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Development of [(18)F]-PSS223 as a PET tracer for imaging of metabotropic glutamate receptor subtype 5 (mGluR5)


Sephton, Selena Milicevic; Dennler, Patrick; Leutwiler, Dominique S; Mu, Linjing; Schibli, Roger; Krämer, Stefanie D; Ametamey, Simon M (2012). Development of [(18)F]-PSS223 as a PET tracer for imaging of metabotropic glutamate receptor subtype 5 (mGluR5). CHIMIA International Journal for Chemistry, 66(4):201-204.

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. [(11)C]-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 [(11)C]-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 [(11)C]-ABP688 structural motif, a novel derivative [(18)F]-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 [(18)F]-PSS223 does not allow visualization of mGluR5 in the rat brain.

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. [(11)C]-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 [(11)C]-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 [(11)C]-ABP688 structural motif, a novel derivative [(18)F]-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 [(18)F]-PSS223 does not allow visualization of mGluR5 in the rat brain.

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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:04 Faculty of Medicine > University Hospital Zurich > Clinic for Nuclear Medicine
Dewey Decimal Classification:610 Medicine & health
Date:2012
Deposited On:04 Feb 2013 12:10
Last Modified:05 Apr 2016 16:22
Publisher:Swiss Chemical Society
ISSN:0009-4293
Publisher DOI:https://doi.org/10.2533/chimia.2012.201
PubMed ID:22613149

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