The serotonin 5-HT, receptor is unique among the seven serotonin recep
tor ''families'' that have been recognized so far. It functions nor as
a G-protein coupled but as a direct ion channel gated receptor. Becau
se of the varied neural functions linked to this receptor, intensive r
esearch interest has developed in recent years about its basic and cli
nical pharmacology, which are summarized in this review. Some new agon
ists and many new antagonists have been developed. These agents have a
useful role as selective pharmacologic research probes, and some of t
hem con be used therapeutically as potent and selective antinausea and
antiemetic drugs, particularly in patients undergoing cancer chemothe
rapy treatment or general anesthesia procedures. Potential application
s of these agents include the treatment of some behavioral disorders i
n mental disease, drug addiction, and certain types of pain syndromes.