Table 1.
Degree of receptor occupancy for antipsychotic drugs and the parameters involved
| Receptor systems | ||||||||
|---|---|---|---|---|---|---|---|---|
| Dopaminergic (D2) | Serotonergic (5‐HT2A) | Muscarinic (M1) | ||||||
| FGAPs & SGAPs | C'T* (ng ml–1) | fu (%) | Ki (nM) | Degree (%) | Ki (nM) | Degree (%) | Ki (nM) | Degree (%) |
| Chlorpromazine | 300 | 4.0 | 50.12 | 42.94 | 7.94 | 82.61 | 30.83 | 55.03 |
| Fluphenazine | 10 | 5.0 | 1.45 | 44.10 | 31.62 | 3.49 | 1093.96 | 0.10 |
| Haloperidol | 10 | 8.0 | 7.94 | 21.17 | 100.00 | 2.09 | >10 000.00 | 0.02 |
| Loxapine | 30 | 3.0 | 7.76 | 28.66 | 7.94 | 28.20 | 105.68 | 2.87 |
| Perphenazine | 2 | 7.0 | 0.60 | 40.99 | 6.31 | 6.19 | 2000.00 | 0.02 |
| Pimozide | 20 | 1.0 | 12.59 | 3.33 | 39.81 | 1.08 | 800.00 | 0.05 |
| Prochlorperazine | 40 | 5.0 | 3.63 | 59.62 | 15.00 | 26.33 | 547.78 | 0.97 |
| Thioridazine | 200 | 5.0 | 14.59 | 64.93 | 19.95 | 57.52 | 6.22 | 81.29 |
| Thiothixene | 15 | 1.0 | 1.40 | 19.47 | 50.12 | 0.67 | 2600.00 | 0.01 |
| Trifluoperazine | 2 | 1.0 | 1.11 | 4.84 | 12.59 | 0.45 | 663.33 | 0.01 |
| AMISULPRIDE | 320 | 84.0 | 12.59 | 98.30 | 8304.00 | 8.06 | >10 000.00 | 6.79 |
| ARIPIPRAZOLE | 500 | 1.0 | 0.79 | 93.40 | 15.85 | 41.37 | 6776.42 | 0.16 |
| ASENAPINE | 5 | 5.0 | 1.20 | 42.22 | 0.06 | 93.60 | 8128.31 | 0.01 |
| CLOZAPINE | 600 | 5.0 | 446.68 | 17.08 | 5.01 | 94.83 | 6.59 | 93.31 |
| ILOPERIDONE | 10 | 5.0 | 5.94 | 16.49 | 0.35 | 77.02 | 4897.79 | 0.02 |
| MELPERONE | 100 | 50.0 | 152.00 | 55.54 | 180.00 | 51.33 | >10 000.00 | 1.86 |
| OLANZAPINE | 80 | 7.0 | 2.09 | 89.57 | 1.78 | 90.97 | 11.38 | 61.19 |
| PALIPERIDONE | 60 | 26.0 | 5.01 | 87.96 | 0.79 | 97.89 | 8800.00 | 0.41 |
| QUETIAPINE | 500 | 17.0 | 63.10 | 77.85 | 199.53 | 52.65 | 240.44 | 47.99 |
| RISPERIDONE | 60 | 11.0 | 0.44 | 97.34 | 0.22 | 98.65 | >10 000.00 | 0.16 |
| SERTINDOLE | 100 | 0.5 | 3.31 | 25.55 | 0.50 | 69.44 | >10 000.00 | 0.01 |
| ZIPRASIDONE | 200 | 0.1 | 2.82 | 14.68 | 0.70 | 40.94 | 6081.35 | 0.01 |
| ZOTEPINE | 150 | 3.0 | 10.97 | 55.34 | 2.51 | 84.41 | 1342.77 | 1.00 |
C'T*, total plasma concentration of a drug; FGAPs, first‐generation antipsychotic drugs; SGAPs, second‐generation antipsychotic drugs (SGAP written in upper case letters); fu, free fraction of a drug in the plasma; Ki, equilibrium dissociation constant