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. Author manuscript; available in PMC: 2013 Feb 1.
Published in final edited form as: Bioorg Med Chem. 2011 Dec 22;20(3):1291–1297. doi: 10.1016/j.bmc.2011.12.019

Table 1.

Binding of Phenyl Piperidine Analogs at Dopamine and Serotonin Receptors of Interest.

graphic file with name nihms346421t1.jpg
Compounds Binding (Ki ± SEM) data of phenyl piperazine analogs at selected receptors (nM)
# X Y D2 D3 D4 5HT1A 5HT2A 5HT2C
Cloza 130 240 54 140 8.9 17
Hal, 1a C=O COH 0.89 4.6 10 3600 120 4700
5 CH2 COH 24 ± 2 666 ± 39 1.5 ± 0.1 658 ± 50 302 ± 23 MP
6 S COH 8.8 ± 9.5 49.0 ± 1.7 247.8 ± 4.3 317 ± 29 72 ± 7 >10000
7 O COH 5.3 ± 0.3 182 ± 22 2.4 ± 0.1 74.0 ± 6 93 ± 10 MP
8 S CH 185 ± 13 130 ± 14 39 ± 3 454 ± 92 112 ± 17 >10000
9 O CH 41 ± 4 696 ± 50 9.5 ± 0.3 169 ± 15 121 ± 9 >10000
10 S=O CH 998 ± 68 243 ± 35 35 ± 1 613 ± 216 222 ± 17 >10000

MP = Missed primary assay threshold of 50% inhibition, Cloz, Clozapine; Hal, Haloperidol.

a

The binding data of these compounds were previously reported in Refs 7, 9 and 10.