TABLE 1

Dopamine uptake inhibition potencies and binding affinities of structurally diverse DAT inhibitors at CHO cells stably expressing WT or D79E DAT

	K_i
	WT	D79E
	nM
[³H]Dopamine uptake
WIN 35,428^a	74 ± 17	71 ± 12
4-ARA-127	1630 ± 200	1540 ± 120
Cocaine^a	555 ± 29	1126 ± 32^b
8-Oxa-norcocaine	9777 ± 1489	8196 ± 340
Mazindol^a	31 ± 3	47 ± 4
Methylphenidate^a	152 ± 20	161 ± 9
Benztropine	160 ± 37	19 ± 3^b
GBR-12,909	15 ± 3	14 ± 3
Rimcazole	643 ± 43	691 ± 76
[³H]WIN 35,428 inhibition
WIN 35,428^a	20 ± 1^c	68 ± 4^b
4-ARA-127	3300 ± 40^c	1570 ± 210^b
Cocaine^a	128 ± 5^c	1066 ± 84^b
8-Oxa-norcocaine	1564 ± 212^c	5533 ± 653^b^,^c
Mazindol^a	13 ± 1^c	41 ± 3^b
Methylphenidate^a	57 ± 3^c	167 ± 2^b
Benztropine	127 ± 22	51 ± 5^b^,^c
GBR-12,909	31 ± 5	40 ± 9
Rimcazole	180 ± 26^c	226 ± 38^c

↵ a Data from Wang et al. (2003).
↵ b p < 0.05 vs. WT DAT for that assay.
↵ c p < 0.05 for WIN inhibition vs. dopamine uptake at the same DAT construct.