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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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).
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SSR-181507 hydrochloride
0 ImagesCat. No.: HY-19372CAS No.: 223502-85-0SSR-181507 hydrochloride is a dopamine D2 receptor antagonist and 5-HT1A receptor agonist. SSR-181507 antagonizes Apomorphine (HY-12723)-induced climbing in mice and stereotypies in rats. SSR-181507 hydrochloride can be used in the research of depression and anxiety.
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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.
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Roxindole
0 ImagesCat. No.: HY-106100CAS No.: 112192-04-8Synonyms: EMD 49980Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor. Antipsychotic and antidepressant activities.
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Flupenthixol decanoate
0 ImagesCat. No.: HY-105657CAS No.: 30909-51-4Flupenthixol decanoate is a dopamine D2 receptor antagonist with antipsychotic effects. Flupenthixol decanoate can be used for schizophrenia and depression research.
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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).
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Clocapramine dihydrochloride hydrate
0 ImagesCat. No.: HY-B2073ACAS No.: 60789-62-0Synonyms: 3-Chlorocarpipramine dihydrochloride hydrateClocapramine hydrochloride hydrate is an antagonist of the D2 and 5-HT2A receptors.
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BGC20-761
0 ImagesCat. No.: HY-21995CAS No.: 17375-63-2BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor Ki values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent.
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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).
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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.
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(-)-IHCH7041
0 ImagesCat. No.: HY-153162ACAS No.: 2813335-07-6(-)-IHCH7041 (Compound (-)-(S)-I-10) is a selective and orally active dopamine D2 receptor agonist with a Ki of 22.44 nM. (-)-IHCH7041 can activate Gαi1 protein and β-arrestin2 signaling pathway with EC50 values of 1.38 and 2.75 nM. (-)-IHCH7041 can improve cognitive impairment and memory capacity. (-)-IHCH7041 can be used for the research of neurological disease, such as Alzheimer's disease.
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Clozapine dihydrochloride
0 ImagesCat. No.: HY-14539BCAS No.: 2711603-38-0Synonyms: HF 1854 dihydrochlorideClozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
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RU-24213 hydrochloride
0 ImagesCat. No.: HY-136786CAS No.: 67383-44-2RU-24213 hydrochloride is a selective D-2 dopamine receptor agonist. RU-24213 hydrochloride is also a KAPPA-opioid receptor antagonist. RU-24213 hydrochloride induces stereotyped behaviors.
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Itopride
0 ImagesCat. No.: HY-B0732ACAS No.: 122898-67-3Synonyms: HSR803 free baseItopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).
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Haloperidol-13C6
0 ImagesCat. No.: HY-14538S3Haloperidol-13C6 is the 13C6 labeled Haloperidol. Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.
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Antipsychotic agent-2
0 ImagesCat. No.: HY-149247CAS No.: 3043786-44-0Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability.
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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.
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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.
