Kinetic characterization of GABA transport in HEK cells expressing mGAT1 or mGAT2 by EF1502 HEK cells transiently expressing mGAT1 and mGAT2 were prepared as detailed under Materials and Methods, and the kinetic analysis of GABA transport was performed in the absence or presence of 5 μM EF1502 using a series of GABA concentrations as described under Materials and Methods.
| Km | Vmax | Ki | Type | |||
|---|---|---|---|---|---|---|
| Control | EF1502 | Control | EF1502 | |||
| μM | nmol × min-1 × mg-1 | μM | ||||
| mGAT1 | 12 ± 4 | 17 ± 5 | 1.65 ± 0.19 | 0.73 ± 0.11* | 4 | Noncompetitive |
| mGAT2 | 55 ± 6 | 52 ± 9 | 0.41 ± 0.04 | 0.21 ± 0.02* | 5 | Noncompetitive |
↵* Statistically significant differences (p < 0.01) from control (Students t test)