Journal of molecular graphics & modelling
April 1, 2010
Donna L Mcgovern, Philip D Mosier, Bryan L. Roth et al.
16 citations
The highly potent and kappa-opioid (KOP) receptor-selective hallucinogen Salvinorin A and selected analogs have been analyzed using the 3D quantitative structure-affinity relationship technique Comparative Molecular Field Analysis (CoMFA) in an effort to derive a statistically significant and predictive model of salvinorin affinity at the KOP receptor and to provide additional statistical...
Pharmacology, Biochemistry, and Behavior
December 1, 2009
Aashish S Morani, Bronwyn M Kivell, Thomas E Prisinzano et al.
91 citations
Our previous work indicated that pretreatment with the selective kappa-opioid receptor (KOPr) agonist, U69593, attenuated the ability of priming injections of cocaine to reinstate extinguished cocaine-seeking behavior. The present study expanded these initial tests to include other traditional KOPr agonists, U50488H, spiradoline (SPR), and salvinorin A (Sal A), an active constituent of the...
Pharmaceutical Biology
October 19, 2009
Lukasz Kutrzeba, Vardan T. Karamyan, Robert C. Speth et al.
16 citations
Microbial transformation of natural products is a well established model for mammalian metabolism. Salvinorin A, a diterpenoid isolated from the hallucinogenic mint Salvia divinorum Epling & Játiva-M (Lamiaceae), is a potent non-nitrogenous κ-opioid receptor agonist. The metabolism of salvinorin A has still not yet been well established. Thirty fungal species were screened for the ability to...
Organic & Biomolecular Chemistry
September 21, 2009
Denise S Simpson, Kimberly M Lovell, Anthony Lozama et al.
Further synthetic modification of the furan ring of salvinorin A (1), the major active component of Salvia divinorum, has resulted in novel neoclerodane diterpenes with opioid receptor affinity and activity. A computational study has predicted 1 to be a reproductive toxicant in mammals and is suggestive that use of 1 may be associated with adverse effects. We report in this study that...
Neuropharmacology
September 2009
Jacob M Hooker, Thomas A Munro, Cécile Béguin et al.
Salvinorin A (SA) is a potent kappa opioid agonist with a brief duration of action. Consistent with this, our previous positron emission tomography (PET) studies of carbon-11 labeled SA showed that brain levels decrease rapidly after intravenous administration. SA is rapidly metabolized, giving the much less potent salvinorin B (SB), which is presumed to be responsible in part for SA's brief...
Journal of Psychoactive Drugs
September 1, 2009
Dawn N Albertson, Laura E Grubbs
29 citations
Salvia divinorum is a naturally occurring psychedelic considered to be one of the most potent hallucinogens found to date. The few behavioral studies conducted conclude that Salvia's effects may be similar to traditional psychedelics, which is noteworthy because Salvia acts via a unique molecular mechanism as a kappa opioid receptor agonist. One hundred and ninety-three participants, including...
Synapse
August 1, 2009
Philip Seeman, Hong-Chang Guan, Hélène Hirbec
83 citations
Although it is commonly stated that phencyclidine is an antagonist at ionotropic glutamate receptors, there has been little measure of its potency on other receptors in brain tissue. Although we previously reported that phencyclidine stimulated cloned-dopamine D2Long and D2Short receptors, others reported that phencyclidine did not stimulate D2 receptors in homogenates of rat brain striatum....
Biochemistry
July 28, 2009
Feng Yan, Ruslan V Bikbulatov, Viorel Mocanu et al.
81 citations
Salvinorin A, the most potent naturally occurring hallucinogen, has attracted an increasing amount of attention since the kappa-opioid receptor (KOR) was identified as its principal molecular target by us [Roth, B. L., et al. (2002) Proc. Natl. Acad. Sci. U.S.A. 99, 11934-11939]. Here we report the design, synthesis, and biochemical characterization of novel, irreversible, salvinorin A-derived...
American Journal of Psychiatry
July 1, 2009
Persistent psychosis associated with salvia divinorum use.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
June 1, 2009
Zeynep S Teksin, Insong J. Lee, Noble N Nemieboka et al.
76 citations
Salvinorin A is an unregulated potent hallucinogen isolated from the leaves of Salvia divinorum. It is the only known non-nitrogenous kappa-opioid selective agonist, and rivals synthetic lysergic acid diethylamide (LSD) in potency. The objective of this study was to characterize the in vitro transport, in vitro metabolism, and pharmacokinetic properties of Salvinorin A. The transport...