TABLE 1

Kinetic parameters of UGT activities in liver microsomes from male and female mice and rats

TFP N-glucuronide was not detected in liver microsomes from male and female mice and rats.


Substrate

Species

Sex

Km (S50)

Vmax

Ksi

CLint (CLmax)

n a
μM nmol/min/mg protein μM μl/min/mg protein
Estradiol Mouse M 17 ± 3b 6.1 ± 0.3 179c 2.3
F 18 ± 2b 6.6 ± 0.4 183c 2.3
Rat M 16 ± 3b 6.1 ± 0.4 193c 1.8
F 16 ± 2b 7.1 ± 0.3 231c 1.8
4-MU Mouse M 71 ± 8b 214 ± 9 1975c 1.2
F 59 ± 3b 159 ± 3 1436c 1.5
Rat M 130 ± 11b 264 ± 11 1146c 1.4
F 130 ± 6b 286 ± 7 1241c 1.3
4-NP Mouse M 116 ± 23 40 ± 2 341
F 112 ± 24 33 ± 2 293
Rat M 378 ± 73 81 ± 7 213
F 635 ± 108 73 ± 6 115
Propofol Mouse M 31 ± 3 1.9 ± 0.1 1069 ± 96 62
F 51 ± 11 2.5 ± 0.3 514 ± 105 49
Rat M 16 ± 4 0.22 ± 0.07 14
F 51 ± 21 0.06 ± 0.01 1.2
MPA Mouse M 307 ± 59 24 ± 2 78
F 242 ± 21 27 ± 1 111
Rat M 344 ± 26 5.9 ± 0.2 17
F 304 ± 24 3.0 ± 0.1 9.9
Morphine Mouse M 421 ± 17 19 ± 0 46
F 318 ± 15 20 ± 0 64
Rat M 1406 ± 17 39 ± 0 27


F
1319 ± 79
35 ± 1

26

  • a Hill coefficient.

  • b S50.

  • c CLmax.