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. Author manuscript; available in PMC: 2008 May 21.
Published in final edited form as: Mol Pharmacol. 2007 Dec 21;73(3):1029–1036. doi: 10.1124/mol.107.043869

Table 1.

Kinetic parameters for midazolam metabolism by liver and intestinal microsomes. All values are the means of three independent experiments ± S.D. Incubations were performed as described in Materials and Methods.



1′-OH Midazolam
4-OH Midazolam
Microsomes Strain Kma Vmaxb Vmax/Kmc Kma Vmaxb Vmax/Kmc
Liver Cyp3a+/+ 0.95 ± 0.18 630 ± 29 662 8.43 ± 0.27 224 ± 12.7 26.6
Cyp3a−/− 6.38 ± 1.2 735 ± 11 115 17.5 ± 6.9 49.8 ± 5.0 2.36
Human 2.93 ± 0.33 2097 ± 155 715 38.7 ± 6.3 1226 ± 87 27.8
Intestine Cyp3a+/+ 10.4 ± 1.8 62.3 ± 3.2 6.02 55.9 ± 2.0 38.0 ± 5.2 0.68
Cyp3a−/− -d -d -d -d -d -d
Human 1.61 ± 0.04 596 ± 18 369 24.5 ± 3.3 330 ± 11 13.5
a

Km expressed in μM

b

Vmax expressed in pmol/min/mg protein

c

Vmax/Km expressed in μL/min/mg protein

d

No metabolite detected (detection limit <5 pmol/min/mg protein)