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
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
GYKI 52466 hydrochloride, solid
SMILES string
Cl[H].CC1=NN=C(c2ccc(N)cc2)c3cc4OCOc4cc3C1
InChI key
RUBSCPARMVJNKX-UHFFFAOYSA-N
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
assay
≥98% (HPLC)
form
solid
color
yellow
solubility
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
Quality Level
Gene Information
human ... GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
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Application
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.
Biochem/physiol Actions
GYKI 52466 serves as an antagonist of several processes, mediated by glutamate.
Selective allosteric AMPA receptor antagonist; anticonvulsant; skeletal muscle relaxant.
Features and Benefits
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.
Legal Information
Sold under exclusive license from the Institute for Drug Research Ltd., Budapest, Hungary.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
法规信息
新产品
此项目有
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
29th Colloquium, Protides of Biological Fluids null
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
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