TABLE 3

Metabolic parameters for N-dealkylated VP, O-demethylated VP, and NVP in rat small intestinal microsomes

Each value represents the mean ± S.D. (n = 4).



N-Dealkylated VP

O-Demethylated VP

NVP

S
R
S
R
S
R
Km (μM) 125.3 ± 18.2 65 ± 11.2* 140 ± 52.2 74.4 ± 11.3 79.6 ± 18.6 59.5 ± 11.6
Vmax (pmol/min/mg protein) 11.2 ± 1.9 13.8 ± 5.2 6.7 ± 2.2 8.7 ± 2.7 13.1 ± 3.4 16.0 ± 3.4
Vmax/Km (μl/min/g protein)
0.09 ± 0.02
0.21 ± 0.08*
0.06 ± 0.03
0.12 ± 0.06
0.07 ± 0.03
0.27 ± 0.06*
  • * p < 0.05 (versus S-enantiomer).