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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Piribedil hydrochloride
0 ImagesCat. No.: HY-12707CCAS No.: 78213-63-5Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
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NRA-0562
0 ImagesCat. No.: HY-182504CAS No.: 244276-65-1NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia..
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Ordopidine
0 ImagesCat. No.: HY-19845CAS No.: 871351-60-9Synonyms: ACR-325Ordopidine is a dopamine D2 receptor antagonist. Ordopidine can inhibit hyperactivity caused by psychostimulants. Ordopidine can be used in neurological research.
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EF-7412
0 ImagesCat. No.: HY-182677CAS No.: 221452-76-2EF-7412 is a dual antagonist of the 5-HT1A receptor and dopamine D2 receptor, with Ki values of 27 nM and 22 nM, respectively. EF-7412 acts as an antagonist at both pre- and postsynaptic 5-HT1A receptor sites, blocking 8-OH-DPAT (HY-112061)-induced hypothermia, behavioral syndrome, and corticosterone elevation in vivo. EF-7412 increases hypothalamic 5-HIAA/5-HT and DOPAC/DA ratios, alters 5-HT and DA neuronal activity, and slightly decreases spontaneous motor activity. EF-7412 can be used for research on 5-HT1A/D2 receptor regulation and related neural pathways.
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PD 118717
0 ImagesCat. No.: HY-114578CAS No.: 104229-37-0PD 118717 is a selective dopamine (DA) D-2 autoreceptor agonist. PD 118717 has significant affinity for 5-HT1A but not 5-HT1B and 5-HT2 receptors. PD 118717 is active in antagonizing the tau-Butyrolactone-induced accumulation of dopa in rat striatum and mesolimbic regions. PD 118717 exhibits an antipsychotic-like profile.
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BMY 28674
0 ImagesCat. No.: HY-100057CAS No.: 125481-61-0Synonyms: 6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
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Dehydrate haloperidol
0 ImagesCat. No.: HY-W708196CAS No.: 52669-92-8Dehydrohaloperidol, Haloperidol (HY-14538) analogue, is a selective human dopamine D2 receptor antagonist with a pKd of 8 and a pki of 8. Dehydrohaloperidol can be used for the research of schizophrenia.
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Asenapine citrate
0 ImagesCat. No.: HY-10121BCAS No.: 1411867-74-7Synonyms: Org 5222 citrateAsenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder.
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Flupentixol
0 ImagesFlupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.
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Dopamine D2 receptor agonist-3
0 ImagesDopamine D2 receptor agonist-3 (compound 3) is a selective D2 receptor partial agonist and Dopamine D3 receptor antagonist (with pEC50 of 8.3 and <5.5 respectively).
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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.
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CSP-2503
0 ImagesCat. No.: HY-180372CAS No.: 581813-10-7CSP-2503 is a potent and selective 5-HT1A receptor agonist , with an EC50 of 0.15 μM and a Ki of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (Ki > 1000 nM), 5-HT4 receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.
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Dopamine D4 receptor ligand 2
0 ImagesCat. No.: HY-157563CAS No.: 219125-63-0Dopamine D4 receptor ligand 2 (compound 17) is a potent and selective dopamine D4 ligand with IC50 values of 0.057, >1000, 220, 270 nM for D4, D2, 5-HT1A, α1, respectively.
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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.
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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.
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Dopamine D2 receptor modulator-1
0 ImagesCat. No.: HY-184573CAS No.: 90471-34-4Dopamine D2 receptor modulator-1 is a positive allosteric modulator of hD2R. Dopamine D2 receptor modulator-1 enhances the potency of Dopamine (HY-B0451) on hD2R without intrinsic agonist activity. Dopamine D2 receptor modulator-1 protects dopaminergic differentiated cells from neurotoxic damage. Dopamine D2 receptor modulator-1 exhibits neuroprotective activity. Dopamine D2 receptor modulator-1 can be used in the research of Parkinson's disease.
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Bromperidol hydrochloride
0 ImagesSynonyms: R-11333 hydrochlorideBromperidol (R-11333) hydrochloride possesses antipsychotic activity, with a high affinity for central dopamine receptors D2. Bromperidol hydrochloride can kill Mycobacteria in a synergistic manner with Spectinomycin.
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PZ-1129
0 ImagesCat. No.: HY-179725CAS No.: 1919029-61-0PZ-1129 is a selective 5-HT7 receptor ligand with a Ki of 7 nM. PZ-1129 shows Ki values of 159 and 24 nM for 5-HT1A receptor and D2 receptor. PZ-1129 can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 13.7 nM). PZ-1129 can be used for the research of emotional disorders, such as depression and bipolar disorder.
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Loxapine hydrochloride
0 ImagesCat. No.: HY-17390BCAS No.: 54810-23-0Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
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Sibenadet
0 ImagesCat. No.: HY-135487CAS No.: 154189-40-9Synonyms: AR-C68397AA free base; AR-C68397XXSibenadet (AR-C68397AA free base) is a dual dopamine D2/β2-adrenoceptor agonist with selective β2-adrenoceptor agonism. Sibenadet inhibits capsaicin-induced plasma protein extravasation in rat trachea. Sibenadet suppresses edema from sensory nerve fiber activation by activating β2-adrenoceptor. Sibenadet is promising for research of chronic obstructive pulmonary disease (COPD).
