Table 3.
Receptor binding profiles of aripiprazole (5) and other dopamine partial agonists as atypical antipsychotics.
| Receptor Ki (nM) 1 | Aripiprazole (5) 3 | Brexpiprazole (6) 4 | Cariprazine (40) 5 |
|---|---|---|---|
| D2 | 0.34 | 0.30 | 0.49 |
| D1 | 1960 | 160 | NA |
| D3 | 0.8 | 1.1 | 0.085 |
| D4 | 44 | 6.3 | NA 2 |
| D5 | 2590 | NA | NA |
| 5-HT1A | 1.7 | 0.12 | 2.6 |
| 5-HT2A | 3.4 | 0.47 | 18.6 |
| 5-HT2C | 15 | 34 | 135 |
| α1A adrenergic | 26 | 3.8 | 132 |
| α1B adrenergic | 35 | 0.17 | >1000 |
| H1 histaminergic | 61 | 19 | 23.4 |
| M1 muscarinic | 6780 | 67% inhibition at 10 μM | NA |
1Receptor binding affinities were obtained from the NIMH Psychoactive Drug Screening Program (PDSP) Database [61].2NA stands for not available. 3 Data from the cited literatures [108, 120]. 4 Data from the cited literatures [121, 122]. 5 Data calculated based upon the pKi reported in the cited literature [118].