Table 1

Estimates of apparent Vmax and Km of HL for CYP probe drugs

CYPSubstrateConcentrationMicrosomal PreparationsKmVmax
μM μM nmol/min/mg
CYP1A2phenacetin25–150MHL-G1-b 48.7  ± 11.01-a 2.2  ± 0.3
HL-767.1  ± 15.00.4  ± 0.2
HL-1452.1  ± 25.42.5  ± 1.3
CYP2C9tolbutamide25–200HL-29152.1  ± 31.50.03  ± 0.01
MHL-B1-c 163.5  ± 26.70.26  ± 0.04
CYP2C19omeprazole25–150HL-2942.2  ± 12.90.13  ± 0.04
MHL-B1-c 55.1  ± 9.20.11  ± 0.01
CYP2D6dextromethorphan10–75MHL-D1-d 26.2  ± 7.50.06  ± 0.01
HL-2926.9  ± 5.50.34  ± 0.03
HL-1022.3  ± 4.00.20  ± 0.02
CYP3Adextromethorphan100–750HL-10236.3  ± 54.90.34  ± 0.08
MHL-B1-c 320.8  ± 75.40.84  ± 0.14
  • 1-a Each value indicates the mean ± S.D. of three to eight different determinations.

  • 1-b Mixed HL-5, -9, -10.

  • 1-c Mixed HL-15, -19, -20.

  • 1-d Mixed HL-8, -11, -14.