TABLE 2

Enzyme kinetic parameters of buspirone metabolism in HLM [14C]Buspirone, at concentrations ranging from 2.5 to 150 μM, was incubated with pooled human liver microsomes (0.1 mg/ml) and NADPH (500 μM) in 100 mM sodium phosphate buffer (pH 7.4) for 5 min. Data presented in this table were averaged from analyses of duplicate incubations.


Metabolic Reaction

Apparent Km

Apparent Vmax

Apparent CLint
μM nmol/min/mg protein ml/min/mg protein
1-PP formation 8.7 ± 1.1 0.74 ± 0.02 0.085
3′-OH-Bu formation 4.3 ± 0.8 0.30 ± 0.01 0.070
6′-OH-Bu formationa 8.8 ± 0.9 1.37 ± 0.04 0.156
5-OH-Bu formationa 11.4 ± 5.6 0.77 ± 0.25 0.068
514 ± 231 7.5 ± 2.2 0.015
Bu N-oxide formation
34.0 ± 8.9
1.64 ± 0.8
0.048
  • a Kinetic plots of the formation of the metabolite are presented in Fig. 4