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 (296)
Related Products (296)
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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).
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Lirexapride
0 ImagesCat. No.: HY-105524CAS No.: 145414-12-6Lirexapride is a 5-HT4/Dopamine D2 receptor agonist. Lirexapride stimulants gastrointestinal motor. Lirexapride can be used for research on digestive system disorders.
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(Z)-Flupenthixol decanoate
0 ImagesCat. No.: HY-105657ACAS No.: 69079-98-7(Z)-Flupenthixol decanoate is the cis form of Flupenthixol decanoate. (Z)-Flupenthixol decanoate is a potent dopamine D1/D2 receptor antagonist. (Z)-Flupenthixol decanoate shows antipsychotic effect.
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Carmoxirole
0 ImagesCat. No.: HY-105112CAS No.: 98323-83-2Synonyms: EMD 45609Carmoxirole (EMD 45609) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo.
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5-HT2A receptor agonist-13
0 ImagesCat. No.: HY-1790635-HT2A receptor agonist-13 (Compound 28c) is a partial agonist of the 5-HT2A receptor, with an EC50 value of 416.9 nM and a Ki value of 113.9 nM. 5-HT2A receptor agonist-13 exhibits very weak agonistic activity towards the 5-HT2B receptor (EC50 = 120.2 nM), D2 receptor (Ki = 1298 nM), and has no activity towards the 5-HT2C receptor. 5-HT2A receptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC50 = 977.2 nM). 5-HT2A receptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2A receptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD).
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Blonanserin-d8
0 ImagesCat. No.: HY-13575SCAS No.: 2732761-71-4Synonyms: AD-5423-d8Blonanserin-d8 is a deuterium labeled Blonanserin. Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic.
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Bromocriptine-13C,d3
0 ImagesCat. No.: HY-12705SBromocriptine-13C,d3 is the 13C- and deuterium labeled Bromocriptine. Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.
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FMJ-01-054
0 ImagesCat. No.: HY-181049FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a Ki od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R. FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC50 values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders.
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Promazine
0 ImagesPromazine (Romtiazin) is an antipsychotic and a dopamine receptor D2 antagonist. Promazine inhibits dopaminergic neurotransmission.
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Raclopride tartrate
0 ImagesCat. No.: HY-108976CAS No.: 98185-20-7Raclopride tartrate is a selective dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride tartrate binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively.
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BMS-570520
0 ImagesCat. No.: HY-182735CAS No.: 388101-58-4BMS-570520 is an orally bioavailable CCR3 antagonist with an IC50 of 1.9 nM against hCCR3 and an IC50 of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis.
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Dopamine D3 receptor ligand-4
0 ImagesCat. No.: HY-115968CAS No.: 2376333-77-4Dopamine D3 receptor ligand-4 (compound 6) is a potent and selective dopamine D3 receptor ligand, with a Ki of 0.5 nM. Dopamine D3 receptor ligand-4 shows high level of selectivity for D3 over D2 (Ki=7.43 nM).
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Tipepidine citrate
0 ImagesCat. No.: HY-B2185CAS No.: 14698-07-8Tipepidine citrate is a non-narcotic antitussive agent. Tipepidine citrate reversibly inhibits dopamine D2 receptor-mediated GIRK current (IDA(GIRK)), thereby activating VTA dopamine neurons, with an IC50 of 7.0 μM for IDA(GIRK). Tipepidine activates AMPK. Tipepidine citrate has antidepressant-like effects. Tipepidine citrate enhances the analgesic effect of Carbamazepine (HY-B0246). Tipepidine citrate improves adipose tissue fibrosis and glucose intolerance in high-fat diet-induced obese mice.
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Benztropine-13C,d3 mesylate
0 ImagesCat. No.: HY-B0520ASBenztropine-13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
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Fluoroclebopride
0 ImagesFluoroclebopride is a Dopamine receptor ligand with a binding Ki of 0.95 nM for the dopamine D2 receptor and a binding Ki of 5.46 nM for the dopamine D3 receptor. When radiolabeled with 18F, Fluoroclebopride can be used to detect the availability of dopamine D2 and D3 receptors in the caudate nucleus and putamen of primates.
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Mazapertine
0 ImagesMazapertine is an orally active antipsychotic agent. M azapertine antagonizes to dopamine D2/3/4 receptors (Ki values < 3 nM) and also strongly binds to serotonin 5-HT1A receptor (Ki =1.7 nM) and α1-adrenergic receptor (Ki = 1.3 nM). Mazapertine can be used for the research of neurological disease.
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Cinitapride monotartrate
0 ImagesCat. No.: HY-128386CAS No.: 1207859-16-2Cinitapride monotartrate is a 5-HT1A and 5-HT4 agonist. Cinitapride monotartrate is also a 5-HT2A and D2 antagonist. Cinitapride monotartrate can be used for the research of functional dyspepsia.
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Metopimazine acid-d6 (hydrochloride)
0 ImagesCat. No.: HY-143994SMetopimazine-d6 hydrochloride is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks.
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Bifeprunox
0 ImagesCat. No.: HY-14547CAS No.: 350992-10-8Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia.
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Bromopride hydrochloride
0 ImagesCat. No.: HY-B1164ACAS No.: 52423-56-0Bromopride hydrochloride is a selective, irreversible, competitive, and orally active dopamine D2 receptor antagonist. Bromopride hydrochloride can pass through the blood-brain barrier, inhibit the vomiting center, and enhance gastrointestinal motility, exerting antiemetic and gastrointestinal motility effects. Bromopride hydrochloride antagonizes dopamine-mediated vomiting reflexes and promotes gastrointestinal smooth muscle contraction, and has no adverse effects on abdominal wall healing in rats with postoperative abdominal infection. Bromopride hydrochloride can be used for the study of digestive system diseases (such as gastric hypomotility, nausea and vomiting).
