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

Chimia - Tập 66 Số 4 - Trang 201
Selena Milicevic Sephton1, Patrick Dennler2, Dominique S. Leutwiler2, Linjing Mu2, Roger Schibli2, Stefanie D. Krämer2, Simon M. Ametamey3
1SCS-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
2Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences ETH-Hönggerberg, Wolfgang-Pauli Strasse 10, CH-8093 Zürich, Switzerland
3Center for Radiopharmaceutical Sciences of ETH, PSI and USZ Department of Chemistry and Applied Biosciences ETH-Hönggerberg Wolfgang-Pauli Strasse 10 CH-8093 Zürich

Tóm tắt

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.

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Chimia

Tập 66 Số 4

201

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