Switch to
Predicate | Object |
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rdf:type | |
lifeskim:mentions |
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0025519,
umls-concept:C0033497,
umls-concept:C0034693,
umls-concept:C0034721,
umls-concept:C0205054,
umls-concept:C0205332,
umls-concept:C0870883,
umls-concept:C1145667,
umls-concept:C1167622,
umls-concept:C1979928,
umls-concept:C2349209,
umls-concept:C2825311
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pubmed:issue |
2
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pubmed:dateCreated |
1980-6-27
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pubmed:abstractText |
Repetitive oral propranolol administration to rats (100 mg/kg/day for 5 days) resulted in an 80% inhibition of propranolol Type I spectral binding capacity. This paralleled a similar reduction in the microsomal metabolism of propranolol when incubated at low substrate concentrations (less than 2 microM). Propranolo was converted both in vitro and in vivo by a microsomal mixed function oxidase to a reactive intermediate metabolite capable of covalently binding with microsomal macromolecules. We propose that covalent binding of the intermediate to the catalytic site of a form(s) of cytochrome P-450 that metabolizes propranolol would account for the marked inhibition of propranolol metabolism observed following propranolol pretreatment.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0034-5164
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
27
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
211-22
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:6768117-Animals,
pubmed-meshheading:6768117-Cytochrome P-450 Enzyme System,
pubmed-meshheading:6768117-Glutathione,
pubmed-meshheading:6768117-Male,
pubmed-meshheading:6768117-Microsomes, Liver,
pubmed-meshheading:6768117-Propranolol,
pubmed-meshheading:6768117-Protein Binding,
pubmed-meshheading:6768117-Proteins,
pubmed-meshheading:6768117-Rats,
pubmed-meshheading:6768117-Time Factors
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pubmed:year |
1980
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pubmed:articleTitle |
The inhibition of rat hepatic microsomal propranolol metabolism by a covalently bound reactive metabolite.
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pubmed:publicationType |
Journal Article,
In Vitro
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