Automated Radiochemical Synthesis of [18F]3F4AP: A Novel PET Tracer for Imaging Demyelinating Diseases

被引:4
作者
Brugarolas, Pedro [1 ]
Bhuiyan, Mohammed [2 ]
Kucharski, Anna [2 ]
Freifelder, Richard [2 ]
机构
[1] Univ Chicago, Dept Neurol, Chicago, IL 60637 USA
[2] Univ Chicago, Dept Radiol, Chicago, IL 60637 USA
来源
JOVE-JOURNAL OF VISUALIZED EXPERIMENTS | 2017年 / 123期
关键词
Medicine; Issue; 123; Fluorine-18; radiochemistry; PET tracers; multiple sclerosis; automation; 4-AMINOPYRIDINE;
D O I
10.3791/55537
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
3-[F-18] fluoro-4-aminopyridine, [F-18]3F4AP, is a radiofluorinated analog of the FDA-approved drug for multiple sclerosis 4-aminopyridine (4AP). This compound is currently under investigation as a PET tracer for demyelination. We recently described a novel chemical reaction to produce metafluorinated pyridines consisting of direct fluorination of a pyridine N-oxide and the utilization of this reaction for the radiochemical synthesis of [F-18]3F4AP. In this article, we demonstrate how to produce this tracer using an automated synthesizer and an in-house made flow hydrogenation reactor. We also show the standard quality control procedures performed before releasing the radiotracer for preclinical animal imaging studies. This semi-automated procedure may serve as the basis for future production of [F-18]3F4AP for clinical studies.
引用
收藏
页数:9
相关论文
共 17 条
[1]   Molecular imaging with PET [J].
Ametamey, Simon M. ;
Honer, Michael ;
Schubiger, Pius August .
CHEMICAL REVIEWS, 2008, 108 (05) :1501-1516
[2]  
Brugarolas P., 2016, CHEM COMMUNICATIONS
[3]  
Brugarolas P., 2016, ABSTR PAP AM CHEM SO
[4]  
Brugarolas P, 2014, J NUCL MED, V55
[5]  
Brugarolas P, 2015, J NUCL MED, V56
[6]   ORALLY-ADMINISTERED 4-AMINOPYRIDINE IMPROVES CLINICAL SIGNS IN MULTIPLE-SCLEROSIS [J].
DAVIS, FA ;
STEFOSKI, D ;
RUSH, J .
ANNALS OF NEUROLOGY, 1990, 27 (02) :186-192
[7]   Sustained-release oral fampridine in multiple sclerosis: a randomised, double-blind, controlled trial [J].
Goodman, Andrew D. ;
Brown, Theodore R. ;
Krupp, Lauren B. ;
Schapiro, Randall T. ;
Schwid, Steven R. ;
Cohen, Ron ;
Marinucci, Lawrence N. ;
Blight, Andrew R. .
LANCET, 2009, 373 (9665) :732-738
[8]  
Heiss WD, 2006, J NUCL MED, V47, P302
[9]   EFFECTS OF 4-AMINOPYRIDINE IN PATIENTS WITH MULTIPLE-SCLEROSIS [J].
JONES, RE ;
HERON, JR ;
FOSTER, DH ;
SNELGAR, RS ;
MASON, RJ .
JOURNAL OF THE NEUROLOGICAL SCIENCES, 1983, 60 (03) :353-362
[10]   18F-Trifluoroborate Derivatives of [Des-Arg10]Kallidin for Imaging Bradykinin B1 Receptor Expression with Positron Emission Tomography [J].
Liu, Zhibo ;
Amouroux, Guillaume ;
Zhang, Zhengxing ;
Pan, Jinhe ;
Hundal-Jabal, Navjit ;
Colpo, Nadine ;
Lau, Joseph ;
Perrin, David M. ;
Benard, Francois ;
Lin, Kuo-Shyan .
MOLECULAR PHARMACEUTICS, 2015, 12 (03) :974-982