6-氯-3-(((1-[11C]甲基)-2-(S)-吡咯烷基)甲氧基)-5-(2-氟吡啶-4-基)吡啶([11C]JHU85270)，一种用于正电子发射断层扫描进行烟碱型乙酰胆碱受体成像的强效配体。
6-Chloro-3-(((1-[11C]methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine ([11C]JHU85270), a potent ligand for nicotinic acetylcholine receptor imaging by positron emission tomography.
作者信息
Gao Yongjun, Ravert Hayden T, Holt Daniel, Dannals Robert F, Horti Andrew G
机构信息
Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University, School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287-0816, USA.
出版信息
Appl Radiat Isot. 2007 Aug;65(8):947-51. doi: 10.1016/j.apradiso.2007.04.013. Epub 2007 May 6.
6-Chloro-3-((1-methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine (JHU85270), a novel high-affinity ligand for the alpha4beta2 nicotine acetylcholine receptor (nAChR) (K(i)=86, 115 pM; K(i)(JHU85270)/K(i)(epibatidine)=1.7) with a log D(7.4)=1.6 was synthesized in 56% overall yield. [(11)C]JHU85270 was synthesized from [(11)C]-methyl iodide and the corresponding normethyl precursor. The average time of radiosynthesis, purification, and formulation was 37 min from the end of bombardment. The average radiochemical yield of [(11)C]JHU85270 was 37%+/-3% (non-decay corrected). The average specific radioactivity was 398+/-165 GBq/micromol (10750+/-4468 mCi/micromol) and the radiochemical purity was greater than 99%.
6-氯-3-((1-甲基)-2-(S)-吡咯烷基)甲氧基)-5-(2-氟吡啶-4-基)吡啶(JHU85270)是一种新型的α4β2烟碱型乙酰胆碱受体(nAChR)高亲和力配体(K(i)=86、115 pM；K(i)(JHU85270)/K(i)(依博加碱)=1.7)，log D(7.4)=1.6，其总产率为56%。[(11)C]JHU85270由[(11)C]-碘甲烷和相应的去甲基前体合成。从轰击结束起，放射性合成、纯化和制剂的平均时间为37分钟。[(11)C]JHU85270的平均放射化学产率为37%±3%(未校正衰变)。平均比活度为398±165 GBq/μmol(10750±4468 mCi/μmol)，放射化学纯度大于99%。
Zotero 插件