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Studies in experimental models have suggested a potential role for serotonergic transmission in epilepsy, and interest in this research has been increased by the development of positron emission tomography (PET) ligands that can be used to study 5-hydroxytryptamine (5-HT) receptors and transporters. The serotonergic system is very complex. At least 13 distinct G protein-coupled 5-HT receptors and one ligand-gated ion channel receptor (5-HT(3)) are divided into seven distinct classes (5-HT(1) to 5-HT(7)) ((1)). The receptors vary widely in their distribution and effects, innervating vascular structures and gut smooth muscle as well as neuronal tissue. Several receptor subtypes may be relevant to epilepsy.