Serotonin (5-HT) is a neurotransmitter in the central nervous system (eNS) of vertebrates and invertebrates. In vertebrates, 5-HT participates in the regulation of various physiologic functions, including pain perception, blood pressure, sleep, homeothermia, and sexual activity. It is also believed that 5-HT may participate in the expression of symptoms of certain psychiatric disorders, such as depression and anxiety. In this context, most of our knowledge concerning the participation of S-HT and 5-HT receptors in psychopathology has come from the characterization of the mechanisms of action of various drugs that are effective in relieving the symptoms of psychiatric disorders. That the 5-HT receptor population in the periphery might be heterogeneous was fIrst suggested by the early pioneering work of two independent groups (Rocha e Silva et a1. 1953; Gaddum and Hameed 1954). It was not until the late 1970s, however, that Peroutka and Snyder (1979) described, in the eNS, the existence of two different 5-HT recognition sites labeled by lysergic acid diethylamine, the serotonin-1 (5-HT1) and the serotonin-2 (5-HT2) binding sites. © 1993 American College of Neuropsychopharmacology.