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Aryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate

  作者 KEITH JOHN M; APODACA RICH; TICHENOR MARK; XIAO WEI; JONES WILLIAM; PIERCE JOAN; SEIERSTAD MARK; PALMER JAMES; WEBB MICHAEL; KARBARZ MARK; SCOTT BRIAN; WILSON SANDY; LUO LIN; WENNERHOLM MICHELLE; CHANG LEON; BROWN SEAN; RIZZOLIO MICHELE; RYNBERG RAYMOND; CHAPLAN SANDRA; BREITENBUCHER J GUY  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2012年3-10;  页码  823-827  
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[摘要]A series of aryl piperazinyl ureas that act as covalent inhibitors of fatty acid amide hydrolase (FAAH) is described. A potent and selective (does not inhibit FAAH-2) member of this class, JNJ-40355003, was found to elevate the plasma levels of three fatty acid amides: anandamide, oleoyl ethanolamide, and palmitoyl ethanolamide, in the rat, dog, and cynomolgous monkey. The elevation of the levels of these lipids in the plasma of monkeys suggests that FAAH-2 may not play a significant role in regulating plasma levels of fatty acid ethanolamides in primates.

 
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