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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

In Vivo Imaging of the Metabotropic Glutamate Receptor 1 (mGluR1) with Positron Emission Tomography: Recent Advance and Perspective

Author(s): Songye Li and Yiyun Huang

Volume 21, Issue 1, 2014

Page: [113 - 123] Pages: 11

DOI: 10.2174/09298673113209990217

Price: $65

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Abstract

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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