Dopamine receptors, neuroleptics, and schizophrenia

The antipsychotic effects of neuroleptic drugs are mediated by dopamine DA-2 receptors, and dopamine DA-1 receptors, linked to cyclic AMP formation, are not involved. Dopamine receptor binding is enhanced in brain specimens of deceased schizophrenic patients, an increase which may relate to chronic neuroleptic treatment. The binding of 3H-butyrophenones to dopamine receptors can be used for a radioreceptor assay that detects blood levels of all clinically used neuroleptics and their pharmacologically active metabolites and may facilitate routine monitoring of blood levels.