1. シグナル伝達
  2. GPCR/G Protein
    Neuronal Signaling
  3. Dopamine Receptor

Dopamine Receptor

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.

製品番号 製品名 製品効果 純度 構造式
  • HY-179724
    PZ-1657 Inhibitor
    PZ-1657 (Compound 57) is an orally active, blood-brain barrier permeable, highly selective, and metabolically stable 5-HT7 receptor inverse agonist with a Ki value of 5 nM. PZ-1657 inhibits constitutive cyclic adenosine monophosphate (cAMP) production mediated by the Gs signaling pathway (EC50 value of 2.93 nM). PZ-1657 inhibits CYP3A4 P450 (IC50 = 12.2 μM) and hERG channels. PZ-1657 reduces 5-HT7 receptor-mediated MMP-9 activity. PZ-1657 reverses Phencyclidine-induced cognitive impairment. PZ-1657 possesses antidepressant properties.
    PZ-1657
  • HY-W744750
    TDHL-d10
    TDHL-d10 (Tergurid-d10; Terguride-d10; trans-Dihydrolisuride-d10) is the deuterium labeled TDHL (HY-12714). TDHL (Tergurid) is a dopamine receptor agonist with a Kd of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.
    TDHL-d<sub>10</sub>
  • HY-A0007R
    Rotigotine Hydrochloride (Standard) Agonist
    Rotigotine (Hydrochloride) (Standard) is the analytical standard of Rotigotine (Hydrochloride). This product is intended for research and analytical applications. Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki 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 Hydrochloride (Standard)
  • HY-119463
    Trepipam Antagonist
    Trepipam (Trimopam; SCH-12679) is a D1-dopamine receptor antagonist. Trepipam can reduce the self-injurious behavior in 6-OHDA-lesioned rats. Trepipam can be used in the research of epilepsy and anxiety neurosis.
    Trepipam
  • HY-179724A
    PZ-1657 hydrochloride Inhibitor
    PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a Ki of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder.
    PZ-1657 hydrochloride
  • HY-149481
    D4R agonist-1 Agonist
    D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders.
    D4R agonist-1
  • HY-182437
    ASP4345 free base MDM2 Inhibitor
    ASP4345 free base is a blood-brain barrier-permeable dopamine D1 receptor modulator. ASP4345 free base binds to the allosteric site of the dopamine D1 receptor, thereby enhancing dopamine activity. ASP4345 free base can be used in the research of schizophrenia and Parkinson's disease.
    ASP4345 free base
  • HY-15856BR
    Flupentixol dihydrochloride (Standard) Antagonist
    Flupentixol (dihydrochloride) (Standard) is the analytical standard of Flupentixol (dihydrochloride). This product is intended for research and analytical applications. Flupentixol 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.
    Flupentixol dihydrochloride (Standard)
  • HY-15780A
    Brexpiprazole hydrochloride Agonist
    Brexpiprazole (OPC-34712) hydrochloride, 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 hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
    Brexpiprazole hydrochloride
  • HY-129089
    (-)-MDO-NPA Ligand
    (-)-MDO-NPA is an N-propylnorapomorphine analog and a D1R/D2R dual-target ligand. (-)-MDO-NPA has EC50 values of 1949 nM (D1R) and 520 nM (D2R) for β-arrestin. (-)-MDO-NPA has EC50 values of 717.5 nM (D1R) and 7.7 nM (D2R) for cAMP. (-)-MDO-NPA can be used in the research of dopamine-related diseases such as Parkinson’s disease.
    (-)-MDO-NPA
  • HY-B1196A
    Tiapride Antagonist
    Tiapride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride shows anti-dyskinetic activity and anxiolytic activity. Tiapride is a neuroleptic agent.
    Tiapride
  • HY-116430
    (S)-SKF-77434 Ligand
    (S)-SKF-77434 (Compound 11) ((S)-APB) is an enantiomer of SKF-77434 (HY-103417). (S)-SKF-77434 shows an affinity for the D1 receptor with an IC50 of 2800 nM. (S)-SKF-77434 can be used in the research of neuropsychiatric disorders.
    (S)-SKF-77434
  • HY-149387
    D3R/MOR antagonist 2 Antagonist
    D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism.
    D3R/MOR antagonist 2
  • HY-175556
    CNV-dopamine Agonist
    CNV-dopamine is a photoreleasable D2 receptor-selective agonist. CNV-dopamine activates D2 receptors and induces G protein-coupled inwardly rectifying potassium (GIRK) currents. CNV-dopamine is promising for research of disorders like Parkinson’s disease and addiction.
    CNV-dopamine
  • HY-N18279
    Bulbocapnine Antagonist
    Bulbocapnine is an aporphine isoquinoline alkaloid that exerts antagonistic effects on dopamine Receptor) and α-adrenergic receptors, as well as anti-peroxidative effects. The Ki value of bulbocapnine for tyrosine hydroxylase (TH) is 0.20 mM. Bulbocapnine reduces intracellular dopamine content, inhibits TH activity, and decreases Ca2+ concentration. Bulbocapnine antagonizes the dose-dependent inhibitory effect of dopamine on the heart rate acceleration induced by stimulating the postganglionic fibers of the right cardiac accelerator nerve.
    Bulbocapnine
  • HY-124270
    Sibenadet hydrochloride Agonist
    Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.
    Sibenadet hydrochloride
  • HY-19262
    TAK-218 Inhibitor
    TAK-218 is a promising candidate as an agent tor central nervous system trauma and ischemia. TAK-218 exhibits potent scavenging activity and antioxidative activity. TAK-218 also inhibits dopamine release.
    TAK-218
  • HY-111242
    SV 156 Antagonist
    SV 156 is a potent and selective D2 dopamine receptor antagonist, with a Ki of 2.5 nM for hD2. SV 156 has approximately 40-fold binding selectivity for D2 dopamine receptors compared to the D3 receptor subtype. SV 156 can be used for L-DOPA (HY-N0304)-associated abnormal involuntary movements (AIMs) research.
    SV 156
  • HY-119768
    (±)-BAK2-66 Antagonist
    (±)-BAK2-66 is a selectivity dopamine D3 receptor antagonist with theKi values of 1nM and 960 nM for D3R and D2R, respectively. (±)-BAK2-66 can be used for study in animal models of addiction.
    (±)-BAK2-66
  • HY-101313
    (S)-Remoxipride Antagonist
    (S)-Remoxipride ((-)-Remoxipride) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride can be used for the research of psychotic disorder.
    (S)-Remoxipride
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