Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes

Drug Metabolism and Disposition

Volumn 29, Issue 10, 2001, Pages 1325-1331

  Drocourt, Lionel ^a   Pascussi, Jean Marc ^a   Assenat, Eric ^a   Fabre, Jean Michel ^b   Maurel, Patrick ^a   Vilarem, Marie José ^a,c  

^a CNRS   (France)

^b HÔPITAL SAINT ELOI   (France)

^c INSERM   (France)

Author keywords

[No Author keywords available]

Indexed keywords

1,4 DIHYDRO 2,6 DIMETHYL 5 NITRO 4 [2 (TRIFLUOROMETHYL)PHENYL] 3 PYRIDINECARBOXYLIC ACID METHYL ESTER; ANDROSTANE DERIVATIVE; CALCIUM CHANNEL; CALCIUM CHANNEL AFFECTING AGENT; CYTOCHROME P450 2B6; CYTOCHROME P450 2C9; CYTOCHROME P450 3A; DEXAMETHASONE; DIHYDROPYRIDINE DERIVATIVE; GLUTATHIONE TRANSFERASE; IFR 24; ISRADIPINE; NICARDIPINE; NIFEDIPINE; PREGNANE DERIVATIVE; PREGNANE X RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME INDUCTION; ENZYME METABOLISM; GENE EXPRESSION REGULATION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; LIVER CELL; NORTHERN BLOTTING; PRIORITY JOURNAL; PROMOTER REGION; PROTEIN EXPRESSION; RECEPTOR UPREGULATION; SIGNAL TRANSDUCTION; WESTERN BLOTTING;

ARYL HYDROCARBON HYDROXYLASES; CALCIUM CHANNELS; CYTOCHROME P-450 ENZYME SYSTEM; DIHYDROPYRIDINES; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INDUCTION; ENZYME INHIBITORS; HEPATOCYTES; HUMANS; KINETICS; MIXED FUNCTION OXYGENASES; NIFEDIPINE; OXIDOREDUCTASES, N-DEMETHYLATING; PROMOTER REGIONS (GENETICS); RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, STEROID; RIFAMPIN; RNA, MESSENGER; STEROID 16-ALPHA-HYDROXYLASE; STEROID HYDROXYLASES; TIME FACTORS;

EID: 0034827301     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (28)

1. Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction
2. SXR, a novel steroid and xenobiotic-sensing nuclear receptor
3. Induction of microsomal enzymes by foreign chemicals and carcinogenesis by polycyclic aromatic hydrocarbons: G. H. A. Clowes Memorial Lecture
4. Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors
5. Androstane metabolites bind to and deactivate the nuclear receptor CAR-β
6. Induction of CYP2C genes in human hepatocytes in primary culture
7. The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module
8. Effect of cell density and epidermal growth factor on the inducible expression of CYP3A and CYP1A genes in human hepatocytes in primary culture
9. Reactions and significance of cytochrome P-450 enzymes
10. Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism
11. Absorption, excretion and metabolism of a new dihydropyridine diester cerebral vasodilator in rats and dogs
12. Metabolic fate of nicardipine hydrochloride, a new vasodilator, by various species in vitro
13. The nuclear orphan receptor CAR-retinoid X receptor heterodimer activates the phenobarbital-responsive enhancer module of the CYP2B gene
14. Sequence of the 5′-flanking region of CYP3A5: Comparative analysis with CYP3A4 and CYP3A7
15. Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: Prediction of in vivo drug-drug interactions
16. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway
17. On the enzyme-inducing action of calcium antagonists
18. Effect of nifedipine, verapamil and diltiazem on the enzyme-inducing activity of phenobarbital and beta-naphthoflavone
19. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions
20. Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands
21. Dexamethasone induces pregnane X receptor and retinoid X receptor-alpha expression in human hepatocytes: Synergistic increase of CYP3A4 induction by pregnane X receptor activators
22. Dexamethasone enhances constitutive androstane receptor expression in human hepatocytes: Consequences on cytochrome P450 gene regulation
23. Digoxin-verapamil interaction
24. Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes
25. The diltiazem-digoxin interaction
26. The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene
27. Reciprocal activation of xenobiotic response genes by nuclear receptors SXR/PXR and CAR
28. Effect of calcium channel antagonists nifedipine and nicardipine on rat cytochrome P-450 2B and 3A forms