Radiolabelling and in vivo evaluation of 11C-MPEP as a pet radioligand for the imaging of the metabotropic glutamate receptor 5 (MGLUR5)

2001 ◽  
Vol 44 (S1) ◽  
pp. S231-S232 ◽  
Author(s):  
M. Kokic ◽  
M. Honer ◽  
S. M. Ametamey ◽  
F. Gasparini ◽  
H. Andres ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
In Vivo Evaluation ◽  
Metabotropic Glutamate Receptor 5 ◽  
Metabotropic Glutamate

In vitro and in vivo evaluation of [18F]-FDEGPECO as a PET tracer for imaging the metabotropic glutamate receptor subtype 5 (mGluR5)

NeuroImage ◽  
2011 ◽  
Vol 56 (3) ◽  
pp. 984-991 ◽  
Author(s):  
Cindy A. Wanger-Baumann ◽  
Linjing Mu ◽  
Michael Honer ◽  
Sara Belli ◽  
Malte F. Alf ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Subtype ◽  
In Vivo Evaluation ◽  
Metabotropic Glutamate ◽  
Pet Tracer

Evidence that the metabotropic glutamate receptor 5 antagonist MPEP may act as an inhibitor of the norepinephrine transporter in vitro and in vivo

Synapse ◽  
2003 ◽  
Vol 50 (4) ◽  
pp. 269-276 ◽  
Author(s):  
Christian A. Heidbreder ◽  
Massimiliano Bianchi ◽  
Laurent P. Lacroix ◽  
Stefania Faedo ◽  
Elisabetta Perdona ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Norepinephrine Transporter ◽  
Metabotropic Glutamate Receptor 5 ◽  
Metabotropic Glutamate

scholarly journals Altered metabotropic glutamate receptor 5 markers in PTSD: In vivo and postmortem evidence

2017 ◽  
Vol 114 (31) ◽  
pp. 8390-8395 ◽  
Author(s):  
Sophie E. Holmes ◽  
Matthew J. Girgenti ◽  
Margaret T. Davis ◽  
Robert H. Pietrzak ◽  
Nicole DellaGioia ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Molecular Mechanisms ◽  
Metabotropic Glutamate Receptor ◽  
Metabotropic Glutamate Receptor 5 ◽  
Metabotropic Glutamate ◽  
Positron Emission ◽  
Positive Correlations ◽  
Human Postmortem Tissue ◽  
Glutamate System

Posttraumatic stress disorder (PTSD) is a prevalent and highly disabling disorder, but there is currently no targeted pharmacological treatment for it. Dysfunction of the glutamate system has been implicated in trauma and stress psychopathology, resulting in a growing interest in modulation of the glutamate system for the treatment of PTSD. Specifically, the metabotropic glutamate receptor 5 (mGluR5) represents a promising treatment target. We used [18F]FPEB, a radioligand that binds to the mGluR5, and positron emission tomography (PET) to quantify in vivo mGluR5 availability in human PTSD vs. healthy control (HCs) subjects. In an independent sample of human postmortem tissue, we investigated expression of proteins that have a functional relationship with mGluR5 and glucocorticoids in PTSD. We observed significantly higher cortical mGluR5 availability in PTSD in vivo and positive correlations between mGluR5 availability and avoidance symptoms. In the postmortem sample, we observed up-regulation of SHANK1, a protein that anchors mGluR5 to the cell surface, as well as decreased expression of FKBP5, implicating aberrant glucocorticoid functioning in PTSD. Results of this study provide insight into molecular mechanisms underlying PTSD and suggest that mGluR5 may be a promising target for mechanism-based treatments aimed at mitigating this disorder.

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