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The mu-opioid receptor is the target of morphine and the other strong opioids that control most severe cancer pain; the same receptor in the gut causes opioid constipation, which methylnaltrexone and naloxegol relieve by blocking it outside the brain.
Mu-opioid receptors in the spinal cord and brain mediate the pain relief of morphine, oxycodone, fentanyl and methadone, which remain the mainstay of the WHO analgesic ladder for moderate to severe cancer pain. The same receptors in the intestinal wall slow gut movement, so opioid-induced constipation affects most patients on long-term opioids; peripherally acting antagonists such as methylnaltrexone, naloxegol and naldemedine block gut receptors without reaching the brain, and methylnaltrexone is approved specifically for opioid-induced constipation in advanced illness. Whether opioids influence tumour growth or recurrence through receptors on cancer cells is an open research question.
In plain words · The mu-opioid receptor is the target of morphine and the other strong opioids that control most severe cancer pain; the same receptor in the gut causes opioid constipation, which methylnaltrexone and naloxegol relieve by blocking it outside the brain.
The mu-opioid receptor is the target of morphine and the other strong opioids that control most severe cancer pain; the same receptor in the gut causes opioid constipation, which methylnaltrexone and naloxegol relieve by blocking it outside the brain.
A Gi-coupled G-protein-coupled receptor that closes calcium channels and opens potassium channels in neurons, reducing neurotransmitter release; densely expressed in dorsal horn, periaqueductal grey and enteric neurons.
2 products aim at Mu-opioid receptor: 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 tissue enhanced in normal brain, testis, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA OPRM1: RNA tissue enhanced (brain 4 nTPM, testis 3 nTPM); high antibody staining in 1 normal tissue. 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 OPRM1 tissue; Human Protein Atlas OPRM1 pathology; Open Targets ENSG00000112038 associations
First described 1994. Earliest sequence paper UniProt cites for the protein: Wang J.-B. et al, FEBS Lett, 1994, "Human mu opiate receptor. cDNA and genomic clones, pharmacologic characterization and chromosomal assignment". Source.
A Gi-coupled G-protein-coupled receptor that closes calcium channels and opens potassium channels in neurons, reducing neurotransmitter release; densely expressed in dorsal horn, periaqueductal grey and enteric neurons.
RNA: tissue enhanced (brain 4 nTPM, testis 3 nTPM), detected in some normal tissues.
No cancer stained high; medium in melanoma.
HPA OPRM1 tissue · HPA OPRM1 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: mu-opioid receptor in pain pathways and gut. 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.
These are fast-acting forms of the opioid fentanyl, taken as a tablet against the cheek or as a nasal spray, for sudden flares of pain in people whose cancer pain is otherwise controlled by a regular opioid. They are only for patients already tolerant to opioids.
Methylnaltrexone (Relistor) is an injection or tablet that relieves the severe constipation caused by strong painkillers in people with advanced cancer, without blocking the pain relief itself.
Query for this target: (TITLE:"Mu-opioid receptor" OR ABSTRACT:"Mu-opioid receptor" OR TITLE:"OPRM1" OR ABSTRACT:"OPRM1") 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 Mu-opioid receptor, not a curated reading list.