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 (166)
Related Products (166)
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Cabergoline-d5
0 ImagesCat. No.: HY-15296SCAS No.: 1426173-20-7Synonyms: FCE-21336-d5Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
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Dopamine D3 receptor ligand-3
0 ImagesCat. No.: HY-115955CAS No.: 2891605-81-3Dopamine D3 receptor ligand-3 (compound 12C) is a potent D3 receptor ligand with a Ki of 3.6 nM. Dopamine D3 receptor ligand-3 have high selectivity for D3 over D2 (Ki=353 nM).
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PNU-177864 hydrochloride
0 ImagesCat. No.: HY-103406ACAS No.: 1783978-03-9PNU-177864 is a potent, selective, orally active dopamine D3 receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity.
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PD 158771
0 ImagesCat. No.: HY-167648CAS No.: 189152-50-9PD 158771 is an antipsychotic agent that functions as a partial agonist for D2 /D3 receptors (Ki = 42.0/13.7 nM) and as an agonist for 5-HT1A receptors (Ki = 2.6 nM). PD 158771 can be utilized in antipsychotic research.
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Pramipexole-d7 dihydrochloride
0 ImagesCat. No.: HY-17355SPramipexole-d7 dihydrochloride is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride 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 can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
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SK609 hydrochloride
0 ImagesSK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC50 of 1109 nM. SK609 hydrochloride has the potential for parkinson research.
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Dopamine D3 receptor ligand-1
0 ImagesCat. No.: HY-115953CAS No.: 2882828-93-3Dopamine D3 receptor ligand is a potent, selective and high affinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3 Ki= 8 nM, D2 Ki= 715 nM).
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D-520
0 ImagesCat. No.: HY-120156CAS No.: 1619269-47-4D-520 is a potent and brain-penetrant dopamine D2/D3 agonist (D2 EC50 = 4.73 nM, Ki = 41.8 nM; D3 EC50 = 2.18 nM, Ki = 0.35 nM). D-520 inhibits the formation of Aβ aggregates in vitro and promotes the disaggregation of both alpha-synuclein (α-syn) and Aβ aggregates. D-520 exhibits efficacious activity in animal models of Parkinson’s disease (PD). D-520 can be used for PD and PD with dementia (PDD) research[1][2].
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ARN25657
0 ImagesCat. No.: HY-176287ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.
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Piribedil dihydrochloride
0 ImagesCat. No.: HY-12707ACAS No.: 1451048-94-4Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
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BP 897
0 ImagesBP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM).
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Tau-aggregation-IN-1
0 ImagesCat. No.: HY-146135CAS No.: 1619269-19-0Tau-aggregation-IN-1 (Compound D-519) is a tau441 protein aggregation inhibitor with an IC50 of 21 µM. Tau-aggregation-IN-1 is also a dopamine D2 and D3 receptor agonist.
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Clomipramine-d3
0 ImagesCat. No.: HY-B0457ASCAS No.: 136765-29-2Synonyms: Chlorimipramine-d3; G-34586-d3; NSC-169865-d3Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
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L 741742 hydrochloride
0 ImagesCat. No.: HY-101349ACAS No.: 874882-93-6L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma.
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L-745870 trihydrochloride
0 ImagesCat. No.: HY-14325ACAS No.: 866021-03-6L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride 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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Aramisulpride hydrochloride
0 ImagesCat. No.: HY-109167ACAS No.: 2129505-46-8Synonyms: (R)-Amisulpride hydrochloride; (R)-Esamisulpride hydrochloride; (R)-DAN 2163 hydrochlorideAramisulpride hydrochloride is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride hydrochloride is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride hydrochloride can be used in psychiatric research.
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Tiapride
0 ImagesCat. No.: HY-B1196ACAS No.: 51012-32-9Tiapride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride shows anti-dyskinetic activity and anxiolytic activity. Tiapride is a neuroleptic agent.
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AB13-73A
0 ImagesCat. No.: HY-184591AB13-73A is a highly selective partial agonist of dopamine D3R, with a Ki of 0.803 nM and a pEC50 of 11.88 (1.32 pM). AB13-73A serves as a pharmacological tool to dissect the (patho) physiological mechanisms of D3R and support the development of improved neurotherapeutic agents.
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SV 156
0 ImagesCat. No.: HY-111242CAS No.: 873445-60-4SV 156 is a potent and selective D2 dopamine receptor antagonist, with a Ki of 2.5 nM for hD2. SV 156 has approximately 40-fold binding selectivity for D2 dopamine receptors compared to the D3 receptor subtype. SV 156 can be used for L-DOPA (HY-N0304)-associated abnormal involuntary movements (AIMs) research.
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BP 897 hydrochloride
0 ImagesBP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM).
