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GYKI-47261 dihydrochloride

Catalog No. T38601   CAS 1217049-32-5

GYKI-47261 dihydrochloride is a selective AMPA receptor antagonist, administered orally, and exhibits competitive activity with an IC 50 of 2.5 μM. It displays a wide range of anticonvulsive effects and demonstrates neuroprotective properties. Additionally, GYKI-47261 dihydrochloride is a potent inducer of CYP2E1.

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GYKI-47261 dihydrochloride Chemical Structure
GYKI-47261 dihydrochloride, CAS 1217049-32-5
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GYKI-47261 dihydrochloride is a selective AMPA receptor antagonist, administered orally, and exhibits competitive activity with an IC 50 of 2.5 μM. It displays a wide range of anticonvulsive effects and demonstrates neuroprotective properties. Additionally, GYKI-47261 dihydrochloride is a potent inducer of CYP2E1.
In vivo GYKI-47261 dihydrochloride, administered intravenously at 6 mg/kg, demonstrates an anti-ischemic effect in a rat model of transient focal ischemia. When given orally, it effectively reduces tremors induced by oxotremorine in male CD1 mice, with an ED50 of 16.8 mg/kg. Additionally, an intraperitoneal dose of 20 mg/kg in male C57 black mice (weighing 23-30 g) counteracts the dopamine depletion caused by MPTP, showing a reversal in the reduced striatal concentrations.
Molecular Weight 395.71
Formula C18H17Cl3N4
CAS No. 1217049-32-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Abrahám G, et al. New non competitive AMPA antagonists. Bioorg Med Chem. 2000;8(8):2127-2143. 2. Tamási V, et al. GYKI-47261, a new AMPA [2-amino-3-(3-hydroxymethylisoxazole-4-yl)propionic acid] antagonist, is a CYP2E1 inducer. Drug Metab Dispos. 2003;31(11):1310-1314.

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Keywords

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