Dopamine D2 receptor
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.
Overview
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.
- 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 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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
A Gi-coupled G-protein-coupled receptor that lowers cyclic AMP; in the pituitary it suppresses prolactin gene expression and lactotroph proliferation.
- 3 · How drugs use it
No product in this corpus aims at Dopamine D2 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 lowers cyclic AMP; in the pituitary it suppresses prolactin gene expression and lactotroph proliferation.
- Pituitary lactotrophs, striatum and chemoreceptor trigger zone
- Prolactinomas, some neuroendocrine tumours and gliomas
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- IdeaSSTR antagonist radioligands to increase tumour dose
- CompanyPOINT Biopharma
- TrialNETTER-1
- PersonMartyn E. Caplin
- TargetTryptophan hydroxylase 1
- CollectionNational Brain Tumor Society (NBTS)
Shares Dordaviprone, Glioma & glioblastoma.
- InstitutionHolden Comprehensive Cancer Center, University of Iowa
Shares Somatostatin receptor 2, Neuroendocrine tumours, Glioma & glioblastoma.
- PersonJonathan R. Strosberg