GYKI 47261 dihydrochloride

Modify Date: 2024-01-10 18:04:28

GYKI 47261 dihydrochloride Structure
GYKI 47261 dihydrochloride structure
Common Name GYKI 47261 dihydrochloride
CAS Number 1217049-32-5 Molecular Weight 395.713
Density N/A Boiling Point N/A
Molecular Formula C18H17Cl3N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

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

 GYKI 47261 dihydrochloride Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C18H17Cl3N4
Molecular Weight 395.713
Exact Mass 394.051880

 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)