GYKI 47261 dihydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

220445-20-5

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	Yellow solid
Storage	Store at -20°C
M.Wt	395.71
Cas No.	220445-20-5
Formula	C₁₈H₁₅ClN₄·2HCl
Solubility	<35.92mg/ml in DMSO
Chemical Name	4-(8-chloro-2-methyl-11H-benzo[e]imidazo[1,2-b][1,2]diazepin-6-yl)aniline dihydrochloride
Canonical SMILES	CC1=CN2C(CC3=C(C(C4=CC=C(N)C=C4)=N2)C=C(Cl)C=C3)=N1.Cl.Cl
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

GYKI 47261 dihydrochloride is a selective and non-competitive antagonist of AMPA receptor with IC50 value of 2.5 μM [1].

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) is an ionotropic transmembrane receptor for glutamate and mediates fast synaptic transmission in the central nervous system. AMPA receptors are oligomeric assemblies of four protein subunits, GluR1-4.

GYKI 47261 dihydrochloride is a selective and non-competitive AMPA receptor antagonist. In isolated cerebellar Purkinje cells, GYKI 47261 (10 μM) inhibited currents induced by kainate or AMPA in a non-competitive way [1]. In rat hepatocytes, GYKI-47261 (10 μM) significantly increased CYP2E1 activity. In human hepatocytes, GYKI-47261 produced the maximal induction at 0.01 μM [2].

In mice, GYKI 47261 induced muscle relaxant effects with ED50 values of 15.8-36.5 mg/kg. In a transient focal ischemia rat model, GYKI 47261 significantly reduced infarct size by 62.3-67.4%. In mice, GYKI 47261 effectively reduced oxotremorine-induced tremor and inhibited MPTP-induced neurotoxicity [1]. In Parkinson’s disease rat model, administration of GYKI-47261 and MK-801 completely normalized the response shortening induced by levodopa. In monkeys, administration of amantadine and GYKI-47261 significantly reduced dyskinesias induced by levodopa by 51% [3].

References:
[1]. Abrahám G, Sólyom S, Csuzdi E, et al. New non competitive AMPA antagonists. Bioorg Med Chem, 2000, 8(8): 2127-2143.
[2]. Tamási V, Hazai E, Porsmyr-Palmertz M, 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.
[3]. Bibbiani F, Oh JD, Kielaite A, et al. Combined blockade of AMPA and NMDA glutamate receptors reduces levodopa-induced motor complications in animal models of PD. Exp Neurol, 2005, 196(2): 422-429.