Abstract
Metabotropic glutamate receptor subtype 2 (mGlu2) is a G-protein-coupled receptor and involved in the physiopathology of several major mental disorders and neurodegenerative diseases. Nowadays, with the development of positron emission tomography (PET) tracers, the distribution and concentration of mGlu2 in vivo can be quantitatively evaluated, which could substantially facilitate disease diagnosis and drug discovery. To demonstrate continuous efforts in the development of mGlu2 PET tracers, we present an example with detailed protocols, including step-by-step procedures of chemical synthesis of an mGlu2-negative allosteric modulator, namely 7-((2,5-dioxopyrrolidin-1-yl)methyl)-4-(2-fluro-4-methoxyphenyl) quinoline-2-carboxamide (QCA), radiolabeling of [11C]QCA, ex vivo whole-body biodistribution, autoradiography, and dynamic PET imaging.
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Zhang, X. et al. (2021). Positron Emission Tomography (PET) Imaging of Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Based on a Negative Allosteric Modulator Radioligand. In: Olive, M.F., Burrows, B.T., Leyrer-Jackson, J.M. (eds) Metabotropic Glutamate Receptor Technologies. Neuromethods, vol 164. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-1107-4_2
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DOI: https://doi.org/10.1007/978-1-0716-1107-4_2
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