TABLE 1

Effects of ketoconazole, BNPP, paraoxon, DCMB, anisic acid, and SAH on the metabolism of [14C]MK-0767 in rat hepatocyte suspensions

Inhibitor
Concentration
Percentage Inhibition of Formationa
M5, M9
M16
M20
M24
M25
μM
Ketoconazole 1 75 85 100 100 100
5 73 88 100 100 100
10 62 85 100 100 100
BNPP 100 100 -b - - -
500 100 - 3 - -
1000 100 9 65 - 100
Paraoxon 100 100 - - - -
500 100 72 86 - 100
1000 100 89 100 - 100
DCMB 100 23 25 26 - -
500 36 85 85 52 100
1000 100 81 100 100 100
Anisic acid 100 - 3 - - -
500 58 2 33 - -
1000 15 - 8 - -
SAH 100 - 6 - 12 -
1000 - - - - -
2000
-
-
-
-
-

  • ↵ a Inhibition of metabolites was calculated relative to control incubations.

  • ↵ b -, no inhibition.