D2 Receptor
Dopamine D2 receptor (D2R) provides negative-feedback control of dopamine neuron firing, dopamine synthesis, reuptake, and release, making it a core regulator of dopaminergic transmission[1]. Mechanistically, D2R signaling connects Gi activation, β-arrestin recruitment, receptor trafficking, and striatal A2A-D2R-AC5 complexes that integrate adenosine and dopamine signals in striatopallidal neurons[2][3][4]. In disease models, altered D2R signaling appears in schizophrenia-related assays, DYT1 dystonia, Huntington’s disease models, Parkinson’s disease research, and substance-use-disorder biology[1][2][5][6][7]. Compared with related isoforms, D2R-short, but not D2R-long, couples to the RhoA/ROCK/cofilin pathway and contributes to striatal vulnerability to expanded huntingtin[6]. This isoform distinction is experimentally important because D2R-short also supports dopamine- and TGFβ1-mediated growth inhibition in pituitary lactotropes[8]. For research applications, D2R agonists such as quinpirole, bromocriptine, ropinirole-related ligands, and radiolabeled MCL-536 help define receptor activity, D2high states, and disease-linked signaling responses[7][9][10]. D2R antagonists including haloperidol and clozapine show concentration-dependent dopamine antagonism, while haloperidol displays stronger β-arrestin-2 inhibition than Gi antagonism under specific assay conditions[2].
References:
- [1]. Chen R, et al. Dopamine D2 autoreceptor interactome: Targeting the receptor complex as a strategy for treatment of substance use disorder. Pharmacol Ther. 2020 Sep;213:107583. [Content Brief]
- [2]. Silva RR, et al. Evaluation of Functional Selectivity of Haloperidol, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine D2 Receptor. Front Pharmacol. 2019 Jun 4;10:628. [Content Brief]
- [3]. Tirotta E, et al. Signaling by dopamine regulates D2 receptors trafficking at the membrane. Cell Cycle. 2008 Jul 15;7(14):2241-8. [Content Brief]
- [4]. Ferré S, et al. Essential Control of the Function of the Striatopallidal Neuron by Pre-coupled Complexes of Adenosine A2A -Dopamine D2 Receptor Heterotetramers and Adenylyl Cyclase. Front Pharmacol. 2018 Apr 9;9:243. [Content Brief]
- [5]. Scarduzio M, et al. Strength of cholinergic tone dictates the polarity of dopamine D2 receptor modulation of striatal cholinergic interneuron excitability in DYT1 dystonia. Exp Neurol. 2017 Sep;295:162-175. [Content Brief]
- [6]. Galan-Rodriguez B, et al. Coupling of D2R Short but not D2R Long receptor isoform to the Rho/ROCK signaling pathway renders striatal neurons vulnerable to mutant huntingtin. Eur J Neurosci. 2017 Jan;45(1):198-206. [Content Brief]
- [7]. Subburaju S, et al. The High Affinity Dopamine D2 Receptor Agonist MCL-536: A New Tool for Studying Dopaminergic Contribution to Neurological Disorders. ACS Chem Neurosci. 2021 Apr 21;12(8):1428-1437. [Content Brief]
- [8]. Sarkar DK, et al. Dopamine, dopamine D2 receptor short isoform, transforming growth factor (TGF)-beta1, and TGF-beta type II receptor interact to inhibit the growth of pituitary lactotropes. Endocrinology. 2005 Oct;146(10):4179-88. [Content Brief]
- [9]. Subburaju S, et al. New Dopamine D2 Receptor Agonist, [3H]MCL-536, for Detecting Dopamine D2high Receptors in Vivo. ACS Chem Neurosci. 2018 Jun 20;9(6):1283-1289. [Content Brief]
- [10]. Mickevicius NJ. Locally Linearized Approximation of RF Pulse Propagators for Faster Simulation of Magnetization Dynamics With Slice Profile Effects in 2D MR Fingerprinting. Magn Reson Med. 2026 Jun 8. doi: 10.1002/mrm.70462. Epub ahead of print. PMID: 42260330. et al. Locally Linearized Approximation of RF Pulse Propagators for Faster Simulation of Magnetization Dynamics With Slice Profile Effects in 2D MR Fingerprinting. Magn Reson Med. 2026 Jun 8. [Content Brief]
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D2 Receptor Related Products (298)
Related Products (298)
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Molindone hydrochloride (Standard)
0 ImagesSynonyms: EN-1733A (Standard)Molindone hydrochloride (Standard) is the analytical standard of Molindone hydrochloride (HY-B1017). This product is intended for research and analytical applications. Molindone hydrochloride (EN-1733A) is an orally active and brain-penetrant dopamine D2/D5 receptor antagonist. Molindone hydrochloride shows antipsychotic and antidepressant-like activities. Molindone hydrochloride suppresses spontaneous locomotion, and antagonizes apomorphine-induced emesis. Molindone hydrochloride can be used for the research of neurological disease.
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UCSF34
0 ImagesCat. No.: HY-112320CAS No.: 14862-80-7UCSF34 (Compound 54) is a Haloperidol (HY-14538) analogue. UCSF34 binds to the human D2L receptor, with an estimated pKi of 7.49. UCSF34 can be used in the research of schizophrenia.
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Ziprasidone mesylate
0 ImagesCat. No.: HY-14542CCAS No.: 185021-64-1Synonyms: CP-88059 mesylateZiprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
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A-69024
0 ImagesCat. No.: HY-116773CAS No.: 58939-37-0A-69024 is a selectivity dopamine D-1 receptor antagonist with the Ki values of 12.6 nM and 1290 nM for dopamine D-1 receptor and dopamine D-2 receptor, respectively.
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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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5-HT7R antagonist 3
0 ImagesCat. No.: HY-159942CAS No.: 1887043-58-45-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice.
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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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Acetophenazine
0 ImagesAcetophenazine, a phenothiazine derivative, is an antipsychotic agent. Acetophenazine primarily blocks dopamine D2 receptors in the brain. Acetophenazine can be used for researching psychotic disorders such as schizophrenia and anxious depression.
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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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A 80426
0 ImagesCat. No.: HY-120037CAS No.: 152148-63-5A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC50 = 13 nM; Ki = 3.8 nM) and α2-Adrenoceptor receptor antagonist (Ki = 2 nM). A 80426 shows weak antagonistic effect to dopamine D1 receptor (Ki = 744 nM) and D2 receptor (Ki = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression.
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Dopamine D2 receptor antagonist-3
0 ImagesCat. No.: HY-W648166CAS No.: 1032714-06-9Dopamine D2 receptor antagonist-3 (Example 17) is an orally active and selective dopamine D2 receptor antagonist with a pIC50 of 5.52. Dopamine D2 receptor antagonist-3 exhibits antipsychotic activity in the Apomorphine (HY-12723) induced agitation in rats. Dopamine D2 receptor antagonist-3 can be used for psychiatric and neurological disorders research.
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1192U90
0 ImagesCat. No.: HY-106943CAS No.: 155289-31-91192U90 is an antipsychotic agent, dopamine D2 receptor antagonist as well as serotonin 5-HT1a receptor agonist. 1192U90 reduces the number of spontaneously firing neurons in the limbic dopamine system.
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Haloperidol-d4-1
0 ImagesHaloperidol-d4-1 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.
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BRL 34778
0 ImagesCat. No.: HY-106820CAS No.: 86580-77-0BRL 34778 is a potent, selective and orally active dopamine D2 receptor antagonist with a Ki of 2.14 nM. BRL 34778 exhibits antipsychotic activity with low activity for extrapyramidal effects and sedation. BRL 34778 can be used for the research of neurological disease, such as schizophrenia.
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Tefludazine
0 ImagesCat. No.: HY-184802CAS No.: 80273-79-6Tefludazine is an orally active antagonist of dopamine D2 receptor with an IC50 of 8.8 nM and 5-HT2 receptor with an IC50 of 8.6 nM. Tefludazine moderately inhibits the uptake of dopamine, norepinephrine and serotonin in rat brain synaptosomes, with IC50 values of 520 nM, 660 nM and 7000 nM, respectively. Tefludazine exhibits long-acting antipsychotic activity, lacks anticholinergic activity, shows Clozapine (HY-14539)-like effects at low doses and Haloperidol (HY-14538)-like effects at high doses. Tefludazine can be used for the research of psychotic disorders.
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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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Piquindone
0 ImagesCat. No.: HY-105903CAS No.: 78541-97-6Synonyms: Ro 22-1319Piquindone (Ro 22-1319) is a potent antipsychotic agent. Piquindone binds to a D2 dopaminergic receptor subtype in a sodium-dependent manner. Piquindone can be used in the research of schizophrenia.
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Itopride-d6 hydrochloride
0 ImagesCat. No.: HY-B0732SCAS No.: 1346601-02-2Synonyms: HSR803-d6 hydrochloride
