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 (299)
Related Products (299)
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Biriperone
0 ImagesCat. No.: HY-137935CAS No.: 42021-34-1Synonyms: CentbutindoleBiriperone is a D1, D2, and 5-HT2A receptor antagonist with pKi values of 6.372, 7.88 and 7.619. Biriperone blocks amphetamine-induced hyperactivity and stereotypy in rodents. Biriperone blocks secondary conditioned avoidance responses in rodents. Biriperone can be used for the research of schizophrenia.
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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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Spectramide
0 ImagesCat. No.: HY-183927CAS No.: 125141-02-8Spectramide is a blood-brain barrier-permeable, reversible, and selective dopamine D2 receptor ligand. Spectramide shows no strong interactions with dopamine D1 receptors, dopamine uptake sites, adrenergic receptor systems, cholinergic receptor systems, or 5-HTR systems. Spectramide can be labeled with 11C or 123I isotopes for use in PET or SPECT. Spectramide preferentially accumulates in the striatum with low uptake in other brain regions, and its accumulation can be blocked by pre-administration of Haloperidol (HY-14538).
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MS1768
0 ImagesCat. No.: HY-187696CAS No.: 2349365-88-2MS1768 is a G protein-biased, partial, and selective D2R agonist. MS1768 selectively activates the Gi/o signaling pathway rather than recruiting β-arrestin2. MS1768 inhibits hyperkinesia. MS1768 can be used in studies of hyperkinesia.
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Dopamine D3 receptor ligand-5
0 ImagesCat. No.: HY-156239CAS No.: 2899250-94-1Dopamine D3 receptor ligand-5 (13a), a Cariprazine (HY-14763) analogue, is a dopamine D3 receptor ligand, with Ki values of 2.85 nM and 0.14 nM for D2R and D3R, respectively.
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Alentemol hydrobromide
0 ImagesCat. No.: HY-115418CAS No.: 112892-81-6Synonyms: U-68553BAlentemol hydrobromide (U-66444B) is a blood-brain barrier-permeable dopamine receptor D1, D2, D3, and D4 agonist. Alentemol hydrobromide 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 hydrobromide is applicable to research related to schizophrenia.
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Metoclopramide dihydrochloride hydrate
0 ImagesMetoclopramide dihydrochloride hydrate is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide dihydrochloride hydrate can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
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Abaperidone
0 ImagesCat. No.: HY-101619CAS No.: 183849-43-6Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
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Dehydrosertindole
0 ImagesCat. No.: HY-118477CAS No.: 173294-84-3Dehydrosertindole is a blood-brain barrier-permeable, orally active inhibitor of the dopamine D2 receptor. Dehydrosertindole occupies striatal dopamine D2 receptors to mediate receptor regulation. Dehydrosertindole is the active metabolite of Sertindole (HY-14543), which distributes rapidly in guinea pig myocardium and inhibits conditioned avoidance responses in rats. Dehydrosertindole can be used in research related to schizophrenia.
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(S)-Remoxipride hydrochloride hydrate
0 ImagesCat. No.: HY-101313BCAS No.: 117591-79-4Synonyms: (-)-Remoxipride hydrochloride hydrate(S)-Remoxipride ((-)-Remoxipride) hydrochloride hydrate ((S)-Remoxipride hydrochloride hydrate) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride hydrochloride hydrate can be used for the research of psychotic disorder.
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SNAP8719 free base
0 ImagesCat. No.: HY-123514CAS No.: 255893-38-0SNAP8719 free base is a selective α1D-adrenoceptor antagonist (pKi = 8.89). SNAP8719 free base shows affinity for the dopamine D2-, 5-HT1A-, and the human clonal α2a-adrenoceptor, with pKi values of 5.98, 6.47, and <5.0, respectively. SNAP8719 free base causes a concentration-dependent increase in the twitch response.
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Desethoxy Quetiapine dihydrochloride
0 ImagesCat. No.: HY-W151617ACAS No.: 329218-14-6Desethoxy Quetiapine dihydrochloride (Compound 28) is an antagonist for dopamine D2 receptor with an IC50 of 1330 nM. Desethoxy Quetiapine dihydrochloride antagonises Apomorphine (HY-12723)-induced climbing and swimming disruption in mouse models.
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SKF 83509
0 ImagesCat. No.: HY-111160CAS No.: 90955-43-4SKF 83509, a desmethyl analogue of SCH 23390 (HY-19545A), is a selective dopamine D1 antagonist with a Ki of 70.2 nM. SKF 83509 has no activity at dopamine D2 receptors.
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Cariprazine impurity 1
0 ImagesCat. No.: HY-47412CAS No.: 791778-53-5Cariprazine impurity 1 is a dopamine D2 receptor (D2R) agonist. Cariprazine impurity 1 modulates D2R-mediated Gi/o signaling pathway to inhibit cAMP production, and regulates D2R-mediated β-arrestin2 recruitment pathway.
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BL-1020 mesylate
0 ImagesCat. No.: HY-111136CAS No.: 916898-61-8BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate.
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FR 64822
0 ImagesCat. No.: HY-105294CAS No.: 102671-35-2FR 64822 is a dopamine D2 receptor agonist that can induce antinociceptive activity in rats and mice by indirectly stimulating dopamine D2 receptors. FR 64822 can promote penile erection in juvenile rats and improve amnesia in rats induced by scopolamine during passive avoidance tasks.
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Lurasidone metabolite 14326
0 ImagesCat. No.: HY-G0002CAS No.: 186204-33-1Lurasidone metabolite 14326 is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 can be used in the research of schizophrenia and bipolar depression.
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U-101958 maleate
0 ImagesCat. No.: HY-123663CAS No.: 224170-09-6Synonyms: PNU-101958 maleateU-101958 (PNU-101958) maleate is a highly selective ligand and antagonist for dopamine D4 receptor, with an IC50 of 2.7 nM. U-101958 maleate behaves as an agonist in HEK-293 cells expressing the human recombinant D4.4 receptor. U-101958 maleate is an antipsychotic.
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Benzquinamide
0 ImagesBenzquinamide (P2647; BZQ; Benzoquinamide) is an orally active binder of dopamine receptors and adrenergic receptors. Benzquinamide specifically targets dopamine D2, D3, D4 receptors and α-2A, α-2B, α-2C adrenergic receptors. Benzquinamide regulates blood pressure and heart rate, attenuates the pressor effect of adrenaline, and exhibits activities such as antiemesis, anxiolysis, and reduction of histamine-induced bronchoconstriction. Benzquinamide has good safety and does not deplete serotonin or norepinephrine in the brain. Benzquinamide can be used in studies related to nausea/vomiting, mental disorders, anxiety states, neurosis, and psychosis.
