Development of [18F]-PSS223 as a PET Tracer for Imaging of Metabotropic Glutamate Receptor Subtype 5 (mGluR5)

Authors

  • Selena Milicevic Sephton SCS-Metrohm Foundation Award for best oral presentation, Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland
  • Patrick Dennler Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland
  • Dominique S. Leutwiler Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland
  • Linjing Mu Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland
  • Roger Schibli Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland
  • Stefanie D. Krämer Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland
  • Simon M. Ametamey Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland. simon.ametamey@pharma.ethz.ch

DOI:

https://doi.org/10.2533/chimia.2012.201

Keywords:

[11 c]-abp688, [18 f]-fdegpeco, [18 f]-pss223, Mglur5, Pet imaging

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.
CHIMIA Vol. 66 No. 4 (2012): Laureates: Awards and Honors, SCS Fall Meeting

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Published

2012-04-25

Issue

Vol. 66 No. 4 (2012): Laureates: Awards and Honors, SCS Fall Meeting 2011

Section

Scientific Articles

License

Copyright (c) 2012 Swiss Chemical Society

Creative Commons License

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

How to Cite

[1]
S. M. Sephton, P. Dennler, D. S. Leutwiler, L. Mu, R. Schibli, S. D. Krämer, S. M. Ametamey, Chimia 2012, 66, 201, DOI: 10.2533/chimia.2012.201.