No abstract

A silicone resin with silphenylene units in Si-O-Si backbones was synthesized by hydrolysis-polycondensation of 1,4-bis(hydroxydimethylsilyl)benzene (BHB) with chlorosilanes. The structure and property of this novel silicone resin were characterized by gel permeation chromatography (GPC), Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), thermogarvimetric analysis (TG), scanning electron microscope (SEM), and electrochemical impedance spectrum (EIS). This silicone resin could be applied as the film forming material of coating when it is prepared under the condition of R/Si, Ph/R, and the content of silphenylene units being 1.3, 0.5, and 10 mol %, respectively. GPC, IR, and NMR results show that the silphenylene units have been incorporated into the polymer of silicone resin. The TG analysis indicates that this novel silicone resin has good heat resistance with the onset degradation temperature of 500.3 C and residual weight of 85.6% at 900 C. SEM results demonstrate that the silicone resin with silphenylene units can form full and uniform films, and its surface morphology of clear paints were not damaged by heat below 350C. EIS analysis reveals that clear paints of the silicone resin with silphenylene units have good resistance to corrosion.

A silicone resin with silphenylene units in Si—O—Si backbones was prepared through hydrolysis-polycondensation of self-synthesized 1,4-bis(diethoxymethylsilyl)benzene (BDSB) and other alkoxysilanes. The structure and properties of this novel silicone resin were characterized by gel permeation chromatography (GPC), Fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR), thermogravimetric analysis (TG), scanning electron microscope (SEM) and electrochemical impedance spectrum (EIS). The results of GPC, IR and NMR showed that silphenylene units had been successfully incorporated into the backbones of silicone resin. TG analyses reveal that silicone resin with silphenylene units in its backbones had a higher heat resistance than the usual methyl phenyl silicone resin. SEM results demonstrated that this silicone resin could form a full and uniform film, and its clear paints were able to stand temperatures below 350 °C. EIS analysis revealed that clear paints of this silicone resin have good resistance to corrosion.

The low affinity metabotropic glutamate receptor mGluR7 has been implicated in numerous CNS disorders; however, a paucity of potent and selective activators has hampered full delineation of the functional role and therapeutic potential of this receptor. In this work, we present the identification, optimization, and characterization of highly potent, novel mGluR7 agonists. Of particular interest is the chromane CVN636, a potent (EC50 7 nM) allosteric agonist which demonstrates exquisite selectivity for mGluR7 compared to not only other mGluRs, but also a broad range of targets. CVN636 demonstrated CNS penetrance and efficacy in an in vivo rodent model of alcohol use disorder. CVN636 thus has potential to progress as a drug candidate in CNS disorders involving mGluR7 and glutamatergic dysfunction.