Correlation of various P450-selective monooxygenase activities with the hydroxylation of etoricoxib (5 and 200 μM) in a panel of human liver microsomes
Activity2-a | P450s | Correlation Coefficient (r) | |
---|---|---|---|
5 μM | 200 μM | ||
TESTase | CYP3A4/5 | 0.802-165 | 0.892-165 |
ERODase | CYP1A2 | 0.31 | 0.10 |
COHase | CYP2A6 | 0.50 | 0.712-160 |
TAXase | CYP2C8 | 0.49 | 0.722-160 |
TOLase | CYP2C9 | 0.04 | 0.27 |
MEPHase | CYP2C19 | 0.15 | 0.47 |
BUFase | CYP2D6 | 0.34 | 0.38 |
CHLORase | CYP2E1 | 0.19 | 0.04 |
↵2-a The various activities are TOLase, tolbutamide hydroxylase; COHase, COU hydroxylase; ERODase, 7-ethoxyresorufin O-deethylase; CHLORase, chlorzoxazone 6-hydroxylase; BUFase, bufuralol 1′-hydroxylase; TESTase, testosterone 6β-hydroxylase; MEPHase, (S)-(+)-mephenytoin 4′-hydroxylase; and TAXase, Taxol 6-hydroxylase. The correlation coefficient was determined with the liver tissue of 15 different organ donor subjects. Statistical significance (Student's t test) of the correlation is denoted by:
↵2-160 p < 0.01 and
↵2-165 p < 0.001.