Document Detail


Selectivity of 5-HT3 receptor antagonists and anti-emetic mechanisms of action.
MedLine Citation:
PMID:  1525396     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
5-HT3 receptor antagonists, ondansetron, granisetron and tropisetron are highly specific for the 5-HT3 receptor and have a selectivity ratio of approximately 1000:1 compared with affinities for other receptors. Other 5-HT3 receptor antagonists, largely those having a benzamide structure, are non-selective. These include metoclopramide, renzapride and zacopride which stimulate gastric motility via activation of 5-HT4 receptors; metoclopramide is also a potent dopamine receptor antagonist. Selective 5-HT3 receptor antagonists are a major advance in the treatment of chemotherapy- and radiotherapy-induced emesis in cancer patients. These agents inhibit emesis by blocking 5-HT3 receptors on vagal afferent nerve terminals in the gastrointestinal mucosa and on terminals on the same vagal nerves in the vomiting system. Inhibition of acute emesis appears to be produced by blocking the initiation of the emetic reflex induced via 5-HT3 receptors and by 5-HT released from enterochromaffin cells in the small intestine, as well as by blocking 5-HT3 receptors in the hindbrain vomiting system.
Authors:
A J Freeman; K T Cunningham; M B Tyers
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Anti-cancer drugs     Volume:  3     ISSN:  0959-4973     ISO Abbreviation:  Anticancer Drugs     Publication Date:  1992 Apr 
Date Detail:
Created Date:  1992-10-19     Completed Date:  1992-10-19     Revised Date:  2005-11-16    
Medline Journal Info:
Nlm Unique ID:  9100823     Medline TA:  Anticancer Drugs     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  79-85     Citation Subset:  IM    
Affiliation:
Glaxo Group Research, Greenford, Middlesex, UK.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antiemetics / pharmacology*
Humans
Serotonin Antagonists*
Chemical
Reg. No./Substance:
0/Antiemetics; 0/Serotonin Antagonists

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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