TABLE 3

Effect of classic DAT inhibitors on CHO cells stably expressing WT or D79E DAT

Kd (WIN 35,428 only) and Ki values were derived from experiments incubating the stably-transfected cells with nonradioactive substrates in the presence of [3H]dopamine or [3H]WIN 35,428 at 22° C in KRH buffer. Values are presented as mean ± S.E. for three to six independent experiments. Note that values are nanomolar, whereas those in Table 2 are micromolar.

Kd or Ki
WT DAT D79E DAT
nM
[3H]DA uptake
WIN 35,428 74 ± 17 71 ± 12
Cocaine 555 ± 29 1126 ± 32a
Mazindol 31 ± 3 47 ± 4
Methylphenidate 152 ± 20 161 ± 9
[3H]WIN inhibition
WIN 35,428 20 ± 1b 68 ± 4a
Cocaine 128 ± 5b 1066 ± 84a
Mazindol 13 ± 1b 41 ± 3a
Methylphenidate 57 ± 3b 167 ± 2a
  • a P < 0.05 versus WT DAT for that assay (via Student's t test).

  • b P < 0.05 for WIN inhibition versus dopamine uptake at the same DAT construct (via Student's t test).