profile requires additional investigation.