substrate of the cytochrome P450 (CYP) isoform CYP2C19
CAS：70989-04-7
分子式：C12H14N2O2
分子量：218.3
纯度：98%
存储：Store at -20°C

Background:

(S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19, also known as mephenytoin 4-hydroxylase.[1] CYP2C19 metabolizes a variety of therapeutic agents, including omeprazole, proguanil, diazepam, propranolol, citalopram, imipramine, and certain barbiturates.[2] Genetic defects in CYP2C19 result in poor metabolism of these compounds, and (S)-mephenytoin can be used to screen for such mutations by assaying its metabolites in urine.[2],[3],[4] (S)-Mephenytoin has anticonvulsant activities.[5]

Reference:
[1]. Shimada, T., Misono, K.S., and Guengerich, F.P. Human liver microsomal cytochrome P-450 mephenytoin 4-hydroxylase, a prototype of genetic polymorphism in oxidative drug metabolism. The Journal of Biological Chemisty 261(2), 909-921 (1986).
[2]. Ferguson, R.J., de Morais, S.M., Benhamou, S., et al. A new genetic defect in human CYP2C19: Mutation of the initiation codon is responsible for poor metabolism of S-mephenytoin. Journal of Pharmacology and Experimental Therapeutics 284(1), 356-361 (1998).
[3]. Ozawa, S., Soyama, A., Saeki, M., et al. Ethnic differences in genetic polymorphisms of CYP2D6, CYP2C19, CYP3As and MDR1/ABCB1. Drug Metab.Pharmacokinet. 19(2), 83-95 (2004).
[4]. Guttendorf, R.J., Britto, M., Blouin, R.A., et al. Rapid screening for polymorphisms in dextromethorphan and mephenytoin metabolism. British Journal of Clinical Pharmacology 29(4), 373-380 (1990).
[5]. Wong, P.T.H., Tan, S.F., and Lee, H.S. N-demethylation of methyl and dimethyl derivatives of phenytoin and their anticonvulsant activities in mice. Japanese Journal of Pharmacology 48(4), 473-478 (1988).