Linked Life Data

16672569

Source:http://linkedlifedata.com/resource/pubmed/id/16672569

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2006-7-14
pubmed:abstractText
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 C2-substituted derivative salvinorinyl-2-propionate, and salvinorin B can act as kappa-opioid receptor agonists in vivo. We found that following intracerebroventricular injection over a dose range of 1 to 30 microg of both salvinorin A and salvinorinyl-2-propionate produces antinociception in wild-type mice but not in a novel strain of kappa-opioid receptor knockout mice. Moreover, both salvinorin A and salvinorinyl-2-propionate reduce rectal body temperature, similar to conventional kappa-opioid receptor agonists, in a genotype-dependent manner. In addition, we determined that salvinorin A has high affinity for kappa 1- but not kappa 2-opioid receptors, demonstrating selectivity for this receptor subclass. Finally, treatment over the same dose range with salvinorin B, which is inactive in vitro, produced neither antinociceptive nor hypothermic effects in wild-type mice. These data demonstrate that salvinorin A is the active component of S. divinorum, selective for kappa(1)-opioid receptors, and that salvinorin A and specific structurally related analogs produce behavioral effects that require the kappa-opioid receptor.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
318
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
641-8
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed-meshheading:16672569-Analgesics, pubmed-meshheading:16672569-Analgesics, Non-Narcotic, pubmed-meshheading:16672569-Animals, pubmed-meshheading:16672569-Body Temperature, pubmed-meshheading:16672569-Brain, pubmed-meshheading:16672569-Cell Line, pubmed-meshheading:16672569-Cloning, Molecular, pubmed-meshheading:16672569-DNA, Complementary, pubmed-meshheading:16672569-Diterpenes, pubmed-meshheading:16672569-Diterpenes, Clerodane, pubmed-meshheading:16672569-Dose-Response Relationship, Drug, pubmed-meshheading:16672569-Injections, Intravenous, pubmed-meshheading:16672569-Mice, pubmed-meshheading:16672569-Mice, Knockout, pubmed-meshheading:16672569-Mutation, pubmed-meshheading:16672569-Pain Measurement, pubmed-meshheading:16672569-Plant Leaves, pubmed-meshheading:16672569-Radioligand Assay, pubmed-meshheading:16672569-Receptors, Opioid, kappa, pubmed-meshheading:16672569-Salvia
pubmed:year
2006
pubmed:articleTitle
Antinociceptive and hypothermic effects of Salvinorin A are abolished in a novel strain of kappa-opioid receptor-1 knockout mice.
pubmed:affiliation
Department of Neuroscience and Cell Biology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS), 675 Hoes Lane, Piscataway, NJ 08854, USA.
pubmed:publicationType
Journal Article, In Vitro, Research Support, N.I.H., Extramural