CYP2D6 is involved in O-demethylation of diltiazem: An in vitro study with transfected human liver cells

European Journal of Clinical Pharmacology

Volumn 56, Issue 8, 2000, Pages 575-579

  Molden, Espen ^a   Åsberg, Anders ^b   Christensen, Hege ^a  

^a UNIVERSITY OF OSLO   (Norway)

^b OSLO UNIVERSITY HOSPITAL   (Norway)

Author keywords

CYP2D6; Diltiazem; Metabolism

Indexed keywords

CYTOCHROME P450; CYTOCHROME P450 2D6; DILTIAZEM; DILTIAZEM DERIVATIVE; ERYTHROMYCIN; QUINIDINE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; CULTURE MEDIUM; DEMETHYLATION; DRUG METABOLISM; ENZYME POLYMORPHISM; GENETIC TRANSFECTION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; IN VITRO STUDY; LIVER CELL; MICHAELIS MENTEN KINETICS; PRIORITY JOURNAL;

ACETYLATION; CALCIUM CHANNEL BLOCKERS; CYTOCHROME P-450 CYP2D6; DILTIAZEM; EPITHELIAL CELLS; HEPATOCYTES; HUMANS; KINETICS; METHYLATION; TRANSFECTION;

EID: 0033671146     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002280000182     Document Type: Article

References (15)

1. Pharmacokinetics and metabolism of diltiazem in healthy males and females following a single oral dose
2. Deacetylation of diltiazem by several rabbit tissues
3. Role of CYP3A4 in human hepatic diltiazem N-demethylation: Inhibition of CYP3A4 activity by oxidized diltiazem metabolites
4. Diltiazem inhibition of cytochrome P-450 3A activity is due to metabolite intermediate complex formation
5. Pharmacokinetic interactions between microemulsion formulated cyclosporine A and diltiazem in renal transplant recipients
6. Simian virus 40 large tumor antigen-immortalized normal human liver epithelial cells express hepatocyte characteristics and metabolize chemical carcinogens
7. Aflatoxin B1-induced DNA adduct formation and p53 mutations in CYP450-expressing human liver cell lines
8. A simple and sensitive high-performance liquid chromatography assay of diltiazem and main metabolites in renal transplanted patients
9. Highly efficient establishment of immortalized cells from adult human liver
10. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
11. Geographical/interracial differences in polymorphic drug oxidation. Current state of knowledge of cytochromes P450 (CYP) 2D6 and 2C19
12. Drug interactions with calcium channel blockers: Possible involvement of metabolite-intermediate complexation with CYP3A
13. Synthesis, characterization, and Ca2+ antagonistic activity of diltiazem metabolites
14. Calcium channel receptor binding studies for diltiazem and its major metabolites: Functional correlation to inhibition of portal vein myogenic activity
15. Cardiovascular effects of the metabolites of diltiazem in dogs