Table 2

Coefficients of regression for formation of Lu 25-109 metabolites at pH 7.4 with form-selective enzyme activities

Form-Selective Activity2-aCorrelation Coefficient (r2)
Lu 31-1262-bLu 29-2972-bLu 25-0772-bLu 32-1812-b
7-Ethoxyresorufin O-dealkylation (1A2)0.0920.1910.1270.041
Coumarin 7-hydroxylation (2A6)0.0910.5532-150 0.3772-150 0.164
Tolbutamide methyl-hydroxylation (2C9)0.0410.0180.0010.008
S-mephenytoin 4′-hydroxylation (2C19)0.0390.2770.0910.144
DextromethorphanO-demethylation (2D6)0.7942-150 0.2200.2060.158
Chlorzoxazone 6-hydroxylation (2E1)0.2090.1720.1410.182
DextromethorphanN-demethylation (3A4)0.0970.4892-150 0.4702-150 0.008
Testosterone 6β-hydroxylation (3A4/5)0.0240.2130.1730.069
Lauric acid 12-hydroxylation (4A9/11)0.0120.0410.0010.142
N-oxygenation of tertiary amine (FMO3)2-c 0.0440.0030.0050.021
Methyl toluyl sulfide S-oxygenation (FMO3)2-d 0.0740.0750.0200.008
  • 2-150P < 0.05.

  • 2-a Determined by Xenotech as described in Materials and Methods.

  • 2-b Incubations were performed in triplicate at Lu 25-109 concentration of 200 μM.

  • 2-c Determined at pH 7.5.

  • 2-d Determined at pH 8.5.