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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1990-5-30
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pubmed:abstractText |
The effect of continuous intrathecal infusions of opioids was studied in rats. Chronic intrathecal infusion of the highly selective mu agonist, [NMPhe3, D-Pro4]morphiceptin produced a rapid onset of tolerance to the drug in the analgesic test. However, membrane prepared from the spinal cords of the rats chronically infused with a low dose of the drug showed no statistically significant change in the number of mu or delta receptor binding sites. In addition, membrane prepared from rats challenged with a single high-dose bolus injection of [NMPhe3, D-Pro4]morphiceptin did not produce alterations in the receptor binding number. If the chronically treated rats were challenged with an acute bolus dose of [NMPhe3, D-Pro4]morphiceptin, there was a significant decrease in the number of binding sites. The reduced binding site number was observed for the mu ligand but not for the delta ligand. A similar decrease of receptor binding can also be achieved by chronic infusion of the drug at high doses. Scatchard plot showed a decrease of maximum mu binding sites in the membranes prepared from the combined chronic infusion-acute injection treated rats. Brain tissue from the same rats showed no change in the number of mu and delta receptor binding sites, indicating that the down-regulation of mu receptors was confined to the spinal cord only. Morphine did not induce receptor down-regulation by acute, chronic or combined treatments. These results suggest that in the rat spinal cord, tolerance can be induced without apparent receptor down-regulation.(ABSTRACT TRUNCATED AT 250 WORDS)
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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/Endorphins,
http://linkedlifedata.com/resource/pubmed/chemical/Morphine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu,
http://linkedlifedata.com/resource/pubmed/chemical/morphiceptin, N-Me-Phe(3)-
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0022-3565
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
253
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
67-72
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:2158554-Animals,
pubmed-meshheading:2158554-Down-Regulation,
pubmed-meshheading:2158554-Drug Tolerance,
pubmed-meshheading:2158554-Endorphins,
pubmed-meshheading:2158554-Male,
pubmed-meshheading:2158554-Morphine,
pubmed-meshheading:2158554-Rats,
pubmed-meshheading:2158554-Rats, Inbred Strains,
pubmed-meshheading:2158554-Receptors, Opioid,
pubmed-meshheading:2158554-Receptors, Opioid, mu,
pubmed-meshheading:2158554-Spinal Cord
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pubmed:year |
1990
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pubmed:articleTitle |
Dissociation of mu opioid tolerance from receptor down-regulation in rat spinal cord.
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pubmed:affiliation |
Department of Anesthesiology, Duke University Medical Center, Durham, North Carolina.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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