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Ondansetron was the first 5-HT 3 antagonist, developed by Glaxo around 1984. Its efficacy was first established in 1987, in animal models, [10] [11] and it was extensively studied over the following years. [12]
Ondansetron is a highly selective serotonin 5-HT 3 receptor antagonist, with low affinity for dopamine receptors. The 5-HT 3 receptors are present both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema in the medulla.
The genes encoding human 5-HT 3 receptors are located on chromosomes 11 (HTR3A, HTR3B) and 3 (HTR3C, HTR3D, HTR3E), so it appears that they have arisen from gene duplications. The genes HTR3A and HTR3B encode the 5-HT 3A and 5-HT 3B subunits and HTR3C, HTR3D and HTR3E encode the 5-HT 3C, 5-HT 3D and 5-HT 3E subunits.
Approved 5-HT 3 inhibitors include dolasetron (Anzemet), granisetron (Kytril, Sancuso), and ondansetron (Zofran). Their antiemetic effect due to blockade of 5HT3 receptor on vagal afferent in the gut. in addition they also block 5-HT3 receptors in CTZ and STN. The newest 5-HT 3 inhibitor, palonosetron (Aloxi), also prevents delayed nausea and ...
This page was last edited on 6 December 2021, at 06:52 (UTC).; Text is available under the Creative Commons Attribution-ShareAlike 4.0 License; additional terms may apply.
Antagonists of the 5-HT 2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). They include, but are not limited to: Cyproheptadine blocks 5-HT 2A, H1 and is a mild anticholinergic. Methysergide is a 5-HT 2A antagonist and nonselective 5-HT 1 receptor blocker.
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