Table 2.
Neuroreceptor binding profiles of antipsychotics
| Drug | Ki D2 | Ki 5HT1A | Ki 5HT2A | Ki 5HT2C | Ki α1 | Ki α2 | Ki H1 | Ki M2 |
|---|---|---|---|---|---|---|---|---|
| CPZ | 3 | 2,115 | 4.06 | 32.5 | 2.6 | 750 | 3 | 244 |
| HAL | 2.6 | 1,800 | 61 | 4,700 | 17 | 600 | 260 | >10,000 |
| LOX | 9.8 | NA | 2 | NA | 250 | NA | 14.9 | NA |
| MOL | 120 | 3,797 | 5,000 | >10,000 | 2,500 | 625 | >10,000 | NA |
| PER | 1.4 | 421 | 5 | 132 | 10 | 500 | 8 | NA |
| AMI | 1.3 | >10,000 | 2,000 | >10,000 | 7,100 | 1,600 | >10,000 | NA |
| ARI | ±0.7 | ±5.5 | 8.7 | 22 | 26 | 74 | 30 | 3,510 |
| ASE | 1.3 | 2.5 | 0.06 | 0.03 | 1.2 | 1.2 | 1 | >10,000 |
| BRE | ±0.3 | ±0.12 | 0.47 | NA | 3.8 | 0.59 | 19 | NA |
| CAR | ±0.5 | ±2.6 | 18.8 | 134 | 155 | NA | 23.2 | >10,000 |
| CLO | 210 | 160 | 2.59 | 4.8 | 6.8 | 158 | 3.1 | 204 |
| ILO | 6.3 | 168 | 5.6 | 14 | 4.7 | 4.7 | 437 | 3,311 |
| LUR | 1 | ±6.4 | 0.5 | NA | NA | 11 | >10,000 | >10,000 |
| OLA | 20 | 610 | 1.5 | 4.1 | 44 | 280 | 0.1 | 622 |
| PALI | 2.8 | 480 | 1.2 | 48 | 10 | 80 | 3.4 | >10,000 |
| RIS | 3.8 | 190 | 0.1 | 32 | 2.7 | 8 | 5.2 | >10,000 |
| QUE | 770 | 300 | 31 | 3,500 | 8.1 | 80 | 19 | 630 |
| SER | 2.7 | 2,200 | 0.14 | 6 | 3.9 | 190 | 440 | NA |
| ZIP | 4.8 | ±3.4 | 0.4 | 1.3 | 10 | 154 | 4.6 | >3,000 |
| Effects related to receptor blockade | ||||||||
| EPS, hyperprolactinemia, sexual dysfunction, and cognitive dysfunction | Anxiolytic and antidepressant effects | Lower incidence of akathisia and parkinsonism | Weight gain and metabolic effects | Hypotension, priapism, retrograde ejaculation, and low libido | Antidepressant | Appetite, sedation, cognitive dysfunction, and weight gain | Cognitive dysfunction, urinary retention, glaucoma, constipation, and dry mouth | |
Notes: Lower Ki (ie, nanomolar concentration at which 50% of the respective receptor type is occupied) means higher affinity. Light gray, FGAs; ±, partial agonism for the specific receptor. Italics represent FGAs. Data from Correll.35
Abbreviations: CPZ, chlorpromazine; HAL, haloperidol; LOX, loxapine; NA, not applicable; MOL, molindone; PER, perphenazine; AMI, amisulpride; ARI, aripiprazole; ASE, asenapine; BRE, brexpiprazole; CAR, cariprazine; CLO, clozapine; ILO, iloperidone; LUR, lurasidone; OLA, olanzapine; PALI, paliperidone; RIS, risperidone; QUE, quetiapine; SER, sertindole; ZIP, ziprasidone; EPS, extrapyramidal symptoms; FGAs, first-generation antipsychotics; FGA, first-generation antipsychotics.