Title : Terfenadone is a strong inhibitor of CYP2J2 present in the human liver and intestinal microsomes.

Pub. Date : 2018 Jun

PMID : 29759885






4 Functional Relationships(s)
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1 In a previous study, we used recombinant CYP2J2 and determined whether danazol, hydroxyebastine, telmisartan, and terfenadone inhibited CYP2J2 by using four representative CYP2J2 substrates, namely albendazole, astemizole, ebastine, and terfenadine. Terfenadine cytochrome P450 family 2 subfamily J member 2 Homo sapiens
2 In a previous study, we used recombinant CYP2J2 and determined whether danazol, hydroxyebastine, telmisartan, and terfenadone inhibited CYP2J2 by using four representative CYP2J2 substrates, namely albendazole, astemizole, ebastine, and terfenadine. Terfenadine cytochrome P450 family 2 subfamily J member 2 Homo sapiens
3 Among the four CYP2J2 inhibitors tested, terfenadone was strongest inhibitor of CYP2J2-mediated metabolism of albendazole, astemizole, and terfenadine with IC50 values of 0.31, 0.15, and 2.11 muM, respectively, in human liver microsomes (HLMs). Terfenadine cytochrome P450 family 2 subfamily J member 2 Homo sapiens
4 Among the four CYP2J2 inhibitors tested, terfenadone was strongest inhibitor of CYP2J2-mediated metabolism of albendazole, astemizole, and terfenadine with IC50 values of 0.31, 0.15, and 2.11 muM, respectively, in human liver microsomes (HLMs). Terfenadine cytochrome P450 family 2 subfamily J member 2 Homo sapiens