Table 5.
Off-target binding affinities of cariprazine-based analogues.a
| compound | Ki ± SEM (nM) | |||||
|---|---|---|---|---|---|---|
| D1Rb | D4Rc | 5-HT1Ad | 5-HT2Ae | 5-HT2Be | 5-HT2Ce | |
| cariprazine | 2920 ± 300 | 233 ± 20 | 1.81 ± 0.46 | 568 ± 72 | 0.151 ± 0.023 | 221.1 ± 8.0 |
| 11a | >3160 | 1390 ± 480 | 184 ± 25 | 1810 ± 640 | 1.99 ± 0.62 | 644 ± 58 |
| 13a | 4600 ± 400 | 756 ± 63 | 6.0 ± 1.8 | 54 ± 15 | 1.47 ± 0.36 | 252 ± 64 |
| 11b | 5390 ± 730 | 417 ± 40 | 75 ± 25 | 15.1 ± 4.8 | 1.27 ± 0.39 | 253 ± 86 |
| 13b | 6800 ± 480 | 342 ± 15 | 7.7 ± 1.8 | 20.8 ± 6.9 | 1.71 ± 0.43 | 34.0 ± 8.1 |
| 6c | >10000 | 1257 ± 23 | 33.8 ± 5.9 | >10000 | 34.2 ± 9.3 | >10000 |
| 13c | >10000 | 734 ± 16 | 69.9 ± 1.7 | >10000 | 29.6 ± 9.5 | >10000 |
| 11d | >3160 | 1790 ± 430 | 22.3 ± 6.4 | 1450 ± 340 | 18.8 ± 6.2 | 5800 ± 1300 |
| 13d | >10000 | 2520 ± 170 | 9.6 ± 2.6 | 4420 ± 340 | 11.3 ± 2.2 | 3170 ± 200 |
| 6e | >10,000 | 2434± 87 | 45.4 ± 9.0 | 680 ± 200 | 7.3 ± 1.9 | 1062 ± 86 |
| 7e | 8000 ± 1100 | 1346 ± 29 | 54.9 ± 4.2 | 207 ± 74 | 6.2 ± 1.5 | 162 ± 48 |
| 13e | >10,000 | 1870 ± 240 | 108 ± 11 | 158 ± 45 | 5.8 ± 1.7 | 800 ± 280 |
a
Data were obtained through the NIDA Addiction Treatment Discovery Program Contract (ADA12013) with Oregon Health & Science University. The radioligands used in these assays were
b
[3H]-SCH23390,
c
[3H]-spiperone,
d
[3H]-8-OH-DPAT, and
e
[3H]5-HT.