GYKI-47261 dihydrochloride_product_DataBase

Bioactivity	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].
In Vivo	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:
Name	GYKI-47261 dihydrochloride
CAS	1217049-32-5
Formula	C18H17Cl3N4
Molar Mass	395.71
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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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