Since its discovery, serotonin (5-hydroxytryptamine = 5-HT) has become
a major player on the neurotransmitter ''stage''. Multiple receptor s
ubtypes for 5-HT have been identified and classified, and a vast pharm
acology of 5-HT has emerged. In particular, 5-HT has been shown to exe
rt marked effects on the cardiovascular system, central nervous system
(CNS) and gastrointestinal (GI) tract, and important ligands have bee
n developed that mimic or block its action selectively. Furthermore, d
rugs that release 5-HT, and others that prevent its uptake, have been
developed. This brief review focuses on the pharmacology of 5-HT agoni
sts and antagonists that exhibit, at least partly, clinical relevance.