Abstract
Abstract: Medicinal chemistry has played a major role in the improvement of antipsychotic therapy by helping to develop the 02/5-HT2 ratio hypothesis. Early pharmacological insights implicating a role for serotonin in schizophrenia by virtue of its control of the dopamine system have been tested by numerous combined 02/5-HT2 receptor antagonists. Recent work indicates that 5-HT2 receptor blockade can compensate for relatively weaker 02 receptor affinity, lessening the chance of side effects while maintaining antipsychotic efficacy. Many of the newer agents are poised to test the validity of the 02/5-HT2 ratio hypothesis in the clinic.
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