6-2-Dihydroxyflavone - GABA Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE6,2-DihydroxyflavoneCat. No.: HY-N6628CAS No.: 92439-20-8分式: CHO分量: 254.24作靶点: GABA Receptor作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验

2、 DMSO : 155 mg/mL (609.66 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9333 mL 19.6665 mL 39.3329 mL5 mM 0.7867 mL 3.9333 mL 7.8666 mL10 mM 0.3933 mL 1.9666 mL 3.9333 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 6,2-Dihydroxyflavone个新型的

3、 GABAA 受体拮抗剂。IC50 & Target GABAA receptor 1体外研究6,2-Dihydroxyflavone is a novel antagonist of GABAA receptor. 6,2-Dihydroxyflavone inhibits 3H-flunitrazepam binding to the rat cerebral cortex membranes with a Ki of 37.24.5 nM. The current elicited withthe EC50 concentration of GABA is decreased to 73

4、.61.9% of control by co-application of 5 M 6,2-1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEDihydroxyflavone (n=5), compare to a decrease to 65.93.0% by 1 M FG-7142 (n=5). The EC50 for GABAdose response increases from 47.6 to 59.7 M upon co-application of 5 M 6,2-Dihydroxyflavone, and themaximal

5、 GABA-current is decreased 1.体内研究 6,2-Dihydroxyflavone-treated mice exhibit significant differences from control mice with respect to thepercentage of open arms entries F(4,73)=8.01, P (4,73)=5.19, P(4,73)= 0.79,P=0.54. The post-hocNewmaneKeuls tests confirm that 6,2-Dihydroxyflavone significantly d

6、ecreases the percentage of open armentries and time spent in open arms at the doses of 8 and 16 mg/kg. 6,2-Dihydroxyflavone treatmentsimilarly increases step-through latency F(4,75)=4.71, P 1.PROTOCOLCell Assay 1 Membranes from HEK 293T cell are used in this study. Briefly, aliquots of membranes are

7、 incubated with 1nM 3H-flunitrazepam or 8 nM 3H-Ro15-4513 at 4C for 90 min in the presence or absence of 6,2-Dihydroxyflavone. After incubation, the mixtures are filtered onto Whatman GF/B filters with a Brandel 24-wellharvester. Each filter is incubated for at least 1 h with 4 mL scintillation cock

8、tail before measurement ofradioactivity in a Beckman-Coulter LS 6500 scintillation counter. For saturation analysis, the membranes areincubated with increasing concentrations of 3H-flunitrazepam or 3H-Ro15-4513. Binding affinity isdetermined by nonlinear regression analysis 1.MCE has not independent

9、ly confirmed the accuracy of these methods. They are for reference only.Animal Male ICR mice are randomized into six groups (n=12 to 16/group), and receive 0.4 mg/kg scopolamine (i.p.)Administration 1 45 min prior to training, followed with vehicle (dd water, pH 9.0, p.o.), 2, 4, 8 or 16 mg/kg 6,2-D

10、ihydroxyflavone (p.o.), or 30 mg/kg FG-7142 (i.p.) 30 min prior to training. On the training trials, eachmouse is placed into the lighted chamber of a two-compartment box, and the door leading to the darkchamber is opened 10 s later. Once the mouse enters the dark compartment, the door is closed and

11、 aninescapable electric foot-shock (0.4 mA, 1 s) is delivered from the grid floor. The mouse is removed from theapparatus 10 s later. The step-through latency is recorded, with the cut-off step-through latency set at 300 s1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wang F, et al. 6,2-Dihydroxyflavone, a subtype-selective partial inverse agonist of GABAA receptor benzodiazepine site.Neuropharmacology. 2007 Sep;53(4):574-82.McePdfHeightCaution: Produc