Title : Main contribution of the cytochrome P450 isoenzyme 1A2 (CYP1A2) to N-demethylation and 5-sulfoxidation of the phenothiazine neuroleptic chlorpromazine in human liver--A comparison with other phenothiazines.

Pub. Date : 2010 Oct 15

PMID : 20615392






2 Functional Relationships(s)
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1 The obtained results indicate that CYP1A2 is the only CYP isoform that catalyzes the mono-N-demethylation and di-N-demethylation of chlorpromazine (100%) and is the main isoform responsible for chlorpromazine 5-sulfoxidation (64%) at a therapeutic concentration of the drug (10 microM). mono-n-octyl phthalate cytochrome P450 family 1 subfamily A member 2 Homo sapiens
2 Similar results were obtained at a higher, non-therapeutic concentration of the drug (100 microM); however, the contribution of CYP1A2 to chlorpromazine mono-N-demethylation was noticeably lower (75%), mostly in favour of CYP2C19 and CYP3A4 (about 12% each). mono-n-octyl phthalate cytochrome P450 family 1 subfamily A member 2 Homo sapiens