5‐HT2C receptor antagonists: Potential in schizophrenia

The therapeutic success of clozapine and other so‐called atypical antipsychotics has focused attention on the serotonin (5‐hydroxytryptamine; 5‐HT) system and its interaction with the dopaminergic system as a treatment for psychotic illnesses. Clozapine has been shown to display high affinity for the 5‐HT2 receptor family and it has been suggested that this, together with evidence that dopamine D2 receptor blockade following clozapine treatment is lower than typical antipsychotics, contributes to the therapeutic profile of clozapine and, in particular, its efficacy in treating the negative symptoms of schizophrenia. Much attention has concentrated on the interaction of clozapine and atypical antipsychotics with the 5‐HT2A receptor. In this review, we focus on the role of the 5‐HT2C receptor in both the therapeutic profile of atypical antipsychotics and in the regulation of the dopaminergic system. We further suggest that 5‐HT2C receptor antagonists may have therapeutic utility in the treatment of psychotic illnesses. Drug Dev. Res. 54:88–94, 2001.