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About This Item
经验公式（希尔记法）:
C12H11N3O
CAS号:
分子量:
213.24
MDL號碼:
分類程式碼代碼:
12352202
PubChem物質ID:
NACRES:
NA.77
推荐产品
化驗
≥99% (HPLC)
形狀
crystalline
顏色
red
SMILES 字串
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 密鑰
LOCPVWIREQIGNQ-CCEZHUSRSA-N
基因資訊
human ... GRM1(2911) , GRM5(2915)
應用
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
特點和優勢
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.
訊號詞
Warning
危險聲明
危險分類
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
標靶器官
Respiratory system
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
V Bruno et al.
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.
Giuseppe Battaglia et al.
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
M A Varney et al.
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
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