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Lee, Hyosung,Park, Ki Duk,Torregrosa, Robert,Yang, Xiao-Fang,Dustrude, Erik T.,Wang, Yuying,Wilson, Sarah M.,Barbosa, Cindy,Xiao, Yucheng,Cummins, Theodore R.,Khanna, Rajesh,Kohn, Harold American Chemical Society 2014 Journal of medicinal chemistry Vol.57 No.14
<P/><P>We prepared 13 derivatives of <I>N</I>-(biphenyl-4′-yl)methyl (<I>R</I>)-2-acetamido-3-methoxypropionamide that differed in type and placement of a R-substituent in the terminal aryl unit. We demonstrated that the R-substituent impacted the compound’s whole animal and cellular pharmacological activities. In rodents, select compounds exhibited excellent anticonvulsant activities and protective indices (PI = TD<SUB>50</SUB>/ED<SUB>50</SUB>) that compared favorably with clinical antiseizure drugs. Compounds with a polar, aprotic R-substituent potently promoted Na<SUP>+</SUP> channel slow inactivation and displayed frequency (use) inhibition of Na<SUP>+</SUP> currents at low micromolar concentrations. The possible advantage of affecting these two pathways to decrease neurological hyperexcitability is discussed.</P>