Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency

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Abstract
The potencies of 22 neuroleptic drugs competing for binding sites associated with dopamine, serotonin, .alpha.-adrenergic and histamine receptors in [rat] brain membranes were studied. Although many neuroleptics are quite potent in competing at several of these receptor sites, the average antipsychotic clinical potency correlates closely only with the drug affinity for dopamine receptors labeled by 3H-spiroperidol. At clinically effective doses, however, substantial occupancy of serotonin, .alpha.-adrenergic and histamine receptors often occurs and may account for some of the auxiliary actions of neuroleptics.