AMPA-IN-2
AMPA-IN-2 is an orally active AMPA inhibitor that can cross the blood-brain barrier. AMPA-IN-2 improves epileptic seizures by inhibiting the intrinsic excitability of neurons and inhibiting the excitability of glutamatergic transmission. AMPA-IN-2 exerts anti-epileptic effects in the pentylenetetrazol (PTZ) model and can be used as a promising candidates with high broad-spectrum anti-epileptic potential.
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- CAS. Nr.: 75828-06-7
- Formel: C12H18O
- Molecular Weight:178.27
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
AMPA-IN-2 (compound 13) (1 μM, 10 μM) suppresses the intrinsic excitability of neurons and inhibits the excitability of glutamatergic synaptic transmission[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-24 | Cmax | Tmax | CL | Vss | F |
|---|---|---|---|---|---|---|---|---|---|
| Rat | 20 mg/kg | p.o. | 5.72 h | 1962.70 μg/L·h | 474.29 μg/L | 0.50 h | 9.76 L/h/kg | 80.52 L/kg | 114.8 % |
| Rat | 5 mg/kg | i.v. | 1.85 h | 427.55 μg/L·h | 164.26 μg/L | 0.14 h | 11.75 L/h/kg | 31.18 L/kg | / |
In Vivo
AMPA-IN-2 (compound 13) (100 mg/kg, i.p., once) shows anti-epileptic effect and reduces mortality in the maximal electroshock (MES)-induced epilepsy model[1].
AMPA-IN-2 (30 mg/kg 100 mg/kg, i.p., once) demonstrates high anti-epileptic efficacy in the PTZ-induced epilepsy model[1].
AMPA-IN-2 (100 mg/kg, i.p., once) alleviates the severity seizure in a Chronic Hippocampal-Kindled Epilepsy Model[1].
AMPA-IN-2 (30 mg/kg, p.o., once) shows anti-epileptic effect in the PTZ-induced epilepsy model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The MES-induced epilepsy model[1]
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Dosage:100 mg/kg
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Administration:i.p., once
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Result:Showed anti-epileptic effect and reduced mortality in the MES-induced epilepsy model
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Animal Model:The PTZ-induced epilepsy model[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
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Administration:i.p., once
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Result:Prolonged the latency to seizure stages 2, 4, and 6, maintained a lasting therapeutic action, respectively, with no mortality observed.
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Animal Model:Chronic Hippocampal-Kindled Epilepsy Model[1]
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Dosage:100 mg/kg
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Administration:i.p., once
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Result:Attenuated seizure severity in the kindled mice, as demonstrated by a decrease in the behavioral seizure stage from 5.0 to 3.5.
Shortened the generalized seizure duration (GSD) from 17.80 to 9.60 s, but it led to an undesirable increase in the after-discharge duration (ADD).
Chemical Information
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CAS. Nr. 75828-06-7
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Molecular Weight 178.27
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Formel C12H18O
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SMILES
C[C@]12[C@](O)(C[C@@H](CC2)C1(C)C)C#C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AMPA-IN-2 Related Classifications
HY-174899 Related Classifications
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