Title : Transport and uptake of clausenamide enantiomers in CYP3A4-transfected Caco-2 cells: An insight into the efflux-metabolism alliance.

Pub. Date : 2015 Nov 1

PMID : 26301745






3 Functional Relationships(s)
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1 Their bidirectional transports were significantly reduced by 75.6-87.5% after treatment with verapamil (a P-glycoprotein inhibitor) that increased the rate of metabolism by CYP3A4, whereas the CYP3A4 inhibitor ketoconazole treatment markedly enhanced the basolateral to apical flux of (-) and (+)CLA with ERs being 2.934+-1.432 and 1.877+-0.148(x10(-6)cm/s) respectively. Verapamil cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Their bidirectional transports were significantly reduced by 75.6-87.5% after treatment with verapamil (a P-glycoprotein inhibitor) that increased the rate of metabolism by CYP3A4, whereas the CYP3A4 inhibitor ketoconazole treatment markedly enhanced the basolateral to apical flux of (-) and (+)CLA with ERs being 2.934+-1.432 and 1.877+-0.148(x10(-6)cm/s) respectively. Verapamil cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 These changes could be blocked by the duel CYP3A4/P-glycoprotein inhibitor cyclosporine A, consequently, Papp values for CLA enantiomers in both directions were significantly greater than those obtained by using verapamil or ketoconazole, and their ERs were similar to those following (-) or (+)-isomer treatment alone. Verapamil cytochrome P450 family 3 subfamily A member 4 Homo sapiens