Literature DB >> 33479620

Syntheses of [11C]2- and [11C]3-trifluoromethyl-4-aminopyridine: potential PET radioligands for demyelinating diseases.

Karla M Ramos-Torres1, Yu-Peng Zhou1, Bo Yeun Yang2, Nicolas J Guehl1, Moon Sung-Hyun1, Sanjay Telu2, Marc D Normandin1, Victor W Pike2, Pedro Brugarolas1.   

Abstract

Trifluoromethyl groups are of great interest in PET radiopharmaceuticals. Radiolabelled 4-aminopyridine (4AP) derivatives have been proposed for imaging demyelinating diseases. Here, we describe methods for producing 11C-trifluoromethylated derivatives of 4AP and present early imaging results with [11C]3-trifluoromethyl-4AP in a rhesus macaque. This study shows the utility of [11C]CuCF3 for labelling pyridines and provides initial evidence for the potential use of [11C]3-trifluoromethyl-4AP as a PET radioligand. This journal is © The Royal Society of Chemistry 2020.

Entities:  

Year:  2020        PMID： 33479620      PMCID： PMC7651860          DOI： 10.1039/d0md00190b

Source DB:  PubMed          Journal:  RSC Med Chem        ISSN： 2632-8682


  19 in total

1.  A universal procedure for the [¹⁸F]trifluoromethylation of aryl iodides and aryl boronic acids with highly improved specific activity.

Authors:  Dion van der Born; Claudia Sewing; J Koos D M Herscheid; Albert D Windhorst; Romano V A Orru; Danielle J Vugts
Journal:  Angew Chem Int Ed Engl       Date:  2014-08-26       Impact factor: 15.336

Review 2.  Consensus nomenclature rules for radiopharmaceutical chemistry - Setting the record straight.

Authors:  Heinz H Coenen; Antony D Gee; Michael Adam; Gunnar Antoni; Cathy S Cutler; Yasuhisa Fujibayashi; Jae Min Jeong; Robert H Mach; Thomas L Mindt; Victor W Pike; Albert D Windhorst
Journal:  Nucl Med Biol       Date:  2017-10-02       Impact factor: 2.408

3.  [11 C]Fluoroform, a Breakthrough for Versatile Labeling of PET Radiotracer Trifluoromethyl Groups in High Molar Activity.

Authors:  Mohammad B Haskali; Victor W Pike
Journal:  Chemistry       Date:  2017-05-17       Impact factor: 5.236

4.  Trifluoromethylation of aryl and heteroaryl halides with fluoroform-derived CuCF3: scope, limitations, and mechanistic features.

Authors:  Anton Lishchynskyi; Maxim A Novikov; Eddy Martin; Eduardo C Escudero-Adán; Petr Novák; Vladimir V Grushin
Journal:  J Org Chem       Date:  2013-08-21       Impact factor: 4.354

Review 5.  Fluorine in medicinal chemistry.

Authors:  Sophie Purser; Peter R Moore; Steve Swallow; Véronique Gouverneur
Journal:  Chem Soc Rev       Date:  2007-12-13       Impact factor: 54.564

Review 6.  FSL.

Authors:  Mark Jenkinson; Christian F Beckmann; Timothy E J Behrens; Mark W Woolrich; Stephen M Smith
Journal:  Neuroimage       Date:  2011-09-16       Impact factor: 6.556

7.  Development of a PET radioligand for potassium channels to image CNS demyelination.

Authors:  Pedro Brugarolas; Jorge E Sánchez-Rodríguez; Hsiu-Ming Tsai; Falguni Basuli; Shih-Hsun Cheng; Xiang Zhang; Andrew V Caprariello; Jerome J Lacroix; Richard Freifelder; Dhanabalan Murali; Onofre DeJesus; Robert H Miller; Rolf E Swenson; Chin-Tu Chen; Peter Herscovitch; Daniel S Reich; Francisco Bezanilla; Brian Popko
Journal:  Sci Rep       Date:  2018-01-12       Impact factor: 4.379

8.  A Gas Phase Route to [18F]fluoroform with Limited Molar Activity Dilution.

Authors:  Bo Yeun Yang; Sanjay Telu; Mohammad B Haskali; Cheryl L Morse; Victor W Pike
Journal:  Sci Rep       Date:  2019-10-16       Impact factor: 4.379

9.  Structure-activity relationship studies of four novel 4-aminopyridine K+ channel blockers.

Authors:  Sofia Rodríguez-Rangel; Alyssa D Bravin; Karla M Ramos-Torres; Pedro Brugarolas; Jorge E Sánchez-Rodríguez
Journal:  Sci Rep       Date:  2020-01-09       Impact factor: 4.379

10.  Evaluation of the potassium channel tracer [18F]3F4AP in rhesus macaques.

Authors:  Nicolas J Guehl; Karla M Ramos-Torres; Clas Linnman; Sung-Hyun Moon; Maeva Dhaynaut; Moses Q Wilks; Paul K Han; Chao Ma; Ramesh Neelamegam; Yu-Peng Zhou; Brian Popko; John A Correia; Daniel S Reich; Georges El Fakhri; Peter Herscovitch; Marc D Normandin; Pedro Brugarolas
Journal:  J Cereb Blood Flow Metab       Date:  2020-10-22       Impact factor: 6.200
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  1 in total

1.  Synthesis and Screening in Mice of Fluorine-Containing PET Radioligands for TSPO: Discovery of a Promising 18F-Labeled Ligand.

Authors:  Fabrice G Siméon; Jae-Hoon Lee; Cheryl L Morse; Ian Stukes; Sami S Zoghbi; Lester S Manly; Jeih-San Liow; Robert L Gladding; Rachel M Dick; Xuefeng Yan; Sabrina Taliani; Barbara Costa; Claudia Martini; Federico Da Settimo; Sabrina Castellano; Robert B Innis; Victor W Pike
Journal:  J Med Chem       Date:  2021-11-10       Impact factor: 7.446
  1 in total

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