Significant advances in the molecular pharmacological analysis of 5-hydroxytryptamine (5-HT) receptor subtypes occurred in the 1980's. To a significant degree, this progress resulted from 2 independent approaches: molecular biology and molecular pharmacology. This review focuses on the pharmacological data derived from radioligand binding studies. At the present time, 5-HT receptor subtypes are often categorized into at least 3 major "families" as well as a few "orphan" receptors that cannot yet be placed into the major categories. Each "family" consists of multiple receptor subtypes which share similarities in their molecular biological, pharmacological, biochemical and physiological properties. In order to provide a comparative pharmacological analysis of the 7 most extensively characterized 5-HT receptor subtypes, potency information is presented on the 30 pharmacological agents that have been, to date, studied most extensively in the published literature.