TABLE 2

Glucuronidation of compounds in human, dog, and rat liver microsomes Incubations were performed in duplicate at two different microsome concentrations (0.1 and 0.5 mg/ml) and stopped after 10, 20, and 40 min. Reactions were linear with time at one or both microsome concentrations. Reaction velocities were determined by linear regression analysis from the slope of the product formation time course. Results are mean values ± standard error of the fit or mean values ± half-range of the velocities obtained at two microsome concentrations.


Compound

Concentration

Reaction Velocity
HLM
DLM
RLM
mM nmol/min/mg
4MU 0.5 37 ± 7 120 ± 11 34 ± 9
Octyl gallate 0.5 6.7 ± 2.3 3.9 ± 1.3 9.4 ± 0.15
1NP 1 27 ± 4 121 ± 15 38.1 ± 2.2
5α-Androstane-3α,17α-diol 0.25 1.4 ± 0.04 1.4 ± 0.2 1.0 ± 0.04
5α-Androstane-3α,17β-diol 0.25 5.8 ± 0.6 6.8 ± 2.2 7.4 ± 0.8
Hyodeoxycholic acid 1 3.9 ± 0.2 3.8 ± 0.4 <0.3
β-Estradiol 1 1.3 ± 0.03 21.1 ± 1.7 4.1 ± 0.2
Naproxen 1 0.8 ± 0.14 4.6 ± 0.3 4.10 ± 1.0
Naloxone 1 1.4 ± 0.2 5.6 ± 0.5 5.0 ± 0.3
Furosemide 1 0.49 ± 0.04 1.3 ± 0.1 <0.3
Gemfibrozil 1 2.4 ± 1.0 13.8 ± 2.2 3.9 ± 0.3
Valproic acid 1 0.6 ± 0.2 5.0 ± 1.4 11 ± 5
17α-Ethynylestradiol 0.25 0.6 ± 0.1 <0.6 0.6 ± 0.1
Propofol
0.5
1.3 ± 0.3
<0.6
1.4 ± 0.4