Literature DB >> 22244939

[¹⁸F]GE-180: a novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO).

Harry Wadsworth1, Paul A Jones, Wai-Fung Chau, Clare Durrant, Naghmeh Fouladi, Joanna Passmore, Dennis O'Shea, Duncan Wynn, Veronique Morisson-Iveson, Amanda Ewan, Mikkel Thaning, Dimitrios Mantzilas, Ingvil Gausemel, Imtiaz Khan, Andrew Black, Michelle Avory, William Trigg.   

Abstract

A series of tricyclic compounds have been synthesised and evaluated in vitro for affinity against Translocator protein 18 kDa (TSPO) and for preferred imaging properties. The most promising of the compounds were radiolabelled and evaluated in vivo to determine biodistribution and specificity for high expressing TSPO regions. Metabolite profiling in brain and plasma was also investigated. Evaluation in an autoradiography model of neuroinflammation was also carried out for the best compound, 12a ([(18)F]GE-180).
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22244939     DOI： 10.1016/j.bmcl.2011.12.084

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  46 in total

1.  The validity of 18F-GE180 as a TSPO imaging agent.

Authors:  Paolo Zanotti-Fregonara; Mattia Veronese; Belen Pascual; Robert C Rostomily; Federico Turkheimer; Joseph C Masdeu
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-01-17       Impact factor: 9.236

2.  TSPO PET, tumour grading and molecular genetics in histologically verified glioma: a correlative 18F-GE-180 PET study.

Authors:  M Unterrainer; D F Fleischmann; F Vettermann; V Ruf; L Kaiser; D Nelwan; S Lindner; M Brendel; V Wenter; S Stöcklein; J Herms; V M Milenkovic; R Rupprecht; J C Tonn; C Belka; P Bartenstein; M Niyazi; N L Albert
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-09-05       Impact factor: 9.236

3.  TSPO PET for glioma imaging using the novel ligand 18F-GE-180: first results in patients with glioblastoma.

Authors:  Nathalie L Albert; M Unterrainer; D F Fleischmann; S Lindner; F Vettermann; A Brunegraf; L Vomacka; M Brendel; V Wenter; C Wetzel; R Rupprecht; J-C Tonn; C Belka; P Bartenstein; M Niyazi
Journal:  Eur J Nucl Med Mol Imaging       Date:  2017-08-19       Impact factor: 9.236

4.  TSPO PET using 18F-GE-180: a new perspective in neurooncology?

Authors:  Karl-Josef Langen; Antje Willuweit
Journal:  Eur J Nucl Med Mol Imaging       Date:  2017-10-12       Impact factor: 9.236

5.  A Facile Radiolabeling of [18F]FDPA via Spirocyclic Iodonium Ylides: Preliminary PET Imaging Studies in Preclinical Models of Neuroinflammation.

Authors:  Lu Wang; Ran Cheng; Masayuki Fujinaga; Jian Yang; Yiding Zhang; Akiko Hatori; Katsushi Kumata; Jing Yang; Neil Vasdev; Yunfei Du; Chongzhao Ran; Ming-Rong Zhang; Steven H Liang
Journal:  J Med Chem       Date:  2017-06-05       Impact factor: 7.446

6.  Letter to the Editor re: Confirmation of Specific Binding of the 18-kDa Translocator Protein (TSPO) Radioligand [18F]GE-180: a Blocking Study Using XBD173 in Multiple Sclerosis Normal Appearing White and Grey Matter.

Authors:  Paolo Zanotti-Fregonara; Mattia Veronese; Gaia Rizzo; Belen Pascual; Joseph C Masdeu; Federico E Turkheimer
Journal:  Mol Imaging Biol       Date:  2020-02       Impact factor: 3.488

Review 7.  Sifting through the surfeit of neuroinflammation tracers.

Authors:  Paul Cumming; Bjorn Burgher; Omkar Patkar; Michael Breakspear; Neil Vasdev; Paul Thomas; Guo-Jun Liu; Richard Banati
Journal:  J Cereb Blood Flow Metab       Date:  2017-12-19       Impact factor: 6.200

8.  TSPO PET with [18F]GE-180 sensitively detects focal neuroinflammation in patients with relapsing-remitting multiple sclerosis.

Authors:  Marcus Unterrainer; C Mahler; L Vomacka; S Lindner; J Havla; M Brendel; G Böning; B Ertl-Wagner; T Kümpfel; V M Milenkovic; R Rupprecht; M Kerschensteiner; P Bartenstein; Nathalie L Albert
Journal:  Eur J Nucl Med Mol Imaging       Date:  2018-03-09       Impact factor: 9.236

9.  Confirmation of Specific Binding of the 18-kDa Translocator Protein (TSPO) Radioligand [18F]GE-180: a Blocking Study Using XBD173 in Multiple Sclerosis Normal Appearing White and Grey Matter.

Authors:  Sujata Sridharan; Joel Raffel; Ashwini Nandoskar; Chris Record; David J Brooks; David Owen; David Sharp; Paolo A Muraro; Roger Gunn; Richard Nicholas
Journal:  Mol Imaging Biol       Date:  2019-10       Impact factor: 3.488

Review 10.  Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging in Neurological Diseases.

Authors:  Md Maqusood Alam; Jihye Lee; Sang-Yoon Lee
Journal:  Nucl Med Mol Imaging       Date:  2017-03-16
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