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方案
≥98% (HPLC)
质量水平
表单
solid
颜色
yellow
溶解性
DMSO: 0.39 mg/mL
ethanol: 0.4 mg/mL
0.1 M HCl: 0.68 mg/mL
methanol: 1 mg/mL
H2O: >10 mg/mL
SMILES字符串
Cl[H].CC1=NN=C(c2ccc(N)cc2)c3cc4OCOc4cc3C1
InChI
1S/C17H15N3O2.ClH/c1-10-6-12-7-15-16(22-9-21-15)8-14(12)17(20-19-10)11-2-4-13(18)5-3-11;/h2-5,7-8H,6,9,18H2,1H3;1H
InChI key
RUBSCPARMVJNKX-UHFFFAOYSA-N
基因信息
human ... GRIA1(2890) , GRIA2(2891) , GRIA3(2892) , GRIA4(2893)
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应用
GYKI 52466 hydrochloride has been used as an α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor selective antagonist in cell viability assays to evaluate the specificity of kainate (KA) effect on cerebellar granule cells (CGCs).[1] It has also been used as an AMPA blocker to study the function of glutamate in neuroadapted sindbis virus (NSV) -induced motor neuron death.[2]
生化/生理作用
GYKI 52466 serves as an antagonist of several processes, mediated by glutamate.[3]
Selective allosteric AMPA receptor antagonist; anticonvulsant; skeletal muscle relaxant.
特点和优势
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Glutamate Receptors (Ion Channel Family) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
法律信息
Sold under exclusive license from the Institute for Drug Research Ltd., Budapest, Hungary.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
53rd National Meeting of the Italian Society of Biochemistry and Molecular Biology (SIB) and National Meeting of Chemistry of Biological Systems ? Italian Chemical Society (SCI - Section CSB) null
T J Wilding et al.
Molecular pharmacology, 47(3), 582-587 (1995-03-01)
Whole-cell recordings were used to study the antagonism of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-preferring and kainate-preferring receptors by 2,3-benzodiazepines. Current through kainate-preferring receptors was recorded in rat dorsal root ganglion (DRG) neuron-s, whereas AMPA receptor current was measured in cultured neurons from
2013 IEEE International Conference on Solid Dielectrics (ICSD) IEEE null
S D Donevan et al.
Neuron, 10(1), 51-59 (1993-01-01)
In whole-cell voltage-clamp recordings from cultured rat hippocampal neurons, the 2,3-benzodiazepine GYKI 52466 was a potent antagonist of kainate- and AMPA-activated currents (IC50 values, 7.5 and 11 microM, respectively), but was inactive against N-methyl-D-aspartate (NMDA) or gamma-aminobutyric acid responses. The
29th Colloquium, Protides of Biological Fluids null
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