. Author manuscript; available in PMC: 2010 Mar 26.

Published in final edited form as: J Med Chem. 2009 Mar 26;52(6):1530–1539. doi: 10.1021/jm8010993

Table 2.

Inhibition of radioligand binding and [³H] neurotransmitter uptake in HEK-hDAT, HEK-hSERT and HEK-hNET cells^a.

		Binding (K_i, nM)			Reuptake (IC₅₀, nM)

Compound	Description	hDAT	hSERT	hNET	hDAT	hSERT	hNET
Cocaine		371 ± 81	276 ± 87	1115 ± 198	303 ± 74	416 ± 135	835 ± 229
Fluoxetine ^b		6670 ± 850	1.1 ± 0.5	1560 ± 300	19,500 ± 7600	7.3 ± 2.9	1020 ± 180
14	SSRI	6500 ± 828	2.1 ± 0.2	2440 ± 215	27850 ± 5129	2.5 ± 0.6	481 ± 158
15	SSRI	7307 ± 1331	1.1 ± 1.0	10600 ± 1880	16987 ± 1352	2.3 ± 0.6	1930.0 ± 463.0
19	PDE4 inhibitor	>100,000	>100,000	>100,000	>100,000	>100,000	1930.0 ± 463.0
20	N-modified PDE4 inhibitor	>100,000	>100,000	39,119 ± 4915	>100,000	>100,000	>100,000
21	Dual inhibitor	2478 ± 451	156 ± 30	1748 ± 257	3556 ± 377	127 ± 15	957 ± 146
22	Dual inhibitor	5340 ± 1083	194 ± 87	7441 ± 1269	5340 ± 1083	194 ± 87	7441 ± 1269
24	SSRI	66988 ± 14450	21.2 ± 4.3	19332 ± 3577	> 100,000	18.4 ± 6.1	20370 ± 3751

Values are the mean ± S.E.M. of three to four independent experiments conducted with duplicate (binding) or with triplicate (uptake) determinations unless the mean of three experiments exceeded 100 µM. Drug inhibition of [¹²⁵I]-25 binding in HEK-hDAT, HEK-hSERT, or HEK-hNET cell membranes. Inhibition of [³H]-DA, [³H]-5-HT, [³H]-NE in the presence of HEK-hDAT, HEK-hSERT, or HEK-hNET cells, respectively;

Data taken from reference ²⁰.