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D3 Dopamine Receptor Antibodies

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Agonist-induced Serine257/Threonine262 phosphorylation of the D3 Dopamine Receptor
pS257/pT262-D3 (phospho-Dopamine Receptor 3...
Serine257/Threonine262 (S257/T262) is a major phosphorylation site of the D3 dopamine receptor. The pS257/pT262-D3 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S262/T262...
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The dopamine D₃ receptor (D₃R), encoded by DRD3, is a class A G protein-coupled receptor with high affinity for its endogenous agonist, dopamine. It belongs to the D₂-like receptor subfamily and couples primarily to Gi/o, which can inhibit adenylyl cyclase. D₃R is enriched in limbic regions, particularly the ventral striatum, including the nucleus accumbens and islands of Calleja. Its distribution and findings from animal studies link D₃R signaling to motivation, reward-related learning, and drug-seeking behavior. In recombinant systems, dopamine generally induces weaker β-arrestin recruitment and receptor internalization at D₃R than at D₂R, although these responses depend on the ligand and cellular context. Pramipexole, a D₂-like agonist with preferential affinity for D₃R, is used clinically to treat Parkinson’s disease and restless legs syndrome. Cariprazine, a D₃-preferring D₃/D₂ partial agonist, is approved for the treatment of schizophrenia. The selective D₃R antagonist GSK598809 has been evaluated in human studies of receptor occupancy and addiction-related responses, and no drug selective for D₃R is currently approved for therapeutic use. D3 desensitization, ß-arrestin recruitment and signaling are regulated by phosphorylation of third intracellular loop Serine257/threonine262. This nomenclature refers to the human D3. Phosphosite-specific antibodies can provide precise information about partial, full and biased agonism of D3 ligands. For more information on D3 receptor pharmacology please refer to the IUPHAR database.  For further reading refer to:

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.

The dopamine D₃ receptor (D₃R), encoded by DRD3 , is a class A G protein-coupled receptor with high affinity for its endogenous agonist, dopamine. It belongs to the D₂-like receptor subfamily... read more »
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D3 Dopamine Receptor Antibodies

The dopamine D₃ receptor (D₃R), encoded by DRD3, is a class A G protein-coupled receptor with high affinity for its endogenous agonist, dopamine. It belongs to the D₂-like receptor subfamily and couples primarily to Gi/o, which can inhibit adenylyl cyclase. D₃R is enriched in limbic regions, particularly the ventral striatum, including the nucleus accumbens and islands of Calleja. Its distribution and findings from animal studies link D₃R signaling to motivation, reward-related learning, and drug-seeking behavior. In recombinant systems, dopamine generally induces weaker β-arrestin recruitment and receptor internalization at D₃R than at D₂R, although these responses depend on the ligand and cellular context. Pramipexole, a D₂-like agonist with preferential affinity for D₃R, is used clinically to treat Parkinson’s disease and restless legs syndrome. Cariprazine, a D₃-preferring D₃/D₂ partial agonist, is approved for the treatment of schizophrenia. The selective D₃R antagonist GSK598809 has been evaluated in human studies of receptor occupancy and addiction-related responses, and no drug selective for D₃R is currently approved for therapeutic use. D3 desensitization, ß-arrestin recruitment and signaling are regulated by phosphorylation of third intracellular loop Serine257/threonine262. This nomenclature refers to the human D3. Phosphosite-specific antibodies can provide precise information about partial, full and biased agonism of D3 ligands. For more information on D3 receptor pharmacology please refer to the IUPHAR database.  For further reading refer to:

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.

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