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. Author manuscript; available in PMC: 2010 Mar 18.
Published in final edited form as: J Med Chem. 2008 Dec 25;51(24):8048–8056. doi: 10.1021/jm801162z

Table 2.

Monoamine Transporter Binding Properties of 3β-(4-Methoxyphenyl)tropane-2β-carboxylic Acid Ester Analogs

graphic file with name nihms179528u2.jpg
DAT, IC50b (nM) 5-HTT, Kib (nM) NET, Kib (nM) NET/DAT NET/5-HTT
Compda R [3H]12 [3H]paroxetine [3H]nisoxetine Ratioc Ratiod
7a CH3 6.5 ± 1.3 4.3 ± 0.5 1110 ± 64 171 258
8a (CH3)2CH 14 ± 3 135 ± 35 2010 ± 200 144 15
8b graphic file with name nihms179528t1.jpg 6.0 ± 2 29 ± 3 1230 ± 140 205 42
8c graphic file with name nihms179528t2.jpg 13 ± 3 100 ± 8 >3000 231 30
8d graphic file with name nihms179528t3.jpg 42 ± 8 2.9 ± 0.2 330 ± 20 8 114
8e graphic file with name nihms179528t4.jpg 7.0 ± 2 8.3 ± 0.4 2200 ± 300e 314 265
8f graphic file with name nihms179528t5.jpg 6.0 ± 1 5.5 ± 0.5 1460 ± 30 243 265
8g graphic file with name nihms179528t6.jpg 3.3 ± 1.4 4.1 ± 0.6 1850 ± 90 561 451
8h graphic file with name nihms179528t7.jpg 15 ± 6 2.0 ± 0.4 2710 ± 250e 181 1360
8i graphic file with name nihms179528t8.jpg 2.5 ± 0.7 3.5 ± 1 2040 ± 300e 816 583
8j graphic file with name nihms179528t9.jpg 102 ± 15 1.0 ± 0.1 2600 ± 200e 25 2600
9 18 ± 6 860 ± 170 >3000 167 3
a

All compounds were tested as the HCl salt.

b

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

c

NET/DAT are ratios of Ki/IC50 values.

d

NET/5-HTT are ratios of Ki values.

e

N=2.