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The serotonin receptor on the gut's vagus nerve endings and in the brainstem vomiting centre that chemotherapy triggers. Ondansetron and palonosetron block it, the foundation of modern anti-sickness treatment.
Chemotherapy damages enterochromaffin cells in the gut lining, releasing serotonin that activates 5-HT3 receptors on vagal afferents and in the area postrema to provoke acute vomiting. 5-HT3 antagonists, first ondansetron in 1991 and later granisetron and the long-acting palonosetron, block this pathway and transformed the experience of cisplatin-based and anthracycline-based chemotherapy. They are combined with an NK1 antagonist and dexamethasone for highly emetogenic regimens; constipation, headache and QT prolongation are the main side effects.
In plain words · The serotonin receptor on the gut's vagus nerve endings and in the brainstem vomiting centre that chemotherapy triggers. Ondansetron and palonosetron block it, the foundation of modern anti-sickness treatment.
The serotonin receptor on the gut's vagus nerve endings and in the brainstem vomiting centre that chemotherapy triggers. Ondansetron and palonosetron block it, the foundation of modern anti-sickness treatment.
Ligand-gated ion channel for serotonin on vagal afferents and in the brainstem chemoreceptor trigger zone; blocked by setron antiemetics.
1 product aims at 5-HT3 receptor (HTR3A): small molecules. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
Tumour-associated overexpression: HPA finds the RNA cancer enhanced in cancer (Ovary Serous Cystadenocarcinoma (TCGA)) and group enriched in normal brain, intestine, lymphoid tissue, pancreas, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA HTR3A: RNA group enriched (brain 2 nTPM, intestine 2 nTPM, lymphoid tissue 8 nTPM); blood lineage group enriched (B-cells 14 nTPM, dendritic cells 12 nTPM); no normal tissue stained high. Distribution: no corpus cancer carries a prevalence row, threshold or catalogue link for it; Open Targets associates it with 0 specific cancer types at or above 0.5. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas HTR3A tissue; Human Protein Atlas HTR3A pathology; Open Targets ENSG00000166736 associations
First described 1995. Earliest sequence paper UniProt cites for the protein: Miyake et al, Mol. Pharmacol, 1995, "Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species". Source.
Ligand-gated ion channel for serotonin on vagal afferents and in the brainstem chemoreceptor trigger zone; blocked by setron antiemetics.
RNA: group enriched (brain 2 nTPM, intestine 2 nTPM, lymphoid tissue 8 nTPM, pancreas 3 nTPM, salivary gland 5 nTPM), detected in some normal tissues. Blood: group enriched (B-cells 14 nTPM, dendritic cells 12 nTPM).
No normal tissue stained high; medium in Lymph node, Tonsil.
RNA cancer enhanced: Ovary Serous Cystadenocarcinoma 26 pTPM.
No cancer stained high; medium in lymphoma, melanoma.
HPA HTR3A tissue · HPA HTR3A pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Metastatic cancer | host% | Host target: serotonin receptor on gut vagal endings and the vomiting centre. Not a tumour alteration, so no prevalence applies; the drug acts on normal tissue or on symptoms. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Dolasetron is one of the serotonin-blocking antiemetics that transformed chemotherapy in the 1990s, approved in 1997 to prevent nausea and vomiting; its intravenous form lost its chemotherapy indication in 2010 because of heart rhythm effects.
Query for this target: (TITLE:"5-HT3 receptor" OR ABSTRACT:"5-HT3 receptor" OR TITLE:"HTR3A" OR ABSTRACT:"HTR3A") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about 5-HT3 receptor (HTR3A), not a curated reading list.
Shares NK1 receptor (TACR1), Ondansetron, Palonosetron.
Shares Ondansetron, Palonosetron.
Shares NK1 receptor (TACR1), Palonosetron.
Shares Granisetron, Ondansetron, Palonosetron.