In vitro binding affinities (mean Ki values with indication of 95% confidence limits in parentheses) of JNJ-37822681 and reference antipsychotics for various neurotransmitter receptors
| Receptor | JNJ-37822681 | Aripiprazole | Haloperidol | Ziprasidone | Risperidone | Olanzapine | Clozapine | Quetiapine | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ki | n | Ki | n | Ki | n | Ki | n | Ki | n | Ki | n | Ki | n | Ki | n | |
| nM | nM | nM | nM | nM | nM | nM | nM | |||||||||
| D2L | 158 (132–190) | 5 | 0.49 (0.2–1.2) | 7 | 1.8 (1.3–2.3) | 10 | 4.1 (2.8–5.9) | 7 | 5.5 (5.1–5.9) | 133 | 57 (35–93) | 9 | 137 (112–168) | 9 | 554 (419–733) | 6 |
| hD1 | >3000 | 1 | 653 | 1 | 65 | 1 | 41 | 1 | 147 (117–186) | 12 | 16 | 1 | 140 | 1 | 803 | 1 |
| hD3 | 1159 | 1 | 4.5 | 1 | 5.1 (3.3–8) | 6 | 23 (18–29) | 3 | 17 (15–19) | 30 | 55 (36–84) | 6 | 231 (176–304) | 4 | 844 (634–1123) | 10 |
| hα1A | >5000 | 3 | 211 (76–582) | 2 | 122 (41–363) | 4 | 32 (15–66) | 3 | 4.8 (2.6–9.5) | 8 | 189 (100–356) | 5 | 28 (19–41) | 3 | 200 (172–234) | 4 |
| hH1 | 4931 | 1 | 5.08 (3.5–7.4) | 3 | >5000 | 2 | 72 (45–116) | 2 | 67 (61–74) | 13 | 3.3 (2.8–4.0) | 2 | 1.5 (1.2–2) | 3 | 7.4 (6.9–7.9) | 2 |
| h5-HT2A | 2896 (2064–4062) | 2 | 16 (15–17) | 2 | 311 (159–609) | 6 | 1.9 (0.9–4.1) | 6 | 0.66 (0.53–0.82) | 26 | 3.8 (2.6–5.7) | 12 | 8.5 (4.9–13) | 8 | 318 (161–627) | 7 |
| h5-HT2C | >4000 | 2 | 14 (11–18) | 2 | >4000 | 1 | 7.4 (5.7–10) | 3 | 13 (12–14) | 30 | 12 (9.2–15) | 4 | 12 (8.6–15) | 5 | 2197 (1422–3395) | 3 |