Source:http://linkedlifedata.com/resource/pubmed/id/10640294
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2000-2-22
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pubmed:abstractText |
Two highly selective mu-opioid receptor agonists, endomorphin-1 and endomorphin-2, have been identified and postulated to be endogenous mu-opioid receptor ligands. We determined the antinociceptive effects of these two ligands at the supraspinal level in mice with the tail-flick and hot-plate responses. The i.c.v. injection of endomorphin-1 and -2 inhibited the tail-flick and hot-plate responses in a dose-dependent manner. The endomorphin-1 was found to be 3.3- and 2.4-fold more potent than endomorphin-2 in inhibiting the tail-flick and hot-plate responses, respectively. The antinociception induced by endomorphin-1 was blocked by i.c.v. pretreatment with the mu-opioid receptor antagonist beta-funaltrexamine but not by the kappa-opioid receptor antagonist nor-binaltorphimine, the delta(1)-opioid antagonist 7-benzylidene naltrexamine, or the delta(2)-opioid receptor antagonist naltriben. In contrast, the antinociception induced by endomorphin-2 was blocked by i.c.v. pretreatment with beta-funaltrexamine or nor-binaltorphimine but not by 7-benzylidene naltrexamine or naltriben. The inhibition of the tail-flick response induced by endomorphin-2 was blocked by pretreatment with an antiserum against dynorphin A(1-17) but not by antisera against Met-enkephalin, Leu-enkephalin, or beta-endorphin. None of these antisera reduced the endomorphin-1-induced tail-flick inhibition. We propose that endomorphin-1 produces antinociception by stimulating one type of mu-opioid receptor, whereas endomorphin-2 initially stimulates different mu-opioid receptors, which subsequently induce the release of dynorphins that act on kappa-opioid receptors to produce antinociception.
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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,
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Immune Sera,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu,
http://linkedlifedata.com/resource/pubmed/chemical/endomorphin 1,
http://linkedlifedata.com/resource/pubmed/chemical/endomorphin 2
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-3565
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
292
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
576-83
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:10640294-Analgesics,
pubmed-meshheading:10640294-Analgesics, Opioid,
pubmed-meshheading:10640294-Animals,
pubmed-meshheading:10640294-Dose-Response Relationship, Drug,
pubmed-meshheading:10640294-Drug Interactions,
pubmed-meshheading:10640294-Immune Sera,
pubmed-meshheading:10640294-Injections, Intraventricular,
pubmed-meshheading:10640294-Ligands,
pubmed-meshheading:10640294-Male,
pubmed-meshheading:10640294-Mice,
pubmed-meshheading:10640294-Mice, Inbred ICR,
pubmed-meshheading:10640294-Oligopeptides,
pubmed-meshheading:10640294-Pain Measurement,
pubmed-meshheading:10640294-Receptors, Opioid,
pubmed-meshheading:10640294-Receptors, Opioid, mu,
pubmed-meshheading:10640294-Time Factors
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pubmed:year |
2000
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pubmed:articleTitle |
Differential antinociceptive effects of endomorphin-1 and endomorphin-2 in the mouse.
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pubmed:affiliation |
Department of Anesthesiology, Medical College of Wisconsin, Milwaukee, Wisconsin, USA. ltseng@mcw.edu
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.
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