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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2008-6-10
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pubmed:abstractText |
Numerous studies have shown that many clinically employed opioid analgesics are substrates for P-glycoprotein (P-gp), suggesting that up-regulation of P-gp may contribute to the development of central tolerance to opioids. The studies herein focus on the development of SAR for P-gp substrate activity in the meperidine series of opioids. Addition of a 3-OH to meperidine and the ketone analog of meperidine yielding bemidone and ketobemidone, respectively, significantly increased P-gp substrate affinity. The results of this study have implications in the development of novel analgesics to be utilized as tools to study the contribution of P-gp on the development of central tolerance to opioids.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-10331089,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-10665989,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-11602674,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-14406754,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-14576852,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-14698039,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-17251015,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-17593551,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-18311899,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-7910522,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18499452-833816
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3638-40
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pubmed:dateRevised |
2011-9-26
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pubmed:meshHeading |
pubmed-meshheading:18499452-Drug Evaluation, Preclinical,
pubmed-meshheading:18499452-Hydroxyl Radical,
pubmed-meshheading:18499452-Meperidine,
pubmed-meshheading:18499452-Molecular Structure,
pubmed-meshheading:18499452-P-Glycoproteins,
pubmed-meshheading:18499452-Receptors, Opioid,
pubmed-meshheading:18499452-Stereoisomerism,
pubmed-meshheading:18499452-Structure-Activity Relationship,
pubmed-meshheading:18499452-Substrate Specificity
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pubmed:year |
2008
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pubmed:articleTitle |
Opioids and efflux transporters. Part 3: P-glycoprotein substrate activity of 3-hydroxyl addition to meperidine analogs.
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pubmed:affiliation |
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Room 543, Baltimore, MD 21201, USA.
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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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