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

Dopamine Receptor

Dopamine Receptor

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Dopamine Receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling. Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders. Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine receptors. There are at least five subtypes of dopamine receptors, D1, D2, D3, D4, and D5. The D1 and D5 receptors are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4receptors are members of the D2-like family.

Dopamine Receptor Isoform Specific Products:

Dopamine Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-163703
    D4R antagonist-2
    		Antagonist
    D4R antagonist-2 (compound 33) is a D4R antagonist. D4R antagonist-2 has a IC50 value of 210 nM, and a Ki value of 59 nM for D4R. D4R antagonist-2 can be used in the Parkinson's disease research.
    D4R antagonist-2
  • HY-103404
    PNU-96415E
    		Antagonist
    PNU-96415E is a selective D4/5-HT2A antagonist. PNU-96415E may have potential antipsychotic efficacy.
    PNU-96415E
  • 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.
    Octoclothepin dimaleate
  • HY-B0520AS1
    Benztropine-d3 mesylate
    Benztropine-d3 (mesylate) is the 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.
    Benztropine-d<sub>3</sub> mesylate
  • HY-B0457AS
    Clomipramine-d3
    		Inhibitor
    Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
    Clomipramine-d<sub>3</sub>
  • HY-101080
    3'-Fluorobenzylspiperone maleate
    3'-Fluorobenzylspiperone maleate is a ligand for dopamine D2 receptors with activity in improving behavioral disorders. 3'-Fluorobenzylspiperone maleate showed better inhibitory effects than placebo, especially in reducing behavioral disorders.
    3'-Fluorobenzylspiperone maleate
  • HY-101349A
    L 741742 hydrochloride
    		Antagonist
    L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma.
    L 741742 hydrochloride
  • HY-181047
    FMJ-01-042
    		Agonist
    FMJ-01-042 is a blood-brain barrier-permeable, low-efficacy partial agonist with high affinity (Kᵢ = 4.33 nM) and exceptional subtype selectivity for the dopamine D4 receptor. FMJ-01-042 exhibits good metabolic stability and is suitable for research on neurological and psychiatric disorders.
    FMJ-01-042
  • HY-107434
    Molindone
    		Antagonist
    Molindone ((±)-Molindone), an indole derivative, is a potent dopamine D2 and D5 receptor antagonist. Molindone ((±)-Molindone) can be used for the research of schizophrenia and severe mental illness.
    Molindone
  • HY-12751S
    Trimethobenzamide-d6
    		Inhibitor
    Trimethobenzamide-d6 is deuterium labeled Trimethobenzamide. Trimethobenzamide is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
    Trimethobenzamide-d<sub>6</sub>
  • HY-119980B
    Fluphenazine hydrochloride
    		Antagonist
    Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.
    Fluphenazine hydrochloride
  • HY-114576
    Nooglutil
    		Modulator
    Nooglutil (Nooglutyl; ONK-10) is a positive modulator of AMPA-type glutamate receptors (AMPARs). Nooglutil also regulates dopamine D2 receptor function to exert anxiolytic effects. Nooglutil is promising for research of neurodegenerative disorders (e.g., Alzheimer’s disease).
    Nooglutil
  • HY-111155
    RBI-257 maleate
    		Antagonist
    RBI-257 maleate is a potent dopamine D4 receptor antagonist with a Ki value of 0.3 nM.
    RBI-257 maleate
  • HY-103109
    Melperone hydrochloride
    		Antagonist
    Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone hydrochloride
  • HY-W681014
    5-Fluoro-α-methyltryptamine hydrochloride
    5-Fluoro-α-methyltryptamine hydrochloride may cause an increase in intracellular levels of 5-HT followed by an increase in 5-HT release. 5-Fluoro-α-methyltryptamine hydrochloride exhibits EC50 values of 37 nM, 14 nM, 78 nM and 8.47 nM for DA, 5HT, NE and 5-HT2A, respectively.
    5-Fluoro-α-methyltryptamine hydrochloride
  • HY-14325A
    L-745870 trihydrochloride
    		Antagonist
    L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
    L-745870 trihydrochloride
  • HY-W284026
    PIM-35
    		Inhibitor
    PIM-35 is a derivative of Indole (HY-W001132). PIM-35 significantly inhibits serotonin (5HT) and dopamine (DA) uptake with a weak inhibitory effect on noradrenaline (NA) uptake.PIM-35 has antidepressant activity and can be used for depression research.
    PIM-35
  • HY-W748582
    Clozapine N-oxide-d8
    Clozapine N-oxide-d8 is the deuterium labeled Clozapine N-oxide (HY-17366). Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
    Clozapine N-oxide-d<sub>8</sub>
  • 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.
    5-OH-DPAT
  • HY-109167A
    Aramisulpride hydrochloride
    		Antagonist
    Aramisulpride hydrochloride is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride hydrochloride is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride hydrochloride can be used in psychiatric research.
    Aramisulpride hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Dopamine Receptor Isoform Comparison

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