Salvinorin A analogs as probes in opioid pharmacology.
نویسندگان
چکیده
3.1. Other Salvinorins 1735 3.2. Role of the 2-Position Acetyl Group 1735 3.2.1. Ester Modifications 1735 3.2.2. Carbamate and Carbonate Analogs 1737 3.2.3. Ether and Amine Analogs 1737 3.2.4. Amides and Thioesters 1738 3.2.5. Sulfonyl Esters 1738 3.3. Other A Ring Changes 1738 3.4. Role of the 4-Position Carbomethoxy Group 1739 3.5. Role of the 17-Position Carbonyl 1739 3.6. Role of the Furan Ring 1740 3.7. Total Synthesis Efforts 1740 4. Studies on the Mode of Binding of Salvinorin A 1740
منابع مشابه
Antinociceptive and hypothermic effects of Salvinorin A are abolished in a novel strain of kappa-opioid receptor-1 knockout mice.
Salvia divinorum is a natural occurring hallucinogen that is traditionally used by the Mazatec Indians of central Mexico. The diterpene salvinorin A was identified as an active component of S. divinorum over 20 years ago, but only recently has biochemical screening indicated that a molecular target of salvinorin A in vitro is the kappa-opioid receptor. We have examined whether salvinorin A, the...
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Salvinorin A is a potent hallucinogen, isolated from the ethnomedical plant Salvia divinorum. Salvinorin A is a selective high efficacy kappa-opioid receptor (KOPr) agonist, and thus implicates the KOPr system and its endogenous agonist ligands (the dynorphins) in higher functions, including cognition and perceptual effects. Salvinorin A is the only selective KOPr ligand to be widely available ...
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Novel semisynthetic analogs of salvinorin A, a full agonist having extraordinary affinity as well as selectivity for the κ-opioid receptor (KOR), were obtained in good yields. The derivatives are remarkable for their unusual and unique hemiacetal structure in the salvinorin series of compounds. The formation of the hemiacetal occurs with epimerization at C-12, thus preserving the original confi...
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Salvia divinorum is a hallucinogenic plant used by the Mazatec Indians of Mexico for traditional spiritual ceremonies. The active constituent, salvinorin A, induces profound hallucinations, however the biological mechanism for this action is not known. Affinity-binding studies suggest that the biologic activity of salvinorin A involves the kappa-opioid receptor. The purpose of this study was to...
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Previous structure-activity relationship studies of salvinorin A have shown that modification of the acetate functionality off the C-2 position to a methoxy methyl or methoxy ethyl ether moiety leads to increased potency at KOP receptors. However, the reason for this increase remains unclear. Here we report our efforts towards the synthesis and evaluation of C-2 constrained analogs of salvinori...
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ورودعنوان ژورنال:
- Chemical reviews
دوره 108 5 شماره
صفحات -
تاریخ انتشار 2008