TABLE 2

Kinetic parameters estimated from 13-DMT and 12-HT formation

Each reported parameter and computer-generated error estimate (numbers in parentheses, expressed as %CV) represents the average of values obtained from two separate experiments.




Vmax1

Km1,u

CLint1.u

Vmax2

Km2,u

CLint2,u
nmol/min/nmol μM ml/min/nmol nmol/min/nmol μM ml/min/nmol
13-DMT
    rCYP3A4+b5 8.0 (5.6) 0.21 (12.7) 38
    rCYP3A5+b5 17.0 (2.4) 0.21 (6.4) 82
    rCYP3A4 0.1 (53.8) 0.002 (86.8) 58 7.8 (9.6) 0.9 (24.8) 10
    rCYP3A5 0.2 (88.0) 0.003 (148.4) 97 10.8 (25.9) 0.6 (46.5) 23
12-HT
    rCYP3A4+b5 0.6 (12.7) 0.29 (24.9) 2
    rCYP3A5+b5 1.4 (9.2) 0.35 (19.2) 4
    rCYP3A4 0.02 (269.0) 0.011 (295.5) 1.6 0.3 (40.1) 1.2 (85.5) 0.4
    rCYP3A5
0.01 (79.4)
0.005 (100.3)
3.0
0.8 (41.7)
1.1 (65.1)
0.8