Table 1.

Monoamine Transporter Binding Properties of 3β-(Substituted phenyl)tropane-2β-carboxylic Acid Methyl Esters

				DAT, IC50b (nM)	5-HTT, Kib (nM)	NET, Kib (nM)	NET/DAT	NET/5-HTT
Compda	X	Y	R	[3H]12	[3H]paroxetine	[3H]nisoxetine	Ratioc	Ratiod
Cocaine				89.1	95	1990	22	21
6				0.82 ± 0.05	0.95 ± 0.04	21.8 ± 0.6	27	23
7a	H	H	CH3	6.5 ± 1.3	4.3 ± 0.5	1110 ± 64	171	258
7b	H	H	C2H5	92 ± 8	1.7 ± 0.4	1690 ± 50	18	994
7c	F	H	CH3	16 ± 1	4.8 ± 0.5	270 ± 50	17	56
7d	Br	H	CH3	47 ± 15	3.1 ± 0.1	160 ± 20	3	52
7f	Br	Br	CH3	92 ± 22	2.9 ± 0.1	4100 ± 400e	45	1413
7e	I	H	CH3	170 ± 60	3.5 ± 0.4	180 ± 20	1	51
7g	I	I	CH3	1300 ± 200	7.5 ± 0.8	>5000	4	667

^aAll compounds were tested as the HCl salt.

^bAll values are means ± standard error of three or four experiments performed in triplicate.

^cNET/DA are ratios of K_i/IC₅₀ values.

^dNET/5-HTT are ratios of K_i values.

^eN=2.