Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
Bioorganic & Medicinal Chemistry Letters June 1, 2005
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
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Bioorganic & Medicinal Chemistry Letters June 1, 2005
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
Psychopharmacology May 1, 2005 Yong Zhang, Eduardo R Butelman, Stefan D Schlussman et al. 198 citations
Salvinorin A is a naturally occurring hallucinogen derived from the plant Salvia divinorum. Salvinorin A is also a potent and selective kappa opioid receptor agonist in vitro. It has been shown that kappa agonists decrease dopamine levels in the caudate putamen and nucleus accumbens and cause conditioned place aversion in rodents. To study the effects of salvinorin A on basal dopamine levels in...
Journal of Medicinal Chemistry January 27, 2005 Thomas A Munro, Mark A Rizzacasa, Bryan L. Roth et al.
Salvinorin A (1), from the sage Salvia divinorum, is a potent and selective kappa opioid receptor (KOR) agonist. We screened other salvinorins and derivatives for binding affinity and functional activity at opioid receptors. Our results suggest that the methyl ester and furan ring are required for activity but that the lactone and ketone functionalities are not. Other salvinorins showed...
ChemInform January 25, 2005 Kevin Tidgewell, Wayne W Harding, Mark S Schmidt et al.
Abstract: For Abstract see ChemInform Abstract in Full Text.
Pharmacopsychiatry 2005 R Bücheler, C H Gleiter, P Schwoerer et al. 63 citations
: We want to call attention to a mint plant, called diviner's sage ( Salvia divinorum), originally used in shamanic ceremonies of the Mazatec Indians of Mexico. On numerous websites of the internet, this ancient herbal drug and its extracts are offered as a legal means of widening individual awareness. Regarding its dose-response relationship, the active ingredient, salvinorin A, is one of the...
Bioorganic & Medicinal Chemistry Letters October 18, 2004 Kevin Tidgewell, Wayne W Harding, Mark S Schmidt et al. 68 citations
Salvinorin A is a novel hallucinogen isolated from the widely available leaves of Salvia divinorum. Based on its mechanism of action, salvinorin A has shown potential as a stimulant abuse therapeutic. However, there are no methods for the detection of salvinorin A or its metabolites in biological fluids. In order to begin developing salvinorin A as a potential therapeutic, an understanding of...
Life Sciences October 15, 2004 Feng Yan, Bryan L. Roth 68 citations
kappa-opioid receptors (KORs) represent the principal site of action of dynorphin and related neuropeptides. Recently, Salvinorin A--a naturally occurring neoclerodane diterpene hallucinogen was identified to be a highly selective KOR agonist. In this brief review we summarize the known chemistry, pharmacology and biology of salvinorin A. Because salvinorin A profoundly alters human...
Annals of botany June 2004 Daniel J Siebert
Salvia divinorum produces several closely related neoclerodane diterpenes. The most abundant of these, salvinorin A, is responsible for the psychoactive properties of the plant. To determine where these compounds occur in the plant, various organs, tissues and glandular secretions were chemically analysed. A microscopic survey of the S. divinorum plant was performed to examine the various types...
Psychopharmacology March 1, 2004 Eduardo R Butelman, Todd J Harris, Mary Jeanne Kreek 102 citations
Salvinorin A is the active component of the hallucinogenic plant Salvia divinorum. The potential mode of action of this hallucinogen was unknown until recently. A recent in vitro study detected high affinity and efficacy of salvinorin A at kappa-opioid receptors. It was postulated that salvinorin A would produce discriminative stimulus effects similar to those of a high efficacy kappa-agonist...
Journal of Pharmacology and Experimental Therapeutics March 1, 2004 Charles Chavkin, Sumit Sud, Wenzhen Jin et al. 212 citations
The diterpene salvinorin A from Salvia divinorum has recently been reported to be a high-affinity and selective kappa-opioid receptor agonist (Roth et al., 2002). Salvinorin A and selected derivatives were found to be potent and efficacious agonists in several measures of agonist activity using cloned human kappa-opioid receptors expressed in human embryonic kidney-293 cells. Thus, salvinorin...