• Corpus ID: 19673617

Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.

  title={Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.},
  author={Bryan L. Roth and Karen Baner and Richard B. Westkaemper and Daniel J. Siebert and Kenner C. Rice and SeAnna Steinberg and Paul R Ernsberger and Richard B. Rothman},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  volume={99 18},
  • B. Roth, K. Baner, R. Rothman
  • Published 2002
  • Biology, Psychology
  • Proceedings of the National Academy of Sciences of the United States of America
Salvia divinorum, whose main active ingredient is the neoclerodane diterpene Salvinorin A, is a hallucinogenic plant in the mint family that has been used in traditional spiritual practices for its psychoactive properties by the Mazatecs of Oaxaca, Mexico. More recently, S. divinorum extracts and Salvinorin A have become more widely used in the U.S. as legal hallucinogens. We discovered that Salvinorin A potently and selectively inhibited (3)H-bremazocine binding to cloned kappa opioid… 

Neuropharmacology of the Naturally Occurring κ-Opioid Hallucinogen Salvinorin A

Salvinorin A has therapeutic potential as a treatment for pain, mood and personality disorders, substance abuse, and gastrointestinal disturbances, and suggests that nonalkaloids are potential scaffolds for drug development for aminergic G-protein coupled receptors.

Salvinorin A, an Active Component of the Hallucinogenic Sage Salvia divinorum Is a Highly Efficacious κ-Opioid Receptor Agonist: Structural and Functional Considerations

Salvinorin A was found to be a full agonist, being significantly more efficacious than (trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl] benzeneacetamide methane-sulfonate hydrate (U69593) and similar in efficacy to dynorphin A (the naturally occurring peptide ligand for κ-opioid receptors).

The antinociceptive effect of salvinorin A in mice.

Kappa opioid mediation of cannabinoid effects of the potent hallucinogen, salvinorin A, in rodents

These findings suggest that similarities in the pharmacological effects of salvinorin A and those of cannabinoids are mediated by its activation of KOR rather than by any direct action of salvia divinorum A on the endocannabinoid system.

Salvia divinorum: from recreational hallucinogenic use to analgesic and anti-inflammatory action

The role of S. divinorum, SA and its analogues is explored, mainly on their analgesic and anti-inflammatory roles but also mention their psychoactive properties.

Kappa-opioid receptor-mediated effects of the plant-derived hallucinogen, salvinorin A, on inverted screen performance in the mouse

In the mouse, salvinorin A disrupted climbing behavior on an inverted screen task, indicating a rapid, but short-lived induction of sedation/motor incoordination and the possibility that the development of other diterpene-based opioids may yield important therapeutic compounds.

Evaluation of the transport, in vitro metabolism and pharmacokinetics of Salvinorin A, a potent hallucinogen.

  • Z. S. TeksinI. Lee N. Eddington
  • Biology, Medicine
    European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
  • 2009

The discriminative effects of the κ-opioid hallucinogen salvinorin A in nonhuman primates: dissociation from classic hallucinogen effects

These findings support the conclusion that the interoceptive/discriminative cue produced by salvinorin A is mediated by agonism at κ-receptors and is mechanistically distinct from that produced by a classic serotonergic hallucinogen.