Skip to main content
. Author manuscript; available in PMC: 2014 Dec 12.
Published in final edited form as: J Med Chem. 2013 Dec 2;56(23):9709–9724. doi: 10.1021/jm4014136

Table 2.

Binding Data for 5- and 4’-substituted analogues of 1a

graphic file with name nihms542609t17.jpg
Compd Structure R R’ SERT
Ki±SEM (nM)
NET
Ki±SEM (nM)
Ki
(NET)/Ki
(SERT)
24 B CN Br 50.9±3.89 17% b >10,000
25 A CN Br 11.4±0.74 45% b
26 A CN graphic file with name nihms542609t18.jpg 38.0±4.21 44% b >10,000
27 A CN graphic file with name nihms542609t19.jpg 51.5±6.63 2800±353 54
28 A CN graphic file with name nihms542609t20.jpg 125±15.2 7020±581 56
37 C _ _ 681±88.2 4970±738 7.3
a

These novel analogues were assessed by radioligand binding displacement of [3H]1 (for SERT) and [3H]nisoxetine (for NET) in rat brain stem and frontal cortex, respectively.35

b

% Displacement at 10 µM.