Literature DB >> 34607293

Alternative strategies for the synthesis of [11C]ER176 for PET imaging of neuroinflammation.

Jason C Mixdorf1, Dhanabalan Murali2, Yangchun Xin2, Alexandra H DiFilippo3, Eduardo Aluicio-Sarduy4, Todd E Barnhart4, Jonathan W Engle5, Paul A Ellison4, Bradley T Christian3.   

Abstract

[11C]ER176 is a next generation PET radioligand for imaging 18 kDa translocator protein, a biomarker for neuroinflammation. The goal of this work was to investigate alternative strategies for the radiochemical synthesis, purification, and formulation of [11C]ER176. An optimized tri-solvent high-performance liquid chromatography (HPLC) protocol is described to separate the hydro-de-chlorinated byproduct from [11C]ER176. A newly implemented solid phase extraction work-up efficiently removed HPLC solvent while maintaining chemical purity and overall radiochemical yield and purity. This new HPLC purification and final formulation was completed within 40 min, providing 2.7 ± 0.5 GBq of [11C]ER176 at end of synthesis with 1400 ± 300 GBq/μmol molar activity while meeting all specifications for radiopharmaceutical quality control tests for human research use.
Copyright © 2021. Published by Elsevier Ltd.

Entities:  

Keywords:  11-Carbon; ER176; Neuroinflammation; PET; Radiochemistry; TSPO

Mesh：

Substances：

Year:  2021        PMID： 34607293      PMCID： PMC9191690          DOI： 10.1016/j.apradiso.2021.109954

Source DB:  PubMed          Journal:  Appl Radiat Isot        ISSN： 0969-8043            Impact factor:   1.787


  10 in total

1.  Head-to-head comparison of 11C-PBR28 and 11C-ER176 for quantification of the translocator protein in the human brain.

Authors:  Paolo Zanotti-Fregonara; Belen Pascual; Mattia Veronese; Meixiang Yu; David Beers; Stanley H Appel; Joseph C Masdeu
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-05-31       Impact factor: 9.236

2.  11C-ER176, a Radioligand for 18-kDa Translocator Protein, Has Adequate Sensitivity to Robustly Image All Three Affinity Genotypes in Human Brain.

Authors:  Masamichi Ikawa; Talakad G Lohith; Stal Shrestha; Sanjay Telu; Sami S Zoghbi; Sabrina Castellano; Sabrina Taliani; Federico Da Settimo; Masahiro Fujita; Victor W Pike; Robert B Innis
Journal:  J Nucl Med       Date:  2016-11-17       Impact factor: 10.057

3.  Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.

Authors:  Sabrina Castellano; Sabrina Taliani; Ciro Milite; Isabella Pugliesi; Eleonora Da Pozzo; Elisa Rizzetto; Sara Bendinelli; Barbara Costa; Sandro Cosconati; Giovanni Greco; Ettore Novellino; Gianluca Sbardella; Giorgio Stefancich; Claudia Martini; Federico Da Settimo
Journal:  J Med Chem       Date:  2012-04-25       Impact factor: 7.446

4.  Production of [11C]CH3I by single pass reaction of [11C]CH4 with I2.

Authors:  J M Link; K A Krohn; J C Clark
Journal:  Nucl Med Biol       Date:  1997-01       Impact factor: 2.408

5.  Labeling and evaluation of N-[11C]methylated quinoline-2-carboxamides as potential radioligands for visualization of peripheral benzodiazepine receptors.

Authors:  M Matarrese; R M Moresco; A Cappelli; M Anzini; S Vomero; P Simonelli; E Verza; F Magni; F Sudati; D Soloviev; S Todde; A Carpinelli; M G Kienle; F Fazio
Journal:  J Med Chem       Date:  2001-02-15       Impact factor: 7.446

Review 6.  Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers.

Authors:  Fabien Chauveau; Hervé Boutin; Nadja Van Camp; Frédéric Dollé; Bertrand Tavitian
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-10-01       Impact factor: 9.236

Review 7.  Translation of 11C-labeled tracer synthesis to a CGMP environment as exemplified by [11C]ER176 for PET imaging of human TSPO.

Authors:  Jinsoo Hong; Sanjay Telu; Yi Zhang; William H Miller; H Umesha Shetty; Cheryl L Morse; Victor W Pike
Journal:  Nat Protoc       Date:  2021-08-06       Impact factor: 13.491

8.  Synthesis and evaluation of translocator 18 kDa protein (TSPO) positron emission tomography (PET) radioligands with low binding sensitivity to human single nucleotide polymorphism rs6971.

Authors:  Paolo Zanotti-Fregonara; Yi Zhang; Kimberly J Jenko; Robert L Gladding; Sami S Zoghbi; Masahiro Fujita; Gianluca Sbardella; Sabrina Castellano; Sabrina Taliani; Claudia Martini; Robert B Innis; Federico Da Settimo; Victor W Pike
Journal:  ACS Chem Neurosci       Date:  2014-08-25       Impact factor: 4.418

9.  Radical Hydrodehalogenation of Aryl Bromides and Chlorides with Sodium Hydride and 1,4-Dioxane.

Authors:  Tobias Hokamp; Abhishek Dewanji; Maximilian Lübbesmeyer; Christian Mück-Lichtenfeld; Ernst-Ulrich Würthwein; Armido Studer
Journal:  Angew Chem Int Ed Engl       Date:  2017-09-19       Impact factor: 15.336

10.  Comparison of four 11C-labeled PET ligands to quantify translocator protein 18 kDa (TSPO) in human brain: (R)-PK11195, PBR28, DPA-713, and ER176-based on recent publications that measured specific-to-non-displaceable ratios.

Authors:  Masahiro Fujita; Masato Kobayashi; Masamichi Ikawa; Roger N Gunn; Eugenii A Rabiner; David R Owen; Sami S Zoghbi; Mohamad B Haskali; Sanjay Telu; Victor W Pike; Robert B Innis
Journal:  EJNMMI Res       Date:  2017-10-16       Impact factor: 3.138
  10 in total
  1 in total

1.  Tracers progress for positron emission tomography imaging of glial-related disease.

Authors:  Haoran Jia; Tianwu Xie
Journal:  J Biomed Res       Date:  2022-06-28
  1 in total

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