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The CB1 cannabinoid receptor is how dronabinol and nabilone, synthetic cannabinoids approved for chemotherapy nausea that other drugs fail to control, act on the brain; their place is behind the 5-HT3 and NK1 antagonists.
Cannabinoid receptor 1 is the brain receptor for THC and for the body's own endocannabinoids. Dronabinol (synthetic THC) and nabilone are approved for nausea and vomiting from chemotherapy in patients who have not responded to conventional antiemetics, and dronabinol also for appetite loss in AIDS; guidelines place them as later options after 5-HT3 antagonists, NK1 antagonists, dexamethasone and olanzapine because of dizziness, sedation and mood effects. Claims that cannabinoids shrink tumours rest on laboratory and small early studies, and no cannabinoid is approved to treat cancer itself.
In plain words · The CB1 cannabinoid receptor is how dronabinol and nabilone, synthetic cannabinoids approved for chemotherapy nausea that other drugs fail to control, act on the brain; their place is behind the 5-HT3 and NK1 antagonists.
The CB1 cannabinoid receptor is how dronabinol and nabilone, synthetic cannabinoids approved for chemotherapy nausea that other drugs fail to control, act on the brain; their place is behind the 5-HT3 and NK1 antagonists.
A Gi-coupled G-protein-coupled receptor, among the most abundant in the brain, that reduces neurotransmitter release from presynaptic terminals; also present in gut, fat and liver.
2 products aim at Cannabinoid receptor 1: 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 enriched in cancer (Glioblastoma Multiforme (TCGA)) and tissue enhanced in normal adipose tissue, brain, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA CNR1: RNA tissue enhanced (adipose tissue 18 nTPM, brain 19 nTPM); high antibody staining in 6 normal tissues; highest cancer staining thyroid cancer (2 of 4 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 CNR1 tissue; Human Protein Atlas CNR1 pathology; Open Targets ENSG00000118432 associations
First described 1990. Earliest sequence paper UniProt cites for the protein: Gerard et al, Nucleic Acids Res, 1990, "Nucleotide sequence of a human cannabinoid receptor cDNA". Source.
A Gi-coupled G-protein-coupled receptor, among the most abundant in the brain, that reduces neurotransmitter release from presynaptic terminals; also present in gut, fat and liver.
RNA: tissue enhanced (adipose tissue 18 nTPM, brain 19 nTPM), detected in many normal tissues.
Medium: Appendix, Caudate, Cerebral cortex, Colon, Duodenum, Endometrium, Epididymis, Fallopian tube.
RNA cancer enriched: Glioblastoma Multiforme 26 pTPM.
Medium only: breast cancer, carcinoid, endometrial cancer, head and neck cancer.
HPA CNR1 tissue · HPA CNR1 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: brain cannabinoid receptor. 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.
Dronabinol is synthetic THC in a capsule, approved in 1985 for chemotherapy nausea and vomiting that other antiemetics have failed to control, and later for appetite loss in AIDS; it sits well behind the 5-HT3 and NK1 antagonists in today's guidelines.
Nabilone is a synthetic cannabinoid capsule approved in 1985 for chemotherapy-induced nausea and vomiting that standard drugs cannot control; like dronabinol it is a later-line option because of its effects on mood and balance.
Query for this target: (TITLE:"Cannabinoid receptor 1" OR ABSTRACT:"Cannabinoid receptor 1" OR TITLE:"CNR1" OR ABSTRACT:"CNR1") 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 Cannabinoid receptor 1, not a curated reading list.