TABLE 1

Kinetic parameters for haloperidol pyridinium metabolites HPP+and RHPP+in the hOCT1, 2, and 3 stably expressed MDCK cells

Vmax represents the maximal reaction velocity, and Km is the substrate concentration corresponding to 50% of Vmax. The values are estimated from nonlinear least regression analysis using WinNonlin.


Compounds

Kinetic Parameters

hOCT1

hOCT2

hOCT3
HPP+ Km (pmol/min/μg protein) 0.99 ± 0.05 2.79 ± 0.13 2.23 ± 0.16
Vmax (μM) 282.1 ± 4.7 256.1 ± 11.3 400.2 ± 15.2
RHPP+ Km (pmol/min/μg protein) 5.15 ± 0.63 8.21 ± 0.77

Vmax (μM)
1230.9 ± 24.8

1348.6 ± 36.3