In vitro stability and metabolism of salvinorin A in rat plasma.
Kenji Tsujikawa, Kenji Kuwayama, Hajime Miyaguchi, Tatsuyuki Kanamori, Yuko T Iwata, H Inoue
Xenobiotica May 1, 2009 DOI: 10.1080/00498250902769967 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Observational study Peer reviewed |
|---|---|
| Population | Rat plasma |
| Topics | Salvia divinorum |
| Keywords | Potent natural compound This compound Drug metabolism Break down Rapid degradation Efficiently metabolizes Enzymes Carboxylesterase Lactonase Key players Salvinorin b Distinct breakdown products Pharmacokinetics Pharmacology Stability in plasma |
| Citations | 64 |
| Key findings | Carboxylesterase is the main enzyme responsible for salvinorin A hydrolysis in rat plasma, producing salvinorin B and lactone-ring-open forms. |
Abstract
Salvinorin A is the main active psychoactive ingredient in Salvia divinorum, a Mexican plant that has been widely available as a hallucinogen in recent years. The aims of this study were to investigate the stability of salvinorin A in rat plasma, esterases responsible for its degradation, and estimation of the degradation products. The apparent first-order rate constants of salvinorin A at 37 degrees C, 25 degrees C, and 4 degrees C were 3.8 x 10(-1), 1.1 x 10(-1), and < 6.0 x 10(-3) h(-1), respectively. Salvinorin A degradation was markedly inhibited by the addition of sodium fluoride, an esterase inhibitor. Moreover, phenylmethylsulfonyl fluoride (serine esterase inhibitor) and bis-p-nitrophenylphosphate (carboxylesterase inhibitor) also inhibited salvinorin A degradation. In contrast, little or no suppression of the degradation was seen with 5,5'-dithiobis-2-nitrobenzoic acid (arylesterase inhibitor),ethopropazine (butyrylcholinesterase inhibitor), and BW284c51 (acetylcholineseterase inhibitor). These findings indicated that carboxylesterase was mainly involved in the salvinorin A hydrolysis in rat plasma.4. The degradation products of salvinorin A estimated by liquid chromatography-mass spectrometry included the deacetylated form (salvinorin B) and the lactone-ring-open forms of salvinorin A and salvinorin B. This lactone-ring-opening reactions were involved in calcium-dependent lactonase.
Comparable studies
Other observational and cohort studies on salvia divinorum, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Pharmacokinetics of the potent hallucinogen, salvinorin A in primates parallels the rapid onset and short duration of effects in humans. Adult female baboons | 2008 | Observational cohort | n = 6 |
| Salvia divinorum: effects and use among YouTube users. YouTube video posters using salvia | 2010 | Observational study using video analysis | n = 34 |
| Salvia divinorum: exposures reported to a statewide poison control system over 10 years. Exposures to Salvia divinorum reported to the California Poison Control System | 2011 | Retrospective review | n = 37 |
| Time course of pharmacokinetic and hormonal effects of inhaled high-dose salvinorin A in humans. Healthy adults | 2016 | Observational study | n = 6 |
| A Content Analysis of Salvia Divinorum Use on YouTube Users who posted videos of themselves using Salvia divinorum on YouTube | 2013 | Observational study |
Citations in the library
Cited by 18
- Here today, gone tomorrow…and back again? A review of herbal marijuana alternatives (K2, Spice), synthetic cathinones (bath salts), kratom, Salvia divinorum, methoxetamine, and piperazines. Journal of Medical Toxicology March 1, 2012
- Neuropharmacology of the naturally occurring kappa-opioid hallucinogen salvinorin A. Pharmacological Reviews June 1, 2011
- From local to global-fifty years of research on Salvia divinorum. Journal of Ethnopharmacology February 3, 2014
- Pharmacokinetics and Pharmacodynamics of Salvinorin A and Salvia divinorum: Clinical and Forensic Aspects Pharmaceuticals February 3, 2021
- Salvia divinorum: from Mazatec medicinal and hallucinogenic plant to emerging recreational drug. Human Psychopharmacology: Clinical and Experimental September 1, 2013
and 13 more in the library
Cites 7
- Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. Proceedings of the National Academy of Sciences September 3, 2002
- Salvinorin A, an active component of the hallucinogenic sage salvia divinorum is a highly efficacious kappa-opioid receptor agonist: structural and functional considerations. Journal of Pharmacology and Experimental Therapeutics March 1, 2004
- Ethnopharmacology of ska María Pastora (Salvia divinorum, Epling and Játiva-M.). Journal of Ethnopharmacology May 1, 1983
- Salvia divinorum and the unique diterpene hallucinogen, Salvinorin (divinorin) A. Journal of Psychoactive Drugs 1994
- The plant-derived hallucinogen, salvinorin A, produces kappa-opioid agonist-like discriminative effects in rhesus monkeys. Psychopharmacology March 1, 2004
and 2 more in the library