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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AB12-82
0 ImagesCat. No.: HY-184590AB12-82 is a selective dopamine receptor agonist with a Ki value of 1.88 nM for human D3R. AB12-82 achieves subtype-selective D3R activation by enhancing interactions with the D3R H291·32 residue. AB12-82 can be used in the research of nervous system-related diseases.
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D3R ligand 1
0 ImagesCat. No.: HY-149337CAS No.: 2983777-91-7D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling.
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Perphenazine dihydrochloride
0 ImagesPerphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation.
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Cabergoline-d6
0 ImagesCat. No.: HY-15296S1CAS No.: 2738376-76-4Synonyms: FCE-21336-d6Cabergoline-d6 is 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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D2R/D3R/5-HT1AR agonist 1
0 ImagesCat. No.: HY-179713CAS No.: 3028684-07-0D2R/D3R/5-HT1AR agonist 1 (compound 22b) is an orally active triple-target D2R/D3R/5-HT1AR agonist with EC50 values of 1.29, 1.05 and 153.5 nM. D2R/D3R/5-HT1AR agonist 1 can improve the behavioral disorders induced by MPTP (HY-W114750) and exerts anti-depression effect. D2R/D3R/5-HT1AR agonist 1 can be used for the research of Parkinson's disease and depression.
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(Rac)-Rotigotine-d7 (hydrochloride)
0 ImagesCat. No.: HY-15394SCAS No.: 3026226-88-7Synonyms: N-0437-d7 (hydrochloride)(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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7-Hydroxy-DPAT
0 ImagesCat. No.: HY-134015CAS No.: 74938-11-7Synonyms: 7-OH-DPAT7-Hydroxy-DPAT (7-OH-DPAT) is a selective D3 dopamine receptor agonist. 7-Hydroxy-DPAT exhibits significant pharmacological activity in modulating locomotor behavior and dopamine metabolism within the brain. 7-Hydroxy-DPAT can be used for the research of neurological disease .
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OS-3-106
0 ImagesCat. No.: HY-116820CAS No.: 1580000-17-4OS-3-106 is a potent, and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research.
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AB13-08
0 ImagesCat. No.: HY-184588AB13-08 is a selective dopamine receptor agonist with a Ki value of 53.9 nM for human D3R. AB13-08 is applicable to the research of neurological disorders such as Parkinson's disease and schizophrenia.
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MOR agonist-2
0 ImagesCat. No.: HY-155706CAS No.: 2833692-02-5MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism.
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DR/5-HT7AR Ligand-1
0 ImagesCat. No.: HY-187538DR/5-HT7AR Ligand-1 is a ligand with a Ki value of 1.24 nM against human D2R, 5.78 nM against human D3R, 0.67 nM against human 5-HT1AR, and 19.9 nM against human 5-HT7AR. DR/5-HT7AR Ligand-1 can be used for the research of schizophrenia.
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Dopamine D3 receptor ligand-6
0 ImagesCat. No.: HY-174307CAS No.: 687634-09-9Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction).
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Thioridazine 2-Sulfone-d3
0 ImagesCat. No.: HY-B0965SCAS No.: 1329652-09-6Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
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Alentemol
0 ImagesCat. No.: HY-124524CAS No.: 112891-97-1Synonyms: U-66444B free baseAlentemol (U-66444B (free base)) is a blood-brain barrier-permeable dopamine receptor D1, D2, D3, and D4 agonist. Alentemol inhibits dopamine release, reduces dopamine synthesis, regulates dopamine metabolism, suppresses the impulse activity of dopaminergic neurons, and decreases the impulse frequency of dopaminergic neurons in the substantia nigra pars compacta and ventral tegmental area. Alentemol is applicable to research related to schizophrenia.
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Ropinirole-d4 hydrochloride
0 ImagesCat. No.: HY-B0623ASCAS No.: 1330261-37-4Synonyms: SKF 101468-d4 hydrochlorideRopinirole-d4 (SKF 101468-d4) hydrochloride is the deuterium labeled Ropinirole hydrochloride. Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Kiof 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
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Pimozide-d5 N-Oxide
0 ImagesCat. No.: HY-12987S1CAS No.: 1794795-40-6Pimozide-d5 N-Oxide is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
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Iloperidone hydrochloride
0 ImagesCat. No.: HY-17410ACAS No.: 1299470-39-5Synonyms: HP 873 hydrochlorideIloperidone hydrochloride (HP 873 hydrochloride) is a D2/5-HT2 receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms.
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FAUC-312
0 ImagesCat. No.: HY-121740CAS No.: 562104-72-7FAUC-312, a tetrahydropyrimidine, is a strong and highly selective dopamine D4 receptor partial agonist (Ki=1.5 nM).
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Pardoprunox
0 ImagesCat. No.: HY-14958CAS No.: 269718-84-5Synonyms: SLV-308; DU-126891Pardoprunox (SLV-308) is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively.
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Sarizotan dihydrochloride
0 ImagesCat. No.: HY-100820BCAS No.: 177976-12-4Synonyms: EMD 128130 dihydrochlorideSarizotan dihydrochloride (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.
