新型碘代喹啉-2-甲酰胺类化合物用于转位蛋白 SPECT 成像。
New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein.
机构信息
WestCHEM, Department of Chemistry, The Joseph Black Building, University of Glasgow, Glasgow G12 8QQ, UK.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):954-7. doi: 10.1016/j.bmcl.2009.12.061. Epub 2009 Dec 22.
PMID:20045646
Abstract
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 (K(i) 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195.
摘要
为了开发新型的 TSPO（转位蛋白）单光子发射计算机断层成像（SPECT）造影剂，我们合成了一系列碘代喹啉-2-甲酰胺，并测试了它们与 TSPO 的结合亲和力。结果发现 N,N-二乙基-3-碘甲基-4-苯基喹啉-2-甲酰胺具有极好的亲和力（K(i) 12.0 nM），与广泛使用的 TSPO 成像剂 PK11195 相当。
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