ABSTRACT

The success of neuroleptic drugs in the treatment of schizophrenia since their introduction in 1952 has initiated much research into the biochemical actions of these antipsychotic agents in the brain. Many researchers now believe that neuroleptic drugs such as the phenothiazines and butyrophenones exert their actions at sites which are involved with the specific schizophrenic disturbance itself. Thus it has been hypothesized, very hopefully, that if one understood the biochemical mechanism of action of these drugs one might gain insight into the organic abnormalities responsible for the disease process. The neuronal recognition sites to which neuroleptics bind to produce their therapeutic action (and many of their side effects) appear to be receptors for the neurotransmitter dopamine. Thus, while this chapter focuses on neuronal binding sites for neuroleptics, they will be discussed with respect to their association with dopamine receptors. In fact, neuroleptic binding has evolved as one of the major tools for the study and identification of dopamine receptors.