Salvinorin A: a novel and highly selective kappa-opioid receptor agonist.

Salvinorin A, a natural hallucinogen, acts as a highly selective agonist at kappa-opioid receptors (KORs), which are the main site for dynorphin and related neuropeptides. This review summarizes the chemistry, pharmacology, and biology of salvinorin A. Because it profoundly alters consciousness and perception, studying how salvinorin A interacts with KORs may reveal new insights into the molecular and cellular basis of higher human cortical functions.

Study at a glance

Abstract

kappa-opioid receptors (KORs) represent the principal site of action of dynorphin and related neuropeptides. Recently, Salvinorin A--a naturally occurring neoclerodane diterpene hallucinogen was identified to be a highly selective KOR agonist. In this brief review we summarize the known chemistry, pharmacology and biology of salvinorin A. Because salvinorin A profoundly alters human consciousness and perception, a study of how salvinorin A exerts its actions on KORs may yield novel insights into the molecular and cellular basis of uniquely human higher cortical functions.