Table 3.
Binding Data for Aryl Piperazine Analogs at Dopamine and Serotonin Receptors of Interest.
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|---|---|---|---|---|---|---|---|---|
| Compounds | Binding (Ki ± SEM) data of aryl piperazine analogs at selected receptors (nM) | |||||||
| Compd # | X | Ar | D2 | D3 | D4 | 5HT1A | 5HT2A | 5HT2C |
| 19 | C=O | 2-Pyrimidine | 98.0 ± 15.0 | 244.1 ± 106.0 | 6.5 ± 0.8 | 30.5 ± 5 | 22.0 ± 4.0 | 4132 ± 1081 |
| 20 | CH2 | 2-Pyrimidine | 269 ± 17 | 262 ± 17 | 6.2 ± 0.3 | 8.6 ± 0.7 | 41.0 ± 2.0 | MP |
| 21 | S | 2-Pyrimidine | 424 ± 25 | 68.0 ± 10.0 | 21.0 ± 1.0 | 93.1 ± 29.0 | 27.0 ± 2.0 | 8829 ± 2674 |
| 22 | O | 2-Pyrimidine | 636 ± 66 | 778 ± 63 | 4.2 ± 0.1 | 23.0 ± 3.0 | 23.0 ± 1.0 | >10000 |
| 23 | CH2 | 2-Pyridine | 124 ± 10 | 86.0 ± 4.0 | 3.5 ± 0.2 | 1.1 ± 0.1 | 50.0 ± 3.0 | MP |
| 24 | S | 2-Pyridine | 183 ± 21 | 160 ± 16 | 5.7 ± 0.3 | 6.2 ± 0.5 | 26.0 ± 1.0 | 8097 ± 495 |
| 25 | O | 2-Pyridine | 186 ± 16 | 229 ± 20 | 1.8 ± 0.1 | 3.6 ± 0.2 | 18.0 ± 1.0 | 8277 ± 497 |
MP = Missed primary assay threshold of 50% inhibition,
