1. Development of [18F]-PSS223 as a PET Tracer for Imaging of Metabotropic Glutamate Receptor Subtype 5 (mGluR5)
- Author
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Selena Milicevic Sephton, Patrick Dennler, Dominique S. Leutwiler, Linjing Mu, Roger Schibli, Stefanie D. Krämer, and Simon M. Ametamey
- Subjects
[11 c]-abp688 ,[18 f]-fdegpeco ,[18 f]-pss223 ,Mglur5 ,Pet imaging ,Chemistry ,QD1-999 - Abstract
Involvement of metabotropic glutamate receptor subtype 5 (mGluR5) in physiological and pathophysiological processes in the brain has been demonstrated, and hence mGluR5 has emerged as an important drug target. [11C]-ABP688 is clinically the most successful mGluR5 positron emission tomography (PET) tracer to date and it allows visualization and quantification of mGluR5. Due to the short half-life of carbon-11, clinical use of [11C]-ABP688 is limited to facilities with an on-site cyclotron and a fluorine-18 (half-life 110 min) analogue would be more practical. Based on the [11C]-ABP688 structural motif, a novel derivative [18F]-PSS223 was prepared and evaluated as a PET tracer for imaging of mGluR5 in vitro and in vivo. Our results show favourable in vitro binding properties; however rapid defluorination of [18F]-PSS223 does not allow visualization of mGluR5 in the rat brain.
- Published
- 2012
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