D3 Receptor
Dopamine D3 receptor (DRD3) is a member of the D2-like dopamine receptor family and functions as a G protein-coupled receptor that is highly enriched in limbic brain regions involved in cognition, motivation, emotion, and reward processing[1][2]. Mechanistically, DRD3 primarily couples to inhibitory G proteins and suppresses adenylyl cyclase activity, thereby regulating intracellular cAMP-dependent signaling pathways that influence neuronal responsiveness and dopaminergic neurotransmission[1][3][4]. Through this signaling framework, DRD3 contributes to neural circuit functions associated with neuropsychiatric and neurological disorders, and extensive research has examined its role in addiction, schizophrenia, and other dopamine-related disease models[5][6]. Compared with related D2-like receptor isoforms, DRD3 exhibits a distinct anatomical distribution and pharmacological profile, making it an attractive target for subtype-selective investigations aimed at separating therapeutic effects from broader dopamine receptor activity[2][5]. Experimental studies further indicate that DRD3 can participate in receptor-receptor interactions, including functional heteromerization with D2 receptors, which may alter downstream signaling properties and receptor pharmacology[7]. For research applications, selective DRD3 agonists, partial agonists, and antagonists have been developed as molecular probes to investigate receptor-specific mechanisms and to evaluate potential therapeutic strategies in preclinical models of neuropsychiatric disease and substance use disorders[5][8].
References:
- [1]. Sokoloff P, et al. Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature. 1990 Sep 13;347(6289):146-51. [Content Brief]
- [2]. Kiss B, et al. Neuronal Dopamine D3 Receptors: Translational Implications for Preclinical Research and CNS Disorders. Biomolecules. 2021 Jan 14;11(1):104. [Content Brief]
- [3]. Robinson SW, et al. Selective inhibition of adenylyl cyclase type V by the dopamine D3 receptor. Mol Pharmacol. 1997 Sep;52(3):508-14. [Content Brief]
- [4]. D 3 Receptor gene information from NCBI.
- [5]. Luedtkea RR, et al. Progress in developing D3 dopamine receptor ligands as potential therapeutic agents for neurological and neuropsychiatric disorders. Curr Pharm Des. 2003;9(8):643-71. [Content Brief]
- [6]. Martel JC, et al. Dopamine Receptor Subtypes, Physiology and Pharmacology: New Ligands and Concepts in Schizophrenia. Front Pharmacol. 2020 Jul 14;11:1003. [Content Brief]
- [7]. Scarselli M, et al. D2/D3 dopamine receptor heterodimers exhibit unique functional properties[J]. Journal of Biological Chemistry, 2001, 276(32): 30308-30314.
- [8]. Newman AH, et al. Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents. J Med Chem. 2005 Jun 2;48(11):3663-79. [Content Brief]
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D3 Receptor Related Products (167)
Related Products (167)
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Iloperidone
0 ImagesSynonyms: HP 873Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.
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UNC9994 hydrochloride
0 ImagesUNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
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SB-277011 hydrochloride
0 ImagesSynonyms: SB-277011A hydrochlorideSB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
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Piribedil
0 ImagesPiribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
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Pramipexole dihydrochloride hydrate
0 ImagesPramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
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Asenapine
0 ImagesSynonyms: Org 5222Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
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Dehydroaripiprazole
0 ImagesSynonyms: OPC-14857; DM-14857Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D2/D3 receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin 5-HT1A, 5-HT2A and 5-HT2B receptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole.
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L-745870 hydrochloride
0 ImagesL-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
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L-DOPA-2,5,6-d3
0 ImagesL-DOPA-2,5,6-d3 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain.
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Spiperone hydrochloride
0 ImagesSpiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities.
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(+)-PD 128907 hydrochloride
0 Images(+)-PD 128907 hydrochloride is a selective dopamine D2/D3 receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D3 receptors, 179, 770 n M for human and rat D3 receptors, respectively.
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SKF 83959
0 ImagesSKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression.
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Amisulpride hydrochloride
0 ImagesSynonyms: (Rac)-Aramisulpride hydrochloride; (Rac)-Esamisulpride hydrochloride; (Rac)-DAN 2163 hydrochlorideAmisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
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GR 103691
0 ImagesGR 103691 is a potent, selective dopamine D3 receptor antagonist with a Ki value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D3 over hD4 and hD1 sites.
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Tiapride hydrochloride
0 ImagesTiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent.
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Sarizotan
0 ImagesSynonyms: EMD 128130Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
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ML417
0 ImagesML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
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Desmethyl cariprazine
0 ImagesDesmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
