5-HT3 receptors and the therapeutic potential of 5-HT3 receptor antagonists.
5-HT3 receptors have been the focus of much research during the last decade. They are characterised by being located on neurones both peripherally and centrally; 5-HT3 agonists cause a rapid depolarisation of the membrane potential which results from the opening of cation channels; the 5-HT3 response rapidly desensitizes. 5-HT3 receptors appear to have a modulatory role on other neurotransmitters. The identification of selective agonists and antagonists for this receptor type has allowed the discovery of several important new therapeutic applications. The use of 5-HT3 receptor antagonists in psychoactive illnesses is being explored clinically. In addition, ondansetron, a selective 5-HT3 receptor antagonist, is already being used to prevent the severe nausea and vomiting caused by cancer chemotherapy and radiotherapy. The pharmacological properties of 5-HT3 antagonists are discussed in this chapter.
Tyers
M B
MB
Neuropharmacology Department, Glaxo Group Research Ltd, Ware, Herts, UK.
D000818:Animals; D006168:Guinea Pigs; D007093:Imidazoles / Q000494:pharmacology* / Q000627:therapeutic use; D017294:Ondansetron; D011817:Rabbits; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000502:physiology; D012702:Serotonin Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D014840:Vomiting, Anticipatory / Q000188:drug therapy
D007093:Imidazoles; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D017294:Ondansetron