Dopamine D2 receptor modulator-1
Dopamine D2 receptor modulator-1 is a positive allosteric modulator of hD2R. Dopamine D2 receptor modulator-1 enhances the potency of Dopamine (HY-B0451) on hD2R without intrinsic agonist activity. Dopamine D2 receptor modulator-1 protects dopaminergic differentiated cells from neurotoxic damage. Dopamine D2 receptor modulator-1 exhibits neuroprotective activity. Dopamine D2 receptor modulator-1 can be used in the research of Parkinson's disease.
For research use only. We do not sell to patients.
- CAS No.: 90471-34-4
- Formula: C14H20N4O3
- Molecular Weight:292.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Dopamine Receptor Isoforms
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Biological Activity
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hD2 Receptor |
Dopamine D2 receptor modulator-1 (Compound 6c) (0.01 nM; 10 min) acts as a potent positive allosteric modulator of hD2R expressed in CHO cells, increasing dopamine potency by 5.11-fold without intrinsic agonist activity[1].
Dopamine D2 receptor modulator-1 (compound 6c) (0.1-100 μM; 30 min) shows no cytotoxicity and minimal interaction with P-glycoprotein in MDCK-MDR1 cells at concentrations up to 100 μM[1].
Dopamine D2 receptor modulator-1 (compound 6c) (100 μM; 72 h) shows no significant cytotoxicity in HepG2 cells at 100 μM after 72 h of incubation[1].
Dopamine D2 receptor modulator-1 (compound 6c) (100 μM; 48 h) exhibits no significant neurotoxicity in dopaminergic-differentiated SH-SY5Y cells at 100 μM after 48 h of incubation[1].
Dopamine D2 receptor modulator-1 (compound 6c) (100 μM; 60 min preincubation, 48 h coincubation with 6-OHDA) provides significant neuroprotection against 6-OHDA-induced toxicity in dopaminergic-differentiated SH-SY5Y cells at 100 μM, with enhanced protection observed at 50-100 μM 6-OHDA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:100 μM
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Incubation Time:72 h
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Result:Demonstrated no significant cytotoxicity relative to untreated control cells, as measured by mitochondrial metabolic activity.
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Cell Line:Dopaminergic-differentiated SH-SY5Y neuroblastoma cells
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Concentration:100 μM
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Incubation Time:48 h
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Result:Showed no significant cytotoxicity in either the MTT reduction or neutral red (NR) uptake assays, indicating no impairment of mitochondrial function or lysosomal integrity.
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Cell Line:Dopaminergic-differentiated SH-SY5Y human neuroblastoma cells exposed to 6-hydroxydopamine (6-OHDA)
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Concentration:100 μM (preincubation); 50-100 μM (6-OHDA)
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Incubation Time:60 min (preincubation); 48 h (coincubation with 6-OHDA)
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Result:Improved cell viability by approximately 10% relative to the 0.5% DMSO + 6-OHDA control group at 50 and 75 μM 6-OHDA.
Significantly rescued cell survival by 12% (62.44% viability, p < 0.01) compared to the control group at 100 μM 6-OHDA.
Chemical Information
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CAS No. 90471-34-4
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Molecular Weight 292.33
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Formula C14H20N4O3
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SMILES
O=C(N)CNC([C@H](CC(C)C)NC(C1=CN=CC=C1)=O)=O
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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)