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品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear (warmed)
儲存溫度
−20°C
SMILES 字串
FC1=CC=CC(C#CC2=NC=C(C=C2)C(NC3CCC3)=O)=C1.Cl
InChI
1S/C18H15FN2O.ClH/c19-15-4-1-3-13(11-15)7-9-16-10-8-14(12-20-16)18(22)21-17-5-2-6-17;/h1,3-4,8,10-12,17H,2,5-6H2,(H,21,22);1H
InChI 密鑰
NBGAPTWZQXSEAA-UHFFFAOYSA-N
一般說明
VU0360172 is a potent (EC50 = 16.6 nM), systemically active positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5). It is the first orally active mGlu5 PAM to be efficacious in an in vivo preclinical antipsychotic model, producing a dose-dependent reversal of amphetamine-induced hyperlocomotion. It was also found to reduce spontaneous absence seizures in WAG/Rij rats and to inhibit pain. Reduced spontaneous spike and wave discharges without impacting motor behavior in a rat model of absence epilepsy have been observed.
生化／生理作用
VU0360172 is a potent (EC50 = 16.6 nM), systemically active positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5). It is the first orally active mGlu5 PAM to be efficacious in an in vivo preclinical antipsychotic model, producing a dose-dependent reversal of amphetamine-induced hyperlocomotion. It was also found to reduce absence seizures in WAG/Rij rats and to inhibit pain.
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
Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats
V. D'Amore, et al.
Neuropharmacology, 330-338 (2013)
Alice L Rodriguez et al.
Molecular pharmacology, 78(6), 1105-1123 (2010-10-07)
Modulators of metabotropic glutamate receptor subtype 5 (mGluR5) may provide novel treatments for multiple central nervous system (CNS) disorders, including anxiety and schizophrenia. Although compounds have been developed to better understand the physiological roles of mGluR5 and potential usefulness for
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