Binding affinities and functional actions of S18327 as compared to other antipsychotic agents
| pKi | pID50 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| hD1 | hD2 | hD3 | hD4 | h5-HT1A | h5-HT2A | h5-HT2C | hα1A | hα2A | ALOC | CAR | ACLM | DHTW | PLOC | DSTF | |
| μmol/kg | |||||||||||||||
| S18327 | 7.2 | 7.1 | 7.0 | 8.1 | 7.4 | 8.5 | 6.4 | 9.0 | 7.0 | −0.5 | −0.3 | 0.3 | 0.6 | 0.6 | −0.6 |
| Clozapine | 7.8 | 7.1 | 6.6 | 7.4 | 7.0 | 8.8 | 7.3 | 8.9 | 6.7 | −1.4 | −1.2 | −0.8 | 0.9 | 0.7 | −1.0 |
| Haloperidol | 8.5 | 9.4 | 8.5 | 8.8 | 5.7 | 7.1 | 5.0 | 8.2 | 4.7 | 0.9 | 0.7 | 1.4 | 0.7 | 0.7 | −0.4 |
| Amperozide | 6.7 | 6.3 | 6.4 | 5.6 | 5.5 | 8.2 | 5.6 | 7.4 | 5.9 | −1.1 | −1.2 | 0.1 | 0.0 | 0.1 | −0.3 |
| MDL100,907 | 6.6 | 5.5 | 4.9 | 6.2 | 5.0 | 9.2 | 7.6 | 6.6 | 5.0 | −1.4 | −0.8 | 0.7 | 1.9 | 2.6 | −0.8 |
| ORG5222 | 8.8 | 8.9 | 8.9 | 9.0 | 8.4 | 10.1 | 9.6 | 9.2 | 8.2 | 0.8 | 0.6 | 1.5 | 1.0 | 2.2 | 0.0 |
| Ocaperidone | 7.6 | 9.2 | 8.6 | 8.5 | 8.0 | 10.0 | 8.0 | 9.7 | 7.7 | 1.3 | 0.6 | 1.9 | 1.2 | 1.6 | 0.2 |
| Olanzapine | 7.9 | 8.2 | 7.5 | 7.6 | 5.8 | 8.9 | 8.1 | 7.7 | 5.9 | 0.003 | −0.3 | 0.6 | 1.9 | 2.2 | −1.0 |
| Quetiapine | 6.7 | 6.7 | 6.4 | 5.6 | 6.6 | 6.5 | 6.2 | 8.0 | 5.0 | −1.0 | −2.0 | −0.7 | −0.2 | 0.2 | −1.3 |
| Raclopride | 5.0 | 8.9 | 8.8 | 5.4 | 5.1 | 6.7 | 5.0 | 5.0 | 5.0 | 0.4 | 0.7 | 1.3 | 0.9 | 0.1 | −0.9 |
| Risperidone | 7.7 | 8.5 | 8.0 | 8.3 | 6.6 | 9.4 | 7.8 | 9.3 | 7.6 | 0.3 | −0.1 | 2.3 | 1.1 | 2.3 | −0.1 |
| Sertindole | 7.7 | 8.6 | 8.1 | 7.7 | 6.4 | 10.0 | 8.7 | 9.9 | 6.6 | −1.3 | −1.8 | 0.4 | −0.3 | 1.6 | −1.1 |
| Tiospirone | 7.4 | 8.7 | 8.6 | 8.3 | 8.4 | 9.3 | 8.3 | 9.6 | 6.7 | 0.6 | 0.5 | 1.2 | 0.4 | 2.0 | −0.3 |
| Ziprasidone | 8.5 | 8.3 | 7.9 | 7.8 | 8.9 | 9.5 | 8.7 | 8.9 | 6.4 | 0.4 | −0.9 | 0.9 | 0.4 | 1.1 | −0.9 |
ALOC, amphetamine locomotion; CAR, conditioned avoidance responses; ACLM, apomorphine-induced climbing; DHTW, DOI-induced head-twiches; PLOC, PCP-induced locomotion; DSTF, dizocilpine-induced spontaneous tail-flicks; pID50, log inhibitory dose50and pKi = −log Ki. Data from Millan et al., accompanying paper, 1998a and b and unpublished observations.