2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Dopamine Receptor
  5. D2 Receptor Isoform

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:

D2 Receptor Related Products (277):

Cat. No. Product Name Effect Purity
  • HY-14539
    Clozapine
    		Antagonist 99.84%
    Clozapine (HF 1854) 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).
  • HY-14538
    Haloperidol
    		Antagonist 99.69%
    Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic agent. Haloperidol can be used in the study of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.
  • HY-11018
    Risperidone
    		Antagonist 99.87%
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-12705A
    Bromocriptine mesylate
    		Agonist 99.98%
    Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05. Bromocriptine mesylate is permeable to the blood-brain barrier.
  • HY-14546
    Aripiprazole
    		Agonist 99.95%
    Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.
  • HY-184208
    MCL-524
    		Agonist
    MCL-524 is a highly selective full agonist of the dopamine D2 receptor with a Kd value of 1.34 nM. MCL-524 specifically binds to the high-affinity state of the dopamine D2 receptor; this binding is abolished by guanylylimidodiphosphate, and it can distinguish between D2high and D2low sites. MCL-524 is applicable to research related to Parkinson's disease and schizophrenia.
  • HY-106587B
    Octoclothepin dimaleate
    		Antagonist
    Octoclothepin (Clorotepine) dimaleate is a D2 dopamine receptor antagonist and 5-HT2 serotonin receptor antagonist , with Ki values ​​of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D2, 5-HT2A, and 5-HT2C receptors, respectively. Octoclothepin dimaleate also binds to adrenergic receptors, with Ki values ​​of 0.66 nM, 0.56 nM, and 0.77 nM for α1a, α1b, and α1d, respectively. Octoclothepin dimaleate can be used in schizophrenia research.
  • HY-131531A
    5-OH-DPAT
    		Agonist
    5-OH-DPAT (5-Hydroxy-DPAT) is a potent and selective dopamine D2-receptor agonist lacking effects at 5-HT receptors. 5-OH-DPAT produces a moderate facilitation of the male rat sexual behavior.
  • HY-B1019
    Sulpiride
    		Antagonist 99.28%
    Sulpiride is an orally active dopamine D2/D3 receptor antagonist. Sulpiride is an atypical antipsychotic agent of the benzamide family. Sulpiride can be used in research into anxiety, depression and breast cancer.
  • HY-15780
    Brexpiprazole
    		Agonist 99.80%
    Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
  • HY-103414
    Raclopride
    		Antagonist 99.86%
    Raclopride is a dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively.
  • HY-B1077
    Penfluridol
    		Inhibitor 99.93%
    Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 μg/ml.
  • HY-15296
    Cabergoline
    		Agonist 99.86%
    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).
  • HY-B1115A
    Buspirone
    		Antagonist 99.86%
    Buspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research.
  • HY-B0590
    Tetrabenazine
    		Inhibitor 99.95%
    Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.
  • HY-10791
    Ritanserin
    		Inhibitor 99.68%
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
  • HY-N0049
    Nuciferine
    		Agonist 99.90%
    Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
  • HY-14763
    Cariprazine
    		Modulator 99.67%
    Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
  • HY-75502
    Rotigotine
    		Agonist 99.98%
    Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.
  • HY-B0411
    Domperidone
    		Inhibitor 99.87%
    Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.