Serotonin receptor and reuptake sites: pharmacologic significance

The past decade has seen important advances in the clinical use of serotonergic agents. The authors summarize the current status of selective agents for 5-HT receptor subtypes and their utility in the treatment of human neuropsychiatric disorders. The putative novel anxiolytic effects of 5-HT1A partial agonists such as buspirone, the unique and potent antiemetic effects of 5-HT3 antagonists in cancer chemotherapy, and the antidepressant effects of selective 5-HT uptake blockers such as fluoxetine are excellent examples of the clinical relevance of selective 5-HT receptor agents. The increasing ability to modulate serotonergic neurotransmission via distinct serotonin (5-HT) receptor subtypes should greatly facilitate the analysis of the role of 5-HT in both normal and abnormal human brain function.