Title : In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines.

Pub. Date : 1999 Nov 15

PMID : 10597902






2 Functional Relationships(s)
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1 Cetirizine, terfenadine, loratadine, astemizole and mizolastine were compared for their ability to inhibit marker activities for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4 and for some glucuronidation isoenzymes in human liver microsomes. Loratadine cytochrome P450 family 2 subfamily D member 6 Homo sapiens
2 The most pronounced effects were observed with terfenadine, astemizole and loratadine which inhibited CYP3A4-mediated testosterone 6beta-hydroxylation (IC50 of 23, 21 and 32 microM, respectively) and CYP2D6-mediated dextromethorphan O-demethylation (IC50 of 18, 36 and 15 microM, respectively). Loratadine cytochrome P450 family 2 subfamily D member 6 Homo sapiens