D2 Dopamine Receptor Antibodies
The dopamine D2 receptor belongs to the D2-like subfamily of dopamine receptors. It inhibits cAMP production by coupling to inhibitory G proteins. The D2 receptor is a pharmacological target for drugs widely used to treat symptoms for disorders associated with dopaminergic dysfunctions, including Parkinson’s disease and schizophrenia. D2-preferring agonists such as pramipexole, ropinirole, piribedil, rotigotine, and the ergot alkaloids pergolide, bromocriptine and cabergoline have proven useful for the therapy of Parkinson’s disease. A strong correlation exists between the therapeutic effects of antipsychotics and blockade of the D2 dopamine receptor. In fact, all clinically approved antipsychotics including chlorpromazine, haloperidol, olanzapine, sulpiride, quetiapine and clozapine are D2 receptor blockers. D2 desensitization, β-arrestin recruitment and signaling are regulated by phosphorylation of third intracellular loop serine317/threonine318 (pS317/pT318-D2). This nomenclature refers to the human D2. Agonist-induced D2 phosphorylation is primarily mediated by GRK2 and GRK3. The development β-arrestin biased D2 ligands has been proposed as strategy for antipsychotics with fewer side effects. Phosphosite-specific antibodies can provide precise information about partial, full and biased agonism of D2 ligands. For more information on D2 receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Mann A, Keen AC, Mark H, Dasgupta P, Javitch JA, Canals M, Schulz S, Robert Lane J. New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D2 receptor regulation and signaling. Sci Rep. 2021 Apr 15;11(1):8288. doi: 10.1038/s41598-021-87417-2. PMID: 33859231; PMCID: PMC8050214.
Beaulieu JM, Gainetdinov RR. The physiology, signaling, and pharmacology of dopamine receptors. Pharmacol Rev. 2011 Mar;63(1):182-217. doi:10.1124/pr.110.002642. Epub 2011 Feb 8. Review. PubMed PMID: 21303898.
Beaulieu JM, Espinoza S, Gainetdinov RR. Dopamine receptors - IUPHAR Review 13. Br J Pharmacol. 2015 Jan;172(1):1-23. Review. PubMed PMID: 25671228; PubMed Central PMCID: PMC4280963.