G119
GYKI 52466 hydrochloride
≥98% (HPLC), α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist, solid
别名:
1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride
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关于此项目
经验公式（希尔记法）:
C17H15N3O2 · HCl
化学文摘社编号:
分子量:
329.78
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
GYKI 52466 hydrochloride, solid
方案
≥98% (HPLC)
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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相关类别
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). It has also been used as an AMPA blocker to study the function of glutamate in neuroadapted sindbis virus (NSV) -induced motor neuron death.
生化/生理作用
GYKI 52466 serves as an antagonist of several processes, mediated by glutamate.
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
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
29th Colloquium, Protides of Biological Fluids 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
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
S D Donevan et al.
Neuroscience, 87(3), 615-629 (1998-10-03)
Allosteric regulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate (AMPA) receptors include 2,3-benzodiazepines such as GYKI 52466 and GYKI 53655 and the chaotropic anion thiocyanate that inhibit, and benzothiadiazines such as cyclothiazide that potentiate AMPA receptor currents. Here we sought to determine whether the allosteric
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
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