Antagonists of the serotonin 5-HT3 receptor are clinically effective a
ntinausea and anti-emetic drugs for the treatment of cancer patients u
ndergoing chemotherapy and for patients undergoing procedures involvin
g general anaesthesia. These compounds have also been evaluated for th
e treatment of irritable bowel syndrome, other pain-related disorders
(including migraine) and a variety of central nervous system disorders
(including anxiety, psychosis and the treatment of drug abuse). The s
tatus of research into potential clinical applications of these drugs
is evaluated in this review. The evidence from preclinical and clinica
l studies is compared and avenues for future drug development using th
ese compounds are discussed.