Radiosynthesis of racemic and enantiomerically pure (-)-[18F]flubatine-A promising PET radiotracer for neuroimaging of ??4??2 nicotinic acetylcholine receptors

FischerS.; HillerA.; SmitsR.; HoeppingA.; FunkeU.; WenzelB.; CummingP.; SabriO.; SteinbachJ.; BrustP.

首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Radiosynthesis of racemic and enantiomerically pure (-)-[18F]flubatine-A promising PET radiotracer for neuroimaging of ??4??2 nicotinic acetylcholine receptors

【24h】

Radiosynthesis of racemic and enantiomerically pure (-)-[18F]flubatine-A promising PET radiotracer for neuroimaging of ??4??2 nicotinic acetylcholine receptors

机译：外消旋和对映体纯的（-）-[18F]氟丁汀-A的有前途的PET放射性示踪剂对?? 4 ?? 2烟碱乙酰胆碱受体的神经成像的放射合成

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

(-)-[18F]flubatine is a promising agent for visualization by PET of cerebral ??4??2 nicotinic acetylcholine receptors (nAChRs), which are implicated in psychiatric and neurodegenerative disorders. Here, we describe a substantially improved two-step radiosynthesis strategy for (-)-[18F]flubatine, based on the nucleophilic radiofluorination of an enantiomerically pure precursor followed by deprotection of the intermediate. An extensive leaving group/protecting group library of precursors was tested. Application of a trimethylammonium-iodide precursor with a Boc-protecting group provided the best results: labeling efficiencies of 80-95%, RCY of 60??5%, radiochemical purity of 98%, and a specific activity of 350GBq/??mol. The radiosynthesis is easily transferable to an automated synthesis module. ? 2013 Elsevier Ltd.

机译：（-）-[18F]氟巴汀是一种有前途的通过PET显像大脑?? 4 ?? 2烟碱乙酰胆碱受体（nAChRs）的药物，它与精神病和神经退行性疾病有关。在这里，我们基于对映体纯前体的亲核放射性氟化，然后对中间体进行脱保护，描述了（-）-[18F]氟丁汀的实质上改进的两步放射性合成策略。测试了广泛的前体离去基/保护基库。带有Boc保护基的三甲基碘化碘前体的应用提供了最佳结果：标记效率为80-95％，RCY为60-5％，放射化学纯度> 98％，比活度> 350GBq /?。摩尔。放射合成很容易转移到自动化合成模块。？ 2013爱思唯尔有限公司

著录项

来源
《Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine》 |2013年第null期|共9页
作者
FischerS.; HillerA.; SmitsR.; HoeppingA.; FunkeU.; WenzelB.; CummingP.; SabriO.; SteinbachJ.; BrustP.;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类原子核物理学、高能物理学;
关键词
??4??2 nAChR ligands; Fluorine-18; Leaving groups; Neuroimaging; Protecting groups; Radiosynthesis;

机译：?? 4 ?? 2 nAChR配体;Fluorine-18;离去基团;神经成像;保护基;放射合成;

相似文献

外文文献
中文文献
专利

1. Radiosynthesis of racemic and enantiomerically pure (-)-[18F]flubatine-A promising PET radiotracer for neuroimaging of ??4??2 nicotinic acetylcholine receptors [J] . FischerS., HillerA., SmitsR., Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine . 2013,第Null期

机译：外消旋和对映体纯的（-）-[18F]氟丁汀-A的有前途的PET放射性示踪剂对?? 4 ?? 2烟碱乙酰胆碱受体的神经成像的放射合成
2. Synthesis and biological evaluation of both enantiomers of [ 18F]flubatine, promising radiotracers with fast kinetics for the imaging of α4β2-nicotinic acetylcholine receptors [J] . SmitsR., FischerS., HillerA., Bioorganic and medicinal chemistry . 2014,第2期

机译：[18F]氟巴汀的两种对映异构体的合成和生物学评估，这是一种具有快速动力学的放射性示踪剂，可用于成像α4β2-烟碱乙酰胆碱受体
3. Radiosynthesis of 2-exo-(2'-[~18F]Fluoro-3'-(4-fluorophenyl)-pyridin-5'-yl)-7-azabicyclo[2.2.1]heptane([~18F]F_2PhEP), a potent epibatidine-based radioligand for nicotinic acetylcholine receptor PET imaging [J] . Gaelle Roger, Francoise Hinnen, Heric Valette, Journal of Labelled Compounds and Radiopharmaceuticals . 2006,第6期

机译：2-exo-（2'-[〜18F] Fluoro-3'-（4-氟苯基）-吡啶-5'-yl）-7-氮杂双环[2.2.1]庚烷（[〜18F] F_2PhEP）的放射合成，强效的基于依巴替丁的放射性配体用于烟碱乙酰胆碱受体PET成像
4. Regulation of Dopamine Release by Striatal Acetylcholine and Nicotine Is via Distinct Nicotinic Acetylcholine Receptors in Dorsal vs. Ventral Striatum [C] . Richard Exley, Michael A. Clements, Stephanie J. Cragg Triennial Meeting of the International Basal Ganglia Society . 2009

机译：通过纹状体乙酰胆碱和尼古丁对多巴胺释放的调节是通过不同的烟碱乙酰胆碱受体在背侧与腹侧纹状体中
5. Identification, pharmacology and anatomical localization of heteromeric neuronal nicotinic acetylcholine receptors in the rat hippocampus Effects of nicotine on nicotinic receptors expressed in rat primary cultured neurons . [D] . Lomazzo, Ermelinda. 2011

机译：大鼠海马异源神经元烟碱乙酰胆碱受体的鉴定，药理和解剖学定位烟碱对大鼠原代培养神经元表达的烟碱受体的影响。
6. Microfluidic radiosynthesis of 18FFEMPT a high affinity PET radiotracer for imaging serotonin receptors [O] . Thomas Lee Collier, Steven H Liang, J John Mann, 2017

机译：18F FEMPT的微流体放射合成一种高亲和力的PET示踪剂可对5-羟色胺受体成像
7. Automation of the radiosynthesis and purification procedures for [18F]Fluspidine preparation, a new radiotracer for clinical investigations in PET imaging of σ1 receptors in brain [O] . Maisonial-Besset, Aurélie, Funke, Uta, Wenzel, Barbara, 2014

机译：[18F]氟哌啶制剂放射合成和纯化程序的自动化，这是一种新型的放射性示踪剂，用于脑部σ1受体PET成像的临床研究
8. Use of Monoclonal Antibodies to Study the Structural Basis of the Function of Nicotinic Acetylcholine Receptors on Electric Organ and Muscle and to Determine the Structure of Nicotinic Acetylcholine Receptors on Neurons. [R] . Lindstrom, J. M. 1989

机译：使用单克隆抗体研究烟碱型乙酰胆碱受体在电活动器官和肌肉上的功能结构基础，并确定神经元上烟碱型乙酰胆碱受体的结构。

Radiosynthesis of racemic and enantiomerically pure (-)-[18F]flubatine-A promising PET radiotracer for neuroimaging of ??4??2 nicotinic acetylcholine receptors

摘要

著录项

相似文献

相关主题

期刊订阅