Source:http://linkedlifedata.com/resource/pubmed/id/16286814
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
8
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| pubmed:dateCreated |
2005-11-15
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| pubmed:abstractText |
Salvinorin A is a pharmacologically active diterpene that occurs naturally in the Mexican mint Ska Maria Pastora (Salvia divinorum) and represents the first naturally occurring kappa-opioid receptor agonist. The chemical structure of salvinorin A is novel among the opioids, and thus defines a new structural class of kappa-opioid-receptor selective drugs. Few studies have examined the effects of salvinorin A in vivo, and fewer still have attempted to assess the agonist actions of this compound at mu-opioid, delta-opioid, and kappa-opioid receptors using selective antagonists. In the mouse, salvinorin A disrupted climbing behavior on an inverted screen task, indicating a rapid, but short-lived induction of sedation/motor incoordination. Similar effects were observed with the mu-agonist remifentanil and the synthetic kappa-agonist U69,593. When behaviorally equivalent doses of all three opioids were challenged with antagonists at doses selective for mu-opioid, delta-opioid, or kappa-opioid receptors, results suggested that the motoric effects of remifentanil were mediated by mu-receptors, whereas those of salvinorin A and U69,593 were mediated via kappa-receptors. Despite similar potencies and degrees of effectiveness, salvinorin A and U69,593 differed with regard to their susceptibility to antagonism by the kappa-antagonist nor-binaltorphamine. This later finding, coupled with the novel chemical structure of the compound, is consistent with recent findings that the diterpene salvinorin A may bind to the kappa-receptor in a manner that is qualitatively different from that of more traditional kappa-agonists such as the benzeneacetamide U69,593. Such pharmacological differences among these kappa-opioids raise the possibility that the development of other diterpene-based opioids may yield important therapeutic compounds.
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| pubmed:grant | |
| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Benzeneacetamides,
http://linkedlifedata.com/resource/pubmed/chemical/Diterpenes,
http://linkedlifedata.com/resource/pubmed/chemical/Diterpenes, Clerodane,
http://linkedlifedata.com/resource/pubmed/chemical/Hallucinogens,
http://linkedlifedata.com/resource/pubmed/chemical/Naloxone,
http://linkedlifedata.com/resource/pubmed/chemical/Naltrexone,
http://linkedlifedata.com/resource/pubmed/chemical/Narcotic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Psychotropic Drugs,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, delta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu,
http://linkedlifedata.com/resource/pubmed/chemical/U 69593,
http://linkedlifedata.com/resource/pubmed/chemical/naltrindole,
http://linkedlifedata.com/resource/pubmed/chemical/norbinaltorphimine,
http://linkedlifedata.com/resource/pubmed/chemical/remifentanil,
http://linkedlifedata.com/resource/pubmed/chemical/salvinorin A
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| pubmed:status |
MEDLINE
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| pubmed:month |
Dec
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| pubmed:issn |
0955-8810
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
16
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
627-33
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| pubmed:dateRevised |
2009-7-7
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| pubmed:meshHeading |
pubmed-meshheading:16286814-Analgesics, Opioid,
pubmed-meshheading:16286814-Animals,
pubmed-meshheading:16286814-Behavior, Animal,
pubmed-meshheading:16286814-Benzeneacetamides,
pubmed-meshheading:16286814-Diterpenes,
pubmed-meshheading:16286814-Diterpenes, Clerodane,
pubmed-meshheading:16286814-Hallucinogens,
pubmed-meshheading:16286814-Male,
pubmed-meshheading:16286814-Mice,
pubmed-meshheading:16286814-Naloxone,
pubmed-meshheading:16286814-Naltrexone,
pubmed-meshheading:16286814-Narcotic Antagonists,
pubmed-meshheading:16286814-Piperidines,
pubmed-meshheading:16286814-Psychotropic Drugs,
pubmed-meshheading:16286814-Pyrrolidines,
pubmed-meshheading:16286814-Receptors, Opioid, delta,
pubmed-meshheading:16286814-Receptors, Opioid, kappa,
pubmed-meshheading:16286814-Receptors, Opioid, mu
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| pubmed:year |
2005
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| pubmed:articleTitle |
Kappa-opioid receptor-mediated effects of the plant-derived hallucinogen, salvinorin A, on inverted screen performance in the mouse.
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| pubmed:affiliation |
Division of Neuroscience, Yerkes National Primate Research Center, Emory University, Atlanta, Georgia 30322, USA. wfanteg@emory.edu
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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