This review (2020) discusses the history, chemistry, pharmacology, and other aspects of salvinorin A, the main bioactive compound in the drug Salvia divinorum.

Abstract of DARK Classics in Chemical Neuroscience: Salvinorin A

“Salvinorin A is the main bioactive compound in Salvia divinorum, an endemic plant with ancestral use by the inhabitants of the Mazateca mountain range (Sierra Mazateca) in Oaxaca, México. The main use of la pastora, as locally known, is in spiritual rites due to its extraordinary hallucinogenic effects. Being the first known nonalkaloidal opioid-mediated psychotropic molecule, salvinorin A set new research areas in neuroscience. The absence of a protonated amine group, common to all previously known opioids, results in a fast metabolism with the concomitant fast elimination and swift loss of activity. The worldwide spread and psychotropic effects of salvinorin A account for its misuse and classification as a drug of abuse. Consequently, salvinorin A and Salvia divinorum are now banned in many countries. Several synthetic efforts have been focused on the improvement of physicochemical and biological properties of salvinorin A: from total synthesis to hundreds of analogues. In this Review, we discuss the impact of salvinorin A in chemistry and neuroscience covering the historical relevance, isolation from natural sources, synthetic efforts, and pharmacological and safety profiles. Altogether, the chemistry behind and the taboo that encloses salvinorin A makes it one of the most exquisite naturally occurring drugs.”

Authors: R. Bruno Hernández-Alvarado, Abraham Madariaga-Mazón, Alfredo Ortega & Karina Martinez-Mayorga

Summary of DARK Classics in Chemical Neuroscience: Salvinorin A

Introduction and Historical Relevance

Salvia divinorum is a plant from the mint family (Labiatae) that was discovered in 1957 by Gomez-Pompa. Later, Gordon-Wasson and Hofmann obtained enough flowered herbarium material at San Jose Tenango to complete the description and classification of the plant.

Salvia divinorum, described as a perennial herb, grows in large clones to over one meter in height. It is used by Mazatec shamans for divinatory purposes to identify an illness or even to find out a guilty person of a robbery.

Salvinorin A was isolated from dried leaves of Salvia divinorum and found to be a potent agonist of the kappa opioid receptor. It lacks an aminergic functional group, making it the first naturally occurring, nonaminergic, selective KOR agonist.

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DARK Classics in Chemical Neuroscience: Salvinorin A

https://doi.org/10.1021/acschemneuro.0c00608

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Cite this paper (APA)

Hernández-Alvarado, R. B., Madariaga-Mazón, A., Ortega, A., & Martinez-Mayorga, K. (2020). DARK classics in chemical neuroscience: salvinorin A. ACS Chemical Neuroscience, 11(23), 3979-3992.

Study details

Compounds studied
Salvia Divinorum

Topics studied
Chemistry

Study characteristics
Literature Review