The metabotropic glutamate 1 receptors (mGluR1) have been shown to play a role in neuropathic pain and neurological
and psychiatric disorders such as ischemia, epilepsy, anxiety, as well as schizophrenia and other cognitionrelated
disorders. As a result, mGluR1 has been an important target for drug development. As a radiotracer-based in vivo
imaging technique Positron Emission Tomography (PET) is an important tool in the investigation of receptor function in
the living brain under normal conditions and its dysfunction in diseases, as well as in the study of receptor occupancy by
experimental therapeutic agents. In this report we review the development and evaluation of PET radiotracers for mGluR1
and provide an assessment of the tracers that are likely to succeed in the imaging and quantification of mGluR1 in humans.
Keywords: Metabotropic glutamate receptor, mGlu1, radioligand, positron emission tomography, synthesis, evaluation.
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