TABLE 4

Inhibitory potency of PGD toward P450s in CLZ metabolism in recombinantly expressed P450s

P450sMetabolites of CLZVmaxKmKiInhibition Model
pmol/min per milligram of proteinμMmg/ml
1A2norCLZ28.5 ± 4.7a50.8 ± 0.50.9 ± 0.1Noncompetitive
2C19norCLZ23.9 ± 1.330.9 ± 1.40.3 ± 0.0Noncompetitive
2D6norCLZ53.1 ± 4.312.0 ± 4.02.4 ± 0.5Mixed
3A4norCLZ15.2 ± 0.240.2 ± 10.50.6 ± 0.1Competitive
3A4CLZ-N-oxide27.7 ± 3.816.1 ± 2.90.5 ± 0.1Mixed
  • a Data are expressed as mean ± S.E.M. (n = 3).