Dopamine D2 receptor agonist-4
Dopamine D2 receptor agonist-4 is a blood-brain barrier permeable Dopamine D2 receptor agonist with an EC50 value of 0.03 nM. Dopamine D2 receptor agonist-4 reduces intracellular cAMP levels. Dopamine D2 receptor agonist-4 acts as a Ferroptosis inhibitor and iron chelator, selectively chelating iron ions, reducing intracellular ferrous ion levels, and exerting cytoprotective effects against iron-dependent ferroptosis in vitro. Dopamine D2 receptor agonist-4 improves motor dysfunction and exerts neuroprotective effects in mouse models of Parkinson's disease. Dopamine D2 receptor agonist-4 can be used in studies related to Parkinson's disease.
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- CAS No.: 2977213-17-3
- Formula: C25H36N2O3
- Molecular Weight:412.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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D2 Receptor 0.03 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
0.03 nM
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Dopamine D2 receptor agonistic activity in human recombinant D2 dopamine receptor-stable HEK-293 cells assessed via LANCE® Ultra cAMP assay with 1 h incubation of test compound followed by 1 h incubation with Eu-cAMP tracer and ULight™-anti-cAMP solution, detected at 665 nm on EnVision.
Dopamine D2 receptor agonistic activity in human recombinant D2 dopamine receptor-stable HEK-293 cells assessed via LANCE® Ultra cAMP assay with 1 h incubation of test compound followed by 1 h incubation with Eu-cAMP tracer and ULight™-anti-cAMP solution, detected at 665 nm on EnVision.
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42480356 |
| SH-SY5Y | CC50 |
>100 μM
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Cytotoxicity in human neuroblastoma SH-SY5Y cells assessed via Cell Counting Kit-8, with treatment alone showing no effect on cell proliferation.
Cytotoxicity in human neuroblastoma SH-SY5Y cells assessed via Cell Counting Kit-8, with treatment alone showing no effect on cell proliferation.
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42480356 |
Dopamine D2 receptor agonist-4 (Compound 27e) (1 h) potently activates the D2 receptor in HEK-293 cells, with an EC50 value of 0.03 nM[1].
Dopamine D2 receptor agonist-4 (50 μM) selectively binds FeIII and FeII, but does not bind ZnII, in cell-free UV-visible absorption spectroscopy assays[1].
Dopamine D2 receptor agonist-4 (0.5-50 μM; up to 96 h) exerts a dose-dependent neuroprotective effect against MPP+ -induced injury in SH-SY5Y cells, and exhibits higher potency than Rotigotine (HY-75502) within the concentration range of 0.5 μM to 2.0 μM[1].
Dopamine D2 receptor agonist-4 exhibits weak cytotoxicity in SH-SY5Y cells, with a CC50 greater than 100 μM[1].
Dopamine D2 receptor agonist-4 (10 μM; 16 h) exhibits favorable blood-brain barrier permeability, with a measured Pe value of 2.20 × 10-6 cm/s in the cell-free PAMPA assay[1].
Dopamine D2 receptor agonist-4 (2.0 μM; 24 h) inhibits MPP+-induced lipid peroxidation in SH-SY5Y cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y human neuroblastoma cells
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Concentration:25-50 μM (co-treated with 1.5 mM MPP+ for cell viability assessment); 0.5-2.0 μM (co-treated with 1.5 mM MPP+ for 96 h)
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Incubation Time:Up to 96 h (cell viability assessment); 96 h (0.5-2.0 μM group)
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Result:Dose-dependently reversed MPP+-induced cell death; treatment with 25 μM and 50 μM significantly increased cell viability compared to MPP+-only treated cells.
At 0.5 μM, 1.0 μM, and 2.0 μM, conferred significant protection against MPP+-induced injury, with greater efficacy than rotigotine at equivalent concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8- to 9-week-old, MPTP-induced acute Parkinson's disease model)[1]
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Dosage:1 mg/kg
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Administration:i.p.; pre-administered starting 3 days before MPTP exposure
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Result:Ameliorated MPTP-induced motor dysfunction, with time spent on the rotating rod comparable to rotigotine at the same dose.
Reversed the MPTP-induced reduction of TH-positive dopaminergic neurons in the substantia nigra, with a better protective effect against dopaminergic neuron loss than rotigotine at the same dose.
Chemical Information
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CAS No. 2977213-17-3
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Molecular Weight 412.56
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Formula C25H36N2O3
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SMILES
O=C1C(O)=C(C)N(CCCCCCN([C@@H]2CC3=C(C(O)=CC=C3)CC2)CCC)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dopamine D2 receptor agonist-4 Related Classifications
HY-187430 Related Classifications
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