Profiles for the affinity of antipsychotic drugs for neurotransmitter receptors and their clinical implication

Abstract

The binding affinities of 12 different neurotransmitter receptors were measured using a radio-labeled receptor assay. The profiles of the pharmacological affinities of 20 antipsychotic drugs were assessed. Based on the Ki values of the D2 receptor, 5HT2 receptor, and α1 receptor, the antipsychotic drugs were classified into five groups (i.e., three anti-DA activity predominant groups and two anti-5HT activity predominant groups). A theoretical basis for drug choice in clinical settings is also proposed. We recommend that the groups of the drugs having predominantly anti-DA activity be used in the treatment of hallucinations and delusions and that the drugs in the anti-5HT activity predominant group be used to treat hypobulia. If it is necessary to administer two or more of these drugs together, we propose that they should be drugs with different profiles. Extrapyramidal symptoms, side effects of antipsychotic drugs, were interpreted in terms of interaction among the anti-D2 activity, anti-5HT2 activity, and anti-Ach activity.