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--- salvia_divinorum_epling_jativa [2015/08/01 10:34] – andreas
+++ salvia_divinorum_epling_jativa [2019/04/29 08:22] (aktuell) – andreas
@@ Zeile 12: / Zeile 12: @@
 [Salvia divinorum: The botany, ethnobotany, biochemistry and future of a Mexican mint., Marushia, R., 2002] [[http://www.cyjack.com/cognition/Salvia.pdf]]
-"The diterpene [[https://de.wikipedia.org/wiki/Salvinorine|salvinorin A]] from Salvia divinorum has recently been reported to be a high-affinity and selective κ-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 κ-opioid receptors expressed in human embryonic kidney-293 cells. Thus, salvinorin A, salvinorinyl-2-propionate, and salvinorinyl-2-heptanoate were found to be either full (salvinorin A) or partial (2-propionate, 2-heptanoate) agonists for inhibition of forskolin-stimulated cAMP production... 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 (U50488) or (trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl] benzeneacetamide methane-sulfonate hydrate (U69593) (two standard κ-opioid agonists) and similar in efficacy to dynorphin A (the naturally occurring peptide ligand for κ-opioid receptors). Salvinorin A thus represents the first known naturally occurring non-nitrogenous full agonist at κ-opioid receptors." \\
+{{:salvinorinab.jpg}}  [[https://de.wikipedia.org/wiki/Salvinorine|salvinorin A (R=OAc) and B (R=OH)]]
-[Salvinorin A, an active component of the hallucinogenic sage Salvia divinorum is a highly efficacious κ-opioid receptor agonist: structural and functional considerations., Chavkin, C., Sud, S., Jin, W., Stewart, J., Zjawiony, J.K., Siebert, D.J., Roth, B.L., Journal of Pharmacology and Experimental Therapeutics, 308(3), 2004, 1197-1203]
+"The diterpene salvinorin A from Salvia divinorum has recently been reported to be a high-affinity and selective κ-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 κ-opioid receptors expressed in human embryonic kidney-293 cells. Thus, salvinorin A, salvinorinyl-2-propionate, and salvinorinyl-2-heptanoate were found to be either full (salvinorin A) or partial (2-propionate, 2-heptanoate) agonists for inhibition of forskolin-stimulated cAMP production... 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 (U50488) or (trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl] benzeneacetamide methane-sulfonate hydrate (U69593) (two standard κ-opioid agonists) and similar in efficacy to dynorphin A (the naturally occurring peptide ligand for κ-opioid receptors). Salvinorin A thus represents the first known naturally occurring non-nitrogenous full agonist at κ-opioid receptors." \\
+[Salvinorin A, an active component of the hallucinogenic sage Salvia divinorum is a highly efficacious κ-opioid receptor agonist: structural and functional considerations., Chavkin, C., Sud, S., Jin, W., Stewart, J., Zjawiony, J.K., Siebert, D.J., Roth, B.L., Journal of Pharmacology and Experimental Therapeutics, 308(3), 2004, 1197-1203]
+"Salvinorin-A, the main psychoactive constituent in S. divinorum, is a non-nitrogenous neoclerodane diterpene with an affinity for the kappa opioid receptor (KOR; Roth et al., 2002). Despite its intense perception-modifying effects in humans, in vitro studies have shown that salvinorin-A does not bind to 5HT2A receptors, the molecular target of classic psychedelics like lysergic acid diethylamide (LSD), mescaline, psilocybin, and dimethyltryptamine (Roth et al., 2002; Prisinzano, 2005). ... \\
+Salvinorin-A led to a disconnection from external reality, induced elaborate visions and auditory phenomena, and modified interoception. The lower doses increased somatic sensations, but the highest dose led to a sense of a complete loss of contact with the body." \\
+[Maqueda, Ana Elda, et al. "Salvinorin-A induces intense dissociative effects, blocking external sensory perception and modulating interoception and sense of body ownership in humans." International Journal of Neuropsychopharmacology 18.12 (2015): pyv065.] [[https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4675976/]]