1217049-32-5

1217049-32-5 structure

Name: GYKI 47261 dihydrochloride
Chemical Name: 4-(8-Chloro-2-methyl-11H-imidazo[1,2-c][2,3]benzodiazepin-6-yl)aniline dihydrochloride
CAS Number: 1217049-32-5
Molecular Formula: C₁₈H₁₇Cl₃N₄
Molecular Weight: 395.713
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2018-07-20 10:28:47
Modify Date: 2024-01-10 18:04:28
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].

Name	4-(8-Chloro-2-methyl-11H-imidazo[1,2-c][2,3]benzodiazepin-6-yl)aniline dihydrochloride
Synonyms	4-(8-Chloro-2-methyl-11H-imidazo[1,2-c][2,3]benzodiazepin-6-yl)aniline dihydrochloride Benzenamine, 4-(8-chloro-2-methyl-11H-imidazo[1,2-c][2,3]benzodiazepin-6-yl)-, hydrochloride (1:2)

Description	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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> iGluR Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
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: 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.
References	[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.