scholarly journals Discovery of Molecular Switches That Modulate Modes of Metabotropic Glutamate Receptor Subtype 5 (mGlu5) Pharmacology in Vitro and in Vivo within a Series of Functionalized, Regioisomeric 2- and 5-(Phenylethynyl)pyrimidines

2009 ◽  
Vol 52 (14) ◽  
pp. 4103-4106 ◽  
Author(s):  
Sameer Sharma ◽  
Jeffrey Kedrowski ◽  
Jerri M. Rook ◽  
Randy L. Smith ◽  
Carrie K. Jones ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Molecular Switches ◽  
Receptor Subtype ◽  
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

Radiolabeling and in vitro and in vivo evaluation of [18F]-FE-DABP688 as a PET radioligand for the metabotropic glutamate receptor subtype 5

2007 ◽  
Vol 34 (8) ◽  
pp. 973-980 ◽  
Author(s):  
Michael Honer ◽  
Anja Stoffel ◽  
Lea J. Kessler ◽  
P. August Schubiger ◽  
Simon M. Ametamey
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Subtype ◽  
In Vivo Evaluation ◽  
Metabotropic Glutamate

scholarly journals Ketamine and Ceftriaxone-Induced Alterations in Glutamate Levels Do Not Impact the Specific Binding of Metabotropic Glutamate Receptor Subtype 5 Radioligand [18F]PSS232 in the Rat Brain

2018 ◽  
Vol 11 (3) ◽  
pp. 83 ◽  
Author(s):  
Adrienne Müller Herde ◽  
Silvan Boss ◽  
Yingfang He ◽  
Roger Schibli ◽  
Linjing Mu ◽  
...  
Keyword(s):  
Rat Brain ◽  
Glutamate Receptor ◽  
Bolus Injection ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Subtype ◽  
Metabotropic Glutamate ◽  
In Vitro Autoradiography ◽  
Direct Competition

Several studies showed that [11C]ABP688 binding is altered following drug-induced perturbation of glutamate levels in brains of humans, non-human primates and rats. We evaluated whether the fluorinated derivative [18F]PSS232 can be used to assess metabotropic glutamate receptor 5 (mGluR5) availability in rats after pharmacological challenge with ketamine, known to increase glutamate, or ceftriaxone, known to decrease glutamate. In vitro autoradiography was performed on rat brain slices with [18F]PSS232 to prove direct competition of the drugs for mGluR5. One group of rats were challenged with a bolus injection of either vehicle, racemic ketamine, S-ketamine or ceftriaxone followed by positron emission tomography PET imaging with [18F]PSS232. The other group received an infusion of the drugs during the PET scan. Distribution volume ratios (DVRs) were calculated using a reference tissue model. In vitro autoradiography showed no direct competition of the drugs with [18F]PSS232 for the allosteric binding site of mGluR5. DVRs of [18F]PSS232 binding in vivo did not change in any brain region neither after bolus injection nor after infusion. We conclude that [18F]PSS232 has utility for measuring mGluR5 density or occupancy of the allosteric site in vivo, but it cannot be used to measure in vivo fluctuations of glutamate levels in the rat brain.

scholarly journals Correlation of Receptor Occupancy of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Mouse Brain With In Vivo Activity of Allosteric mGluR1 Antagonists

2009 ◽  
Vol 110 (3) ◽  
pp. 315-325 ◽  
Author(s):  
Gentaroh Suzuki ◽  
Hiroko Kawagoe-Takaki ◽  
Takao Inoue ◽  
Toshifumi Kimura ◽  
Hirohiko Hikichi ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Mouse Brain ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Occupancy ◽  
Receptor Subtype ◽  
Metabotropic Glutamate
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