Title : Transcriptional profiling of genes induced in the livers of patients treated with carbamazepine.

Pub. Date : 2006 Nov

PMID : 17112801






2 Functional Relationships(s)
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1 In transactivation studies in CV-1 cells, we demonstrated that both CBZ and its major metabolite, CBZ-10,11-epoxide, activate the nuclear receptor PXR in a concentration-dependent fashion and at therapeutic concentrations with 50% inhibitory concentration values of approximately 50 micromol/L. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
2 CONCLUSIONS: CBZ is a potent inducer of a broad spectrum of drug-metabolizing enzymes and drug transporters in the human liver, and these effects are mediated at least in part by activation of PXR. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens