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The dopamine D2 receptor is how cabergoline and bromocriptine shrink prolactin-secreting pituitary tumours without surgery, and it is the target of the antiemetics metoclopramide and prochlorperazine used during chemotherapy.
The D2 dopamine receptor on pituitary lactotroph cells inhibits prolactin release, so the dopamine agonists cabergoline and bromocriptine are the first-line treatment for prolactinomas, normalising prolactin and shrinking the tumour in most patients; they also have some effect in other pituitary adenomas and in neuroendocrine tumours that express the receptor. In supportive care, D2 antagonists such as metoclopramide, prochlorperazine and olanzapine treat chemotherapy-induced nausea. D2 receptor expression on glioblastoma and other tumour cells has prompted trials of the antagonist ONC201 (dordaviprone), which acts on D2 and on the mitochondrial protease ClpP and was approved in 2025 for H3 K27M-mutant diffuse midline glioma.
In plain words · The dopamine D2 receptor is how cabergoline and bromocriptine shrink prolactin-secreting pituitary tumours without surgery, and it is the target of the antiemetics metoclopramide and prochlorperazine used during chemotherapy.
The dopamine D2 receptor is how cabergoline and bromocriptine shrink prolactin-secreting pituitary tumours without surgery, and it is the target of the antiemetics metoclopramide and prochlorperazine used during chemotherapy.
A Gi-coupled G-protein-coupled receptor that lowers cyclic AMP; in the pituitary it suppresses prolactin gene expression and lactotroph proliferation.
2 products aim at Dopamine D2 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 group enriched in normal brain, pituitary gland, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA DRD2: RNA group enriched (brain 62 nTPM, pituitary gland 57 nTPM); high antibody staining in 1 normal tissue. Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Brain and spinal cord tumours (all types), Neuroendocrine tumours); 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 DRD2 tissue; Human Protein Atlas DRD2 pathology; Open Targets ENSG00000149295 associations
First described 1989. Earliest sequence paper UniProt cites for the protein: Selbie L.A. et al, DNA, 1989, "The major dopamine D2 receptor: molecular analysis of the human D2A subtype". Source.
A Gi-coupled G-protein-coupled receptor that lowers cyclic AMP; in the pituitary it suppresses prolactin gene expression and lactotroph proliferation.
RNA: group enriched (brain 62 nTPM, pituitary gland 57 nTPM), detected in some normal tissues.
Medium: Caudate, Cerebral cortex, Hippocampus.
No cancer stained high; medium in cervical cancer, endometrial cancer, glioma, lymphoma.
HPA DRD2 tissue · HPA DRD2 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: dopamine receptor; also the target in prolactin-secreting pituitary tumours. 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.
Bromocriptine was the first pill that could shrink a pituitary tumour. From the 1970s it turned prolactinomas from a surgical disease into one usually controlled with tablets, and it is still used where cabergoline is unavailable or unsuitable.
Cabergoline is a tablet taken once or twice a week that shrinks prolactin-secreting pituitary tumours and normalises hormone levels in most patients, so surgery is reserved for the few whose tumours resist or who cannot tolerate it.
Query for this target: (TITLE:"Dopamine D2 receptor" OR ABSTRACT:"Dopamine D2 receptor" OR TITLE:"DRD2" OR ABSTRACT:"DRD2") 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 Dopamine D2 receptor, not a curated reading list.
Shares Cabergoline, Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma.
Shares Cabergoline, Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma.
Shares Cabergoline, Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma.
Shares Bromocriptine, Cabergoline, Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma.
Shares Dordaviprone, Glioma & glioblastoma.
Shares Cabergoline, Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma.