Mu-opioid receptor
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
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.
- 3 · How drugs use it
No product in this corpus aims at Mu-opioid receptor yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
External identifiers
Biology
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.
- Central and enteric nervous system
- Expressed on some tumour cells; significance under study
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TechnologyCancer pain management