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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
FPTQ is potent mGluR 1 antagonist with IC 50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo .
In Vitro
FPTQ (0.5-10 μM) does not shows any cytotoxicity was not observed at 0.5, 1, 5, and 10 μM in RAW264.7 macrophage cells. FPTQ (1-20 μM; 24 hours) reduces LPS-induced NO production at > 1 μM FPTQ, and at 10 μM, FPTQ treatment causes a 31% anti-oxidant effect in RAW264.7 macrophage cells. FPTQ (1-20 μM; 24 hours) dramaticly decreases LPS-induced expression levels of IL-1β and Il-6. At a concentration of 10 μM, FPTQ causes a 27% and 44% reduction in the mRNA expression of IL-1β and Il-6, respectively in RAW264.7 macrophage cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: RAW264.7 macrophage cells Concentration: 1, 10, or 20 μM Incubation Time: 24 hours Result: Decreased IL-1β and IL-6 mRNA expression
In Vivo
FPTQ (5-20 μM) decreases the number of neutrophils migrating to the amputation site in zebrafish larvae by tail amputation. In the tailfin wound method, the number of neutrophils collecting at the wound site also decreases in a dose-dependent manner in zebrafish. In a LPS-induced inflammation zebrafish model, LPS solution is injected into the yolks of Tg(mpx:EGFP) i114 zebrafish larvae and exposed the zebrafish larvae immediately to FPTQ treatment. FPTQ (20 μM; 4 hours) significantly decreases the fluorescent neutrophils after yolk injection and has an anti-inflammatory effect during the early phase of inflammation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Human mGluR1 6 nM (IC 50 ) Mouse mGluR1 1.4 nM (IC 50 )