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]
-
D3 Receptor Related Products (162)
Related Products (162)
-
SB-773812
0 ImagesCat. No.: HY-13051CAS No.: 630407-66-8SB-773812 is a moderate-affinity antagonist at dopamine receptor 2 (pKi=7.4) and a high-affinity antagonist at the dopamine receptor 3 (pKi=8.5) and at the serotonin 5-hydroxytryptamine receptors 2A (pKi=9.0), 2C (pKi=8.1), and 6 (pKi=8.1). SB-773812 is promising for research of central nervous system disorders.
-
Obuprazine
0 ImagesCat. No.: HY-183734CAS No.: 2640663-79-0Obuprazine is an orally active dopamine D3 receptor agonist and 5-HT2A receptor antagonist with IC50 values of 0.37 and 4.19 nM, respectively. Obuprazine acts as a G protein-coupled receptor modulater. Obuprazine can be used for the research of schizophrenia.
-
Dopamine D3 receptor antagonist-2
0 ImagesCat. No.: HY-139681CAS No.: 3052236-39-9Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective (Ki = 2.16 nM) or multitarget bitopic ligand potentially useful for central nervous system disorders.
-
AB13-46A
0 ImagesCat. No.: HY-184589AB13-46A is a selective dopamine receptor agonist, with a Ki value of 0.505 nM against human D3R. AB13-46A can be used for research on nervous system-related diseases.
-
PD-143188
0 ImagesCat. No.: HY-19186CAS No.: 150013-70-0Synonyms: CI 1007PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with Ki values of 25.5 nM and 16.6 nM for human D2 and D3 receptors, respectively and lower affinity for D4.2 receptors (Ki=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology.
-
SB-414796
0 ImagesCat. No.: HY-123473CAS No.: 264262-71-7SB-414796 is a selective, orally active and cross the blood-brain barrier dopamine D3 receptor antagonist with Ki values of 4, 400 nM for D3, D2, respectively.
-
Asenapine-13C,d3 hydrochloride
0 ImagesCat. No.: HY-16567SSynonyms: Org 5222-13C,d3 hydrochlorideAsenapine-13C,d3 (hydrochloride) is the 13C- and deuterium labeled Asenapine (hydrochloride). Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
-
Dopamine D3 receptor agonist 1
0 ImagesCat. No.: HY-181721Dopamine D3 receptor agonist 1 is a dopamine D3 Receptor agonist with a Ki value of 0.268 nM. Dopamine D3 receptor agonist 1 exhibits metabolic stability in rat liver microsomes. Dopamine D3 receptor agonist 1 can be used to study severe mental disorders comorbid with substance use disorders.
-
NGB 2904 hydrochloride
0 ImagesCat. No.: HY-12697ACAS No.: 189061-11-8NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis.
-
U-99194
0 ImagesCat. No.: HY-12701CAS No.: 82668-33-5Synonyms: U-99194A free base; PNU-99194A; JPC-211U-99194 (PNU-99194) is a selective, potent dopamine D3 receptor antagonist. U-99194 inhibits the activation of D3 receptor mediated by endogenously released dopamine or exogenous D3 agonists. U-99194 abrogates the IPSC-suppressive effect of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 significantly suppresses Nicotine (HY-127019)-induced tremor in mice. U-99194 can be used for the study of dopamine D3 receptor-mediated motor disorders, particularly kinetic tremors.
-
Dopamine D3 receptor ligand-2
0 ImagesCat. No.: HY-115954CAS No.: 2882828-95-5Dopamine D3 receptor ligand-2 (compound 8) is a potent D3 receptor ligand with a Ki of 11.4 nM. Dopamine D3 receptor ligand-2 have high selectivity for D3 over D2 (Ki=1228 nM).
-
Dopamine D3 receptor agonist-2
0 ImagesCat. No.: HY-183776CAS No.: 1000031-37-7Dopamine D3 receptor agonist-2 is a selective dopamine D3 receptor partial agonist with a Ki of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamine D2 receptor (Ki= 7.67nM).
-
PF-4363467
0 ImagesCat. No.: HY-124583CAS No.: 2040055-84-1PF-4363467, a dopamine D3/D2 receptor antagonist, attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-4363467 exhibits Ki values of 3.1 nM and 692 nM for D3R and D2R.
-
PD 168568
0 ImagesCat. No.: HY-103407CAS No.: 210688-56-5PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research.
-
PF-04363467
0 ImagesCat. No.: HY-11056CAS No.: 1010382-72-5PF-04363467 is a highly preferring D3R antagonist. PF-04363467 produces dose-dependent changes in the EEG profile of freely moving rats. PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-04363467 can be used for the study of addiction, cognitive and mental illness.
-
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.
-
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.
-
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.
-
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).
-
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.
