Table 3. [³H]DA Uptake Inhibition Potency for Selected Analogues Measured in Intact COS7 Cells Expressing the Human DAT Wild Type or the A480T Mutant^a.

compd	hDAT-WT Ki [SE interval] (nM)	n	hDAT-A480T Ki [SE interval] (nM)	n
DA (KM)	1160 [980–1380]	9	1930 [1510–2480]	5
(±)-1	13000 [10000–17000]	6	3090 [2300–4200]	3
4g	5500 [4000–7600]	4	3600 [2010–6300]	3
4h	3700 [2700–5100]	5	2300 [1700–3100]	3
6a	390 [280–540]	3	720 [620–830]	4
6b	1210 [960–1510]	5	1370 [1240–1510]	3

^aThe inhibition potency for [³H]dopamine (DA) uptake was calculated from nonlinear regression analysis of uptake experiments performed on COS7 cells transiently transfected with cDNA of the human dopamine transporter (hDAT) wild type (WT) or the Ala480 to Thr mutant (A480T). The IC₅₀ values used in the calculation of K_M and K_i were calculated from the means of pIC₅₀, and the indicated SE intervals were calculated from pIC₅₀ ± SE. Nonspecific uptake was determined using 50 μM nomifensine.