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The 5-HT3 antagonists, informally known as "setrons", are a class of drugs that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain. With the notable exception of alosetron and cilansetron, which are used in the treatment of irritable bowel syndrome, all 5-HT3 antagonists are antiemetics, used in the prevention and treatment of nausea and vomiting. They are particularly effective in controlling the nausea and vomiting produced by cancer chemotherapy and are considered the gold standard for this purpose. The 5-HT3 antagonists may be identified by the suffix –setron,〔World Health Organization (2006). . Geneva: WHO Press. Retrieved on 2007-05-15.〕 and are classified under code A04AA of the 's Anatomical Therapeutic Chemical Classification System. ==History== The history of the 5-HT3 receptor antagonists began in 1957, when J.H. Gaddum and Zuleika P. Picarelli at the University of Edinburgh proposed the existence of two serotonin receptor subtypes, the ''M'' and ''D'' receptors (thus named because their function could be blocked by morphine and dibenzyline respectively), in a landmark paper. The 5-HT3 receptor was later found to correspond to the M receptor. In the 1970s, John Fozard found that metoclopramide and cocaine were weak antagonists at the 5-HT3 (5-HT-M) receptor. Fozard and Maurice Gittos later synthesized MDL 72222, the first potent and truly selective 5-HT3 receptor antagonist. The antiemetic effects of metoclopramide were found to be partially because of its serotonin antagonism.〔 While Fozard was investigating cocaine analogues, researchers at Sandoz identified the potent, selective 5-HT3 receptor antagonist ICS 205-930 from which the first marketed selective 5-HT3 receptor antagonists ondansetron and granisetron were developed, and approved in 1991 and 1993 respectively.〔 Several compounds related to MDL 72222 were synthesized which eventually resulted in approval of tropisetron in 1994 and dolasetron in 1997.〔 A new and improved 5-HT3 receptor antagonist, named palonosetron, was approved in 2003.〔 The development of selective 5-HT3 receptor antagonists was a dramatic improvement in the treatment of nausea and vomiting.〔 Ondansetron, granisetron, dolasetron and palonosetron are currently approved in the United States, and form the cornerstone of therapy for the control of acute emesis with chemotherapy agents with moderate to high emetogenic potential. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「5-HT3 antagonist」の詳細全文を読む スポンサード リンク
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