New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein

…, A Brunet, FI McGonagle, D Dewar, SL Pimlott…

文献索引：Stevenson, Louise; Tavares, Adriana A.S.; Brunet, Aurelie; McGonagle, Fiona I.; Dewar, Deborah; Pimlott, Sally L.; Sutherland, Andrew Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 954 - 957

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被引用次数: 16

摘要

With the aim of developing new SPECT imaging agents for the translocator protein (TSPO), a small library of iodinated quinoline-2-carboxamides have been prepared and tested for binding affinity with TSPO. N, N-Diethyl-3-iodomethyl-4-phenylquinoline-2-carboxamide was found to have excellent affinity (Ki 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195.