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Metabotropic glutamate receptor subtype 1
(mGluR1; GRM1) binding PET radioligand for
in vivo imaging

A PET radioligand that binds mGluR1 could help diagnose and study neuropsychiatric disorders. In rhesus monkeys, injection of
[18F] 4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide resulted in substantial brain uptake and signal distribution that matched known mGluR1 densities. In the monkeys, pretreatment with an mGluR1 antagonist quickly decreased brain radioactivity, whereas mGluR5 (GRM5) ligand pretreatment had no effect. Next steps could include testing the radioligand in humans.

SciBX 6(47); doi:10.1038/scibx.2013.1369
Published online Dec. 12, 2013

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Xu, R. et al. J. Med. Chem.; published online Oct. 22, 2013;
Contact: Victor W. Pike, National Institutes of Health (NIH), Bethesda, Md.