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

被引：4

作者：

Gao, Yonjun ^{[1
]}

Ravert, Hayden T. ^{[1
]}

Holt, Daniel ^{[1
]}

Dannals, Robert F. ^{[1
]}

Horti, Andrew G. ^{[1
]}

机构：

[1] Johns Hopkins Univ, Sch Med, Dept Radiol, Div Nucl Med, Baltimore, MD 21287 USA

来源：

APPLIED RADIATION AND ISOTOPES | 2007年 / 65卷 / 08期

关键词：

nicotinic acetylcholine receptors; PET; carbon-11; stille coupling;

D O I：

10.1016/j.apradiso.2007.04.013

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

6-Chloro-3-((1-methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine (JHU85270), a novel high-affinity ligand for the alpha 4 beta 2 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. [C-11]JHU85270 was synthesized from [C-11]-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 [C-11]JHU85270 was 37%+/-3% (non-decay corrected). The average specific radioactivity was 398+/-165 GBq/mu mol (10750+/-4468 mCi/mu mol) and the radiochemical purity was greater than 99%. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：947 / 951

页数：5

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