质量水平
检测方案
≥99% (HPLC)
形式
crystalline
颜色
red
SMILES字符串
Cc1ccc(O)c(\N=N\c2ccccc2)n1
InChI
1S/C12H11N3O/c1-9-7-8-11(16)12(13-9)15-14-10-5-3-2-4-6-10/h2-8,16H,1H3/b15-14+
InChI key
LOCPVWIREQIGNQ-CCEZHUSRSA-N
基因信息
human ... GRM1(2911) , GRM5(2915)
应用
SIB 1757 may be used in mGluR5 metabotropic glutamate receptor-mediated cell signaling studies.
生化/生理作用
SIB 1757 is a highly selective mGluR5 metabotropic glutamate receptor antagonist. It non-competitively inhibits glutamate-induced increase in Ca2+ at human metabotropic glutamate receptor 1 (hmGluR1).1 Inhibition of mGlu5 receptor renders protection to neurons2 against methamphetamine-induced oxidative damage.3
特点和优势
This compound is featured on the Glutamate Receptors (G Protein Family) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
警示用语:
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
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
Neuropharmacology, 39(12), 2223-2230 (2000-09-07)
We have used potent and selective non-competitive antagonists of metabotropic glutamate receptor subtype 5 (mGlu5) -- 2-methyl-6-phenylethynylpyridine (MPEP), [6-methyl-2-(phenylazo)-3-pyridinol] (SIB-1757) and [(E)-2-methyl-6-(2-phenylethenyl)pyridine] (SIB-1893) - to examine whether endogenous activation of this particular metabotropic glutamate receptor subtype contributes to neuronal degeneration.
The Journal of pharmacology and experimental therapeutics, 290(1), 170-181 (1999-06-25)
Cell lines expressing the human metabotropic glutamate receptor subtype 5a (hmGluR5a) and hmGluR1b were used as targets in an automated high-throughput screening (HTS) system that measures changes in intracellular Ca2+ ([Ca2+]i) using fluorescence detection. This functional screen was used to
The Journal of neuroscience : the official journal of the Society for Neuroscience, 22(6), 2135-2141 (2002-03-16)
Methamphetamine (MA), a widely used drug of abuse, produces oxidative damage of nigrostriatal dopaminergic terminals. We examined the effect of subtype-selective ligands of metabotropic glutamate (mGlu) receptors on MA neurotoxicity in mice. MA (5 mg/kg, i.p.; injected three times, every
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