Table 1. In vitro uptake inhibition, release and affinity data for aminorex and its analogs.

Aminorex
DAT			NET			SERT			Reference	Cell system
Inhibition IC50 in nM	Release EC50 in nM	Affinity Ki in nM	Inhibition IC50 in nM	Release EC50 in nM	Affinity Ki in nM	Inhibition IC50 in nM	Release EC50 in nM	Affinity Ki in nM
--	9.1±0.9	--	--	15.1±3.5	--	--	414±78	--	Brandt et al.134	Rat brain synaptosomes
710±1050	--	--	1970±1200	--	--	26,290 ±1,030	--	--	Hofmaier et al.117	HEK293 cells
[Ki = 216±7]	--	784±16	--	--	--	[Ki = 1,244±106]	--	27,700±990	Rothman et al.43	Rat brain synaptosomes
[Ki = 216±7]	49.4±7.5	--	[Ki = 54.5±4.8]	26.4±2.8	--	[Ki = 1,244±106]	193±23	--	Rothman et al.111,180,185,186	Rat brain synaptosomes
--	--	--	--	--	--	[Ki = 1,380]	[% above basal flow: 51-116]	--	Tao et al.187	Rat brain tissue
4-methylaminorex
--	1.7±0.2	--	--	4.8±0.9	--	--	53.2±6.8	--	Brandt et al.134	Rat brain synaptosomes ((±)-cis-4-MAR)
4,4’-dimethylaminorex
--	8.6±1.1	--	--	26.9±5.9	--	--	18.5±2.8	--	Brandt et al.134	Rat brain synaptosomes ((±)-cis-4,4’-DMAR)
1040 (95% CI: 848 to 1282)	--	533.8±44.2	500 (95% CI: 447 to 553)	--	266.8±57	1750 (95% CI: 1446 to 2126)	--	1881±183.1	Maier et al.135	HEK293 cells ((±)-cis-4,4’-DMAR)
--	10.9±0.7	--	--	11.8±2.0	--	--	17.7±2.3	--	McLaughlin et al.148	Rat brain synaptosomes ((±)-cis-4,4’-DMAR)
--	24.4±2.7	--	--	31.6±4.6	--	--	59.9±17.2	--	McLaughlin et al.148	Rat brain synaptosomes ((±)-trans-4,4’-DMAR)