Linked Life Data

12350087

Source:http://linkedlifedata.com/resource/pubmed/id/12350087

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-2
pubmed:dateCreated
2002-9-27
pubmed:abstractText
Verapamil is a commonly prescribed cardiovascular drug, but surprisingly its metabolism in the target tissue of pharmacotherapy is basically unknown. We therefore investigated its biotransformation in human heart tissue and correlate the production of metabolites with the gene expression of major drug metabolising enzymes. Using electrospray LC-MS-MS and LC-MS3 experiments, a total of nine metabolites were observed in incubation experiments with verapamil and microsomes isolated from the human heart tissue, and this included a carbinolamine-, N-formyl-, ahemiacetale-, and formate-intermediate of N-demethyl- and O-demethylverapamil. We also observed a hydroxylation product at the benzylic position of atom C-7 (M9). Metabolites M5-M9 are novel and were not observed in previous studies with liver or other human tissues. A fine example of the considerable metabolic competence of human heart is the formation of M1-M4, e.g. dealkylverapamil, norverapamil and isomers of O-demethylverapamil, which were believed to be exclusively produced by the liver.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0021-9673
pubmed:author
pubmed:issnType
Print
pubmed:day
13
pubmed:volume
970
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
117-30
pubmed:dateRevised
2009-1-15
pubmed:meshHeading
pubmed:year
2002
pubmed:articleTitle
Verapamil: new insight into the molecular mechanism of drug oxidation in the human heart.
pubmed:affiliation
Fraunhofer Institute of Toxicology and Aerosol Research, Center of Drug Research and Medical Biotechnology, Hannover, Germany.
pubmed:publicationType
Journal Article