Table 2

Pharmacological characterization of dopamine transporter with multiple mutations

	[³H]Dopamine Uptake		Dopamine Competition		[³H]CFT Binding		[³H]Dopamine UptakeV_max	[³H]CFT BindingB_max
	K_m	% of WT	K_i	% of WT	K_D	% of WT	[³H]Dopamine UptakeV_max	[³H]CFT BindingB_max
	μM		μM		nM		fmol/μg/min	fmol/μg
WT	2.2 ± 0.6	100	0.37 ± 0.14	100	20.9 ± 7.4	100	255.3 ± 9.0	6.3 ± 0.6
T4	0.9 ± 0.1^2-150	41	0.23 ± 0.01	62	46.9 ± 3.7^**	224	62.3 ± 27.8^***	6.6 ± 1.0
T5	3.8 ± 0.8^2-150	173	0.78 ± 0.47	211	60.7 ± 12.6^**	290	3.9 ± 2.0^***	5.8 ± 0.7
F361A	1.5 ± 0.4	68	0.39 ± 0.12	105	36.8 ± 7.0	176	145.1 ± 44.7^***	6.2 ± 0.6
T11	1.1 ± 0.1^2-150	50	0.16 ± 0.01	43	25.2 ± 2.4	121	136 ± 15.2^***	6.0 ± 0.2
T4 + 5	44 ± 11.8^***	2000	6.0 ± 1.9^**	1622	100.0 ± 30.6^**	478	5.5 ± 4.4^***	4.8 ± 0.5^2-150
T4 + F	1.1 ± 0.2^2-150	50	0.34 ± 0.31	92	62.0 ± 6.6^***	297	48.2 ± 34.8^***	6.9 ± 0.2
T4 + 11	0.5 ± 0.1^**	23	0.036 ± 0.023^2-150	10	120.3 ± 35.9^***	576	19.9 ± 12.7^***	5.9 ± 0.3
T5 + F	3.5 ± 0.6^2-150	159	0.59 ± 0.26	159	101.2 ± 19.7^***	484	4.1 ± 0.8^***	5.4 ± 0.1^2-150
T5 + 11	0.4 ± 0.1^**	18	0.025 ± 0.016^**	7	80.6 ± 17.4^***	386	0.6 ± 0.4^***	6.1 ± 0.4
F + T11	0.7 ± 0.1^**	32	0.048 ± 0.023^2-150	13	70.7 ± 3.2^***	338	46.8 ± 34.4^***	6.3 ± 0.1
T4 + 5 + F	13 ± 1.3^***	591	4.80 ± 3.3^2-150	1297	146.1 ± 15.3^***	699	68.7 ± 3.5^***	5.9 ± 0.1
T4 + 5 + 11	0.5 ± 0.1^**	23	0.054 ± 0.02^2-150	15	62.4 ± 11.2^***	299	0.1 ± 0.5^***	4.0 ± 0.9^2-150
T5 + F + 11	0.7 ± 0.1^**	32	0.080 ± 0.011^2-150	22	157.0 ± 57^**	751	1.1 ± 0.1^***	6.2 ± 0.3
T4 + F + 11	5.9 ± 1.4^**	268	2.6 ± 1.6^2-150	703	64.5 ± 11.4^***	309	9.0 ± 2.0^***	4.9 ± 0.6^2-150
T4 + 5 + F + 11	8.6 ± 1.1^***	391	2.6 ± 1.0^**	703	85.5 ± 3.9^***	409	5.4 ± 2.4^***	3.5 ± 1.3^2-150

Values are the mean ± S.D. of three independent experiments, each performed in duplicate determinations.
↵2-150 P < .5 versus WT. ** P < .01 versus WT. *** P < .001 versus WT.