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

Harry Wadsworth; 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

doi:10.1016/j.bmcl.2011.12.084

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

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1308-13. doi: 10.1016/j.bmcl.2011.12.084. Epub 2011 Dec 27.

Authors

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

Affiliation

¹ GE Healthcare, The Grove Centre, White Lion Road, Amersham, Bucks HP9 7LL, UK.

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

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).

MeSH terms

Animals
Carbazoles / chemistry*
Carbazoles / metabolism
Fluorine Radioisotopes* / chemistry
Fluorine Radioisotopes* / metabolism
Ligands
Molecular Structure
Myocardium / metabolism
Positron-Emission Tomography*
Rats
Rats, Sprague-Dawley
Receptors, GABA / metabolism*

Substances

Carbazoles
Fluorine Radioisotopes
GE-180
Ligands
Receptors, GABA
TSPO protein, human