Homo-AMPA
Homo-AMPA is a stereospecific mGluR6 agonist (EC50 = 58 μM) and a weak NMDA (HY-17551) receptor antagonist (IC50 = 131 μM), exerting anxiolytic-like effects and modulating pain-responsive neuronal activity through selective activation of mGluR6. Homo-AMPA can serve as a standard agonist for the pharmacological characterization of mGluR6 in related studies.
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- No. CAS: 179169-88-1
- Fòrmula: C8H12N2O4
- Peso molecular:200.19
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
IC50 & Target
[2]|
mGluR6 58 μM (EC50) |
In Vitro
Homo-AMPA is a potent mGluR agonist that specifically activates mGluR6[2].
Homo-AMPA (1000 μM; 100 μM) lacks detectable agonist activity in rat cortical slice preparations (EC50 > 1000 μM) and shows no antagonist activity at 100 μM[5].
Homo-AMPA (1-300 μM) does not alter extracellular glutamate levels in the nucleus accumbens of adult rats[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Homo-AMPA (microinjected into the ventrolateral midbrain periaqueductal gray (vl-PAG)) modulates RVM ON and OFF cell activity in a manner consistent with the pain-inhibitory effect of mGluR6 within the PAG[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:250 nmol/rat
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Administration:local administration into the hippocampus
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Result:Produced an anxiolytic-like effect at 250 nmol/rat.
Reversed by (RS)-α-cyclopropyl-4-phosphonophenylglycine (CPPG).
Chemical Information
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No. CAS 179169-88-1
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Peso molecular 200.19
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Fòrmula C8H12N2O4
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SMILES
O=C1NOC(C)=C1CCC(C(O)=O)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)