Table 1

Inhibition constants characterizing the inhibition of human liver microsomal DEXTROase activity in the presence of DEX or QND

Parameter1-aSubject IDMean ± SD1-b
ICFHFQGC4
DEX
 Ki (μM)0.20.50.40.4  ± 0.2
 K ies (μM)3.22.21.52.3  ± 0.9
 α164.43.98.1  ± 6.8
QND
 Ki (μM)0.050.08—1-c 0.071-d

  • ↵1-a Ki ,Kies, and α (Kies/Ki ) were determined using Dixon and Cornish-Bowden plots. DEX behaved as a mixed (competitive/noncompetitive) inhibitor (Kies >Ki ; α > 1), and QND exhibited competitive inhibition.

  • ↵1-b Mean ± SD of three livers.

  • ↵1-c —, not determined.

  • ↵1-d Mean of two livers.