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Granisetron is a serotonin 5-HT 3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness.
The 5-HT 3 receptor antagonists suppress vomiting and nausea by inhibiting serotonin binding to the 5-HT 3 receptors. The highest concentration of 5-HT 3 receptors in the central nervous system are found in the STN and chemoreceptor trigger zone (CTZ), and 5-HT 3 antagonists may also suppress vomiting and nausea by acting at these sites. [29]
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. It causes retroperitoneal fibrosis and mediastinal fibrosis. [citation needed] Quetiapine blocks 5-HT 2A, 5-HT 1A, dopamine receptors D 1 and D 2, histamine receptor H1, and A1 adrenoreceptors.
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The drug is a silent antagonist of the serotonin 5-HT 1B receptor, unlike the related agent GR-127935. [ 1 ] [ 4 ] GR-55562 has around 10-fold selectivity for the serotonin 5-HT 1B receptor over the serotonin 5-HT 1D receptor and has only weak affinity for a number of other serotonin receptors .
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.
15550 Ensembl ENSG00000178394 ENSMUSG00000021721 UniProt P08908 Q64264 RefSeq (mRNA) NM_000524 NM_008308 RefSeq (protein) NP_000515 NP_032334 Location (UCSC) Chr 5: 63.96 – 63.96 Mb Chr 13: 105.58 – 105.58 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse The serotonin 1A receptor (or 5-HT 1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin ...
The 5-HT 1B receptor as an example of a metabotropic serotonin receptor. Its crystallographic structure in ribbon representation. 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems.