GYKI 47261 dihydrochloride

GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1[1][2].

Signaling Pathways >> Neuronal Signaling >> iGluR

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

GYKI-47261 dihydrochloride (6 mg/kg; i.v.) shows antiischemice effect in a transient focal ischemia model, in rats. GYKI-47261 dihydrochloride (p.o.) potently mitigated the tremor induced by oxotremorine with ED50 of 16.8 mg/kg in male CD1 mice[1]. GYKI-47261 dihydrochloride(20 mg/kg; i.p.) reverses the dopamine depleting effect of MPTP[1]. Animal Model: Male C57 black mice, weighing 23-30 g[1] Dosage: 20 mg/kg Administration: I.p. Result: Reversed the MPTP-induced decrease in striatal concentrations.

[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.