DARK Classics in Chemical Neuroscience: Salvinorin A.
ACS chemical neuroscience December 2, 2020 R Bruno Hernández-alvarado, Abraham Madariaga-Mazón, Alfredo Ortega et al. 29 citations
Salvinorin A, the main psychoactive compound in the plant Salvia divinorum, is the first known nonalkaloidal opioid that acts through the kappa-opioid receptor, producing rapid and short-lived hallucinogenic effects. Its unique chemical structure lacks a protonated amine group, leading to fast metabolism and swift loss of activity. The compound has been used ancestrally in spiritual rites by the Mazatec people of Oaxaca, Mexico, but its psychotropic effects have led to misuse and bans in many countries. This review covers its history, natural isolation, total synthesis, hundreds of synthetic analogues, and pharmacological and safety profiles, highlighting its impact on neuroscience and drug development.