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Pearce, Larry V.,Ann, Jihyae,Jung, Aeran,Thorat, Shivaji A.,Herold, Brienna K. A.,Habtemichael, Amelework D.,Blumberg, Peter M.,Lee, Jeewoo American Chemical Society 2017 Journal of medicinal chemistry Vol.60 No.19
<P>Transient receptor potential vanilloid 1 (TRPV1) has emerged as a promising therapeutic target. While radiolabeled resiniferatoxin (RTX) has provided a powerful tool for characterization of vanilloid binding to TRPV1, TRPV1 shows 20-fold weaker binding to the human TRPV1 than to the rodent TRPV1. We now describe a tritium radiolabeled synthetic vanilloid antagonist, 1-((2-(4-(methyl-[<SUP>3</SUP>H])piperidin-1-yl-4-[<SUP>3</SUP>H])-6-(trifluoromethyl)pyridin-3-yl)methyl)-3-(3-oxo-3,4-dihydro-2<I>H</I>-benzo[<I>b</I>][1,4]oxazin-8-yl)urea ([<SUP>3</SUP>H]MPOU), that embodies improved absolute affinity for human TRPV1 and improved synthetic accessibility.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2017/jmcmar.2017.60.issue-19/acs.jmedchem.7b00859/production/images/medium/jm-2017-008593_0010.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm7b00859'>ACS Electronic Supporting Info</A></P>