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.
Current Medicinal Chemistry
Title:In Vivo Imaging of the Metabotropic Glutamate Receptor 1 (mGluR1) with Positron Emission Tomography: Recent Advance and Perspective
Volume: 21 Issue: 1
Author(s): Songye Li and Yiyun Huang
Affiliation:
Keywords: Metabotropic glutamate receptor, mGlu1, radioligand, positron emission tomography, synthesis, evaluation.
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.
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Li Songye and Huang Yiyun, In Vivo Imaging of the Metabotropic Glutamate Receptor 1 (mGluR1) with Positron Emission Tomography: Recent Advance and Perspective, Current Medicinal Chemistry 2014; 21 (1) . https://dx.doi.org/10.2174/09298673113209990217
DOI https://dx.doi.org/10.2174/09298673113209990217 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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