pubmed-article:6147254 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0013227 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0023884 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0025519 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0030011 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C1882417 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0182400 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0054212 | lld:lifeskim |
pubmed-article:6147254 | lifeskim:mentions | umls-concept:C0332324 | lld:lifeskim |
pubmed-article:6147254 | pubmed:issue | 3 | lld:pubmed |
pubmed-article:6147254 | pubmed:dateCreated | 1984-9-28 | lld:pubmed |
pubmed-article:6147254 | pubmed:abstractText | The genetically controlled polymorphism causing decreased metabolism of debrisoquine is closely related to that of the metabolism of bufuralol and numerous other drugs and has important clinical consequences. A sensitive in vitro assay was developed which quantifies the production of 1'-hydroxy-bufuralol (carbinol) from bufuralol in human liver microsomes. Initial formation rates of carbinol suggested Michaelis-Menten kinetics with an apparent KM of 61 and 171 mumol l-1 and Vmax of 3.2 and 5.8 nmol mg-1 microsomal protein h-1 in two human liver samples. The Vmax in microsomes of thirty-two liver samples was 4.2 +/- 1.0 (SD) nmol carbinol mg-1 protein h-1. Metabolism of debrisoquine in vivo, as expressed by the 'metabolic ratio' of debrisoquine over 4-OH debrisoquine correlated (r = -0.65, P less than 0.01; n = 18) with carbinol production rate in microsomes in vitro. Microsomes of one individual identified as poor metabolizer of debrisoquine in vivo showed reduction of carbinol formation to 1.97 nmol mg-1 h-1. Mixing his microsomes with those of an extensive metabolizer resulted in additive formation of carbinol excluding mediation of the defect by a soluble inhibitor. These data support the concept of a primary defect in microsomal oxidation of bufuralol. The described assay offers a sensitive tool to investigate the molecular mechanism of the 'debrisoquine polymorphism'. | lld:pubmed |
pubmed-article:6147254 | pubmed:language | eng | lld:pubmed |
pubmed-article:6147254 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:6147254 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:6147254 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:6147254 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:6147254 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:6147254 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:6147254 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:6147254 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:6147254 | pubmed:month | Jun | lld:pubmed |
pubmed-article:6147254 | pubmed:issn | 0014-2972 | lld:pubmed |
pubmed-article:6147254 | pubmed:author | pubmed-author:MinderE IEI | lld:pubmed |
pubmed-article:6147254 | pubmed:author | pubmed-author:MüllerH KHK | lld:pubmed |
pubmed-article:6147254 | pubmed:author | pubmed-author:MinderCC | lld:pubmed |
pubmed-article:6147254 | pubmed:author | pubmed-author:MeyerU AUA | lld:pubmed |
pubmed-article:6147254 | pubmed:author | pubmed-author:MeierP JPJ | lld:pubmed |
pubmed-article:6147254 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:6147254 | pubmed:volume | 14 | lld:pubmed |
pubmed-article:6147254 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:6147254 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:6147254 | pubmed:pagination | 184-9 | lld:pubmed |
pubmed-article:6147254 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
pubmed-article:6147254 | pubmed:meshHeading | pubmed-meshheading:6147254-... | lld:pubmed |
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pubmed-article:6147254 | pubmed:year | 1984 | lld:pubmed |
pubmed-article:6147254 | pubmed:articleTitle | Bufuralol metabolism in human liver: a sensitive probe for the debrisoquine-type polymorphism of drug oxidation. | lld:pubmed |
pubmed-article:6147254 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:6147254 | pubmed:publicationType | In Vitro | lld:pubmed |
pubmed-article:6147254 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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