Table 1

Vmax and Km values for P450-mediated selegiline metabolism to desmethylselegiline and levomethamphetamine

Desmethylselegiline
CYP ContentKmVmaxVmax/KmHepatic ClearanceHepatic Clearance
pmol/mg μM pmol/pmol/min ml/μmolP450*min l/h % of total
1A1 1-b 1617430 1-b
1A250334123676
2A66637651333
2B626255220556257
2C81-a 1-b 82337 1-b 1-b
2C9556283511
2C19262073502624
2D611 1-c 1-c 1-c 1-c 1-c
2E15367871022
3A41-a 127608101687
Levomethamphetamine
CYP ContentKmVmaxVmax/KmHepatic ClearanceHepatic Clearance
pmol/mg μM pmol/pmol/min ml/μmolP450*min l/h % of total
1A1 1-b 11710850 1-b
1A2503793284149
2A666 1-c 1-c 1-c 1-c 1-c
2B626336519946240
2C81-a 1-b 6307110 1-b
2C9552522820
2C1926203015005636
2D611 1-c 1-c 1-c 1-c 1-c
2E15343761432
3A41-a 12761228461912

The subsequent calculation of hepatic clearance uses the conversion factors described under Materials and Methods. The contribution of each specific enzyme to the hepatic clearance is also shown. The data for the specific P450 content were from GENTEST (http://www.gentest.com/prod_inserts/H161_2.htm#immunoquantitation).

  • 1-a  Including human cytochrome P450 reductase and cytochrome b5.

  • 1-b  P450 content not provided.

  • 1-c  Below the limit of detection.