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Radiodefluorination of 3-Fluoro-5-(2-(2-[18F](fluoromethyl)- thiazol-4-yl)ethynyl)benzonitrile ([18F]SP203), a Radioligand for Imaging Brain Metabotropic Glutamate Subtype-5 Receptors with Positron Emission Tomography, Occurs by Glutathionylation in Rat B (2008)
BibTeX
@MISC{Shetty08radiodefluorinationof,
author = {H. Umesha Shetty and Sami S. Zoghbi and Fabrice G. Siméon and Jeih-san Liow and Amira K. Brown and Pavitra Kannan and Robert B. Innis and Victor W. Pike},
title = {Radiodefluorination of 3-Fluoro-5-(2-(2-[18F](fluoromethyl)- thiazol-4-yl)ethynyl)benzonitrile ([18F]SP203), a Radioligand for Imaging Brain Metabotropic Glutamate Subtype-5 Receptors with Positron Emission Tomography, Occurs by Glutathionylation in Rat B},
year = {2008}
}
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Abstract
Metabotropic glutamate subtype-5 receptors (mGluR5) are impli-cated in several neuropsychiatric disorders. Positron emission tomography (PET) with a suitable radioligand may enable moni-toring of regional brain mGluR5 density before and during treat-ments. We have developed a new radioligand, 3-fluoro-5-(2-(2-[18F](fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile ([18F]SP203), for imaging brain mGluR5 in monkey and human. In monkey, radioactivity was observed in bone, showing release of [18F]-fluoride ion from [18F]SP203. This defluorination was not inhib-ited by disulfiram, a potent inhibitor of CYP2E1. PET confirmed bone uptake of radioactivity and therefore defluorination of [18F]SP203 in rats. To understand the biochemical basis for defluorination, we administered [18F]SP203 plus SP203 in rats for ex vivo analysis of metabolites. Radio-high-performance
