scholarly journals Noninvasive Quantification of Metabotropic Glutamate Receptor Type 1 with [11C]ITDM: a Small-Animal PET Study

2014 ◽  
Vol 34 (4) ◽  
pp. 606-612 ◽  
Author(s):  
Tomoteru Yamasaki ◽  
Masayuki Fujinaga ◽  
Joji Yui ◽  
Yoko Ikoma ◽  
Akiko Hatori ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Arterial Input Function ◽  
Small Animal Pet ◽  
Receptor Type ◽  
Binding Potential ◽  
Reference Tissue ◽  
Metabotropic Glutamate

Because of its role in multiple central nervous system (CNS) pathways, metabotropic glutamate receptor type 1 (mGluR1) is a crucial target in the development of pharmaceuticals for CNS disorders. N-[4-[6-(isopropylamino)-pyrimidin-4-yl]-1,3-thiazol-2-yl]- N-methyl-4-[11C]-methylbenzamide ([11C]ITDM) was recently developed as a positron emission tomography (PET) ligand for mGluR1. To devise a method for measurement of the binding potential ( BP ND) of [11C]ITDM to mGluR1, reference tissue methods aimed at replacing measurement of the arterial input function are desirable. In this study, we evaluated a noninvasive quantification method of mGluR1 with [11C]ITDM, demonstrating its accuracy using Huntington disease model R6/2 mice. The BP ND measurements based on the Logan reference (Logan Ref) method have closely approximated that based on the arterial input method. We performed PET analysis with Logan Ref to assess its accuracy in quantifying the decline of mGluR1 expression in R6/2 mice. Significant decreases in BP ND values in R6/2 mice were detected in cerebellum, thalamus, striatum, and cingulate cortex. We compared autoradiographs of R6/2 mouse brain sections with immunohistochemical images, and found a close correlation between changes in radioactive signal intensity and degree of mGluR1 expression. In conclusion, [11C]ITDM-PET is a promising tool for in vivo quantification of mGluR1 expression.

Radiosynthesis and evaluation of [11C]YM-202074 as a PET ligand for imaging the metabotropic glutamate receptor type 1

2010 ◽  
Vol 37 (5) ◽  
pp. 615-624 ◽  
Author(s):  
Kazuhiko Yanamoto ◽  
Fujiko Konno ◽  
Chika Odawara ◽  
Tomoteru Yamasaki ◽  
Kazunori Kawamura ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Type ◽  
Metabotropic Glutamate

scholarly journals Metabotropic glutamate receptor type 1 in taste tissue

2009 ◽  
Vol 90 (3) ◽  
pp. 743S-746S ◽  
Author(s):  
Ana San Gabriel ◽  
Takami Maekawa ◽  
Hisayuki Uneyama ◽  
Kunio Torii
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Type ◽  
Metabotropic Glutamate

scholarly journals Metabotropic glutamate receptor type 1 autoimmunity

Neurology ◽  
2016 ◽  
Vol 86 (11) ◽  
pp. 1009-1013 ◽  
Author(s):  
A. Sebastian Lopez-Chiriboga ◽  
Lars Komorowski ◽  
Tania Kümpfel ◽  
Christian Probst ◽  
Shannon R. Hinson ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Type ◽  
Metabotropic Glutamate

scholarly journals Autoimmune encephalitis associated with antibodies against the metabotropic glutamate receptor type 1: case report and review of the literature

2019 ◽  
Vol 12 ◽  
pp. 175628641984741 ◽  
Author(s):  
Monika Christ ◽  
Torsten Müller ◽  
Corinna Bien ◽  
Thomas Hagen ◽  
Markus Naumann ◽  
...  
Keyword(s):  
Cerebellar Ataxia ◽  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Clinical Symptoms ◽  
Clinical Course ◽  
Autoimmune Encephalitis ◽  
Receptor Type ◽  
Metabotropic Glutamate

Autoimmune encephalitis associated with antibodies against the metabotropic glutamate receptor type 1 is a rare autoimmune disease with only 18 cases being described in the literature so far. Most patients present with subacute cerebellar ataxia. In more than one third of cases a paraneoplastic aetiology has been suspected. Here we report a case of a 45-year-old man without known malignancy, who presented with progressive dysarthria and subsequently developed subacute cerebellar ataxia. Immunotherapy with glucocorticoids, i.v. immunoglobulins and rituximab improved clinical symptoms and resulted in a stable disease course up to the present. The article describes the clinical course of the patient with a follow-up-period of approximately 24 months and reviews the cases reported in the literature so far.

scholarly journals Preclinical anaylses of [18F]cEFQ as a PET tracer for imaging metabotropic glutamate receptor type 1 (mGluR1)

2016 ◽  
Vol 37 (6) ◽  
pp. 2283-2293 ◽  
Author(s):  
Boeun Lee ◽  
Yu Kyeong Kim ◽  
Ji Youn Lee ◽  
Young Joo Kim ◽  
Yun-Sang Lee ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Specific Activity ◽  
Receptor Type ◽  
Metabotropic Glutamate ◽  
Pet Tracer ◽  
Specific Antagonist ◽  
Pre Treatment

Metabotropic glutamate receptor type 1 (mGluR1) is related with various neurological and psychiatric diseases, such as anxiety, depression, epilepsy, Parkinson’s disease, and neuropathic pain. Hence, mGluR1 is an important target for drug development and imaging. We synthesized [18F]cEFQ (3-ethyl-2-[18F]fluoroquinolin-6-yl cis-(4-methoxycyclohexyl)methanone) as a PET tracer for selective mGluR1 imaging and evaluated its properties in rodents. A chloroquinoline precursor was labeled by a nucleophilic substitution reaction, and the resulting [18F]cEFQ was obtained with high radiochemical purity (>99%) and specific activity (63-246 GBq/µmol). The log D value was 3.24, and the initial brain uptake at 10 min was over 4% of injected dose per gram in BALB/c mice. According to PET/CT and autoradiography in SD rats, [18F]cEFQ showed wide distribution in the whole brain and the highest uptake in the cerebellum. Pre-treatment with unlabeled cEFQ or the mGluR1-specific antagonist JNJ16259685 blocked the uptake of [18F]cEFQ. However, the uptake was not blocked by pre-treatment with the mGluR5-specific antagonist ABP688. The trans isomer [18F]tEFQ did not show high uptake in the mGluR1-rich region. [18F]cEFQ was straightforwardly prepared using a chloro-derivative precursor. Its feasibility as a specific and selective PET agent for imaging mGluR1 was proved by in vitro and in vivo experiments using rodents.

scholarly journals In vivo characterization of metabotropic glutamate receptor type 5 abnormalities in behavioral variant FTD

2015 ◽  
Vol 221 (3) ◽  
pp. 1387-1402 ◽  
Author(s):  
Antoine Leuzy ◽  
Eduardo Rigon Zimmer ◽  
Jonathan Dubois ◽  
Jens Pruessner ◽  
Cory Cooperman ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Type ◽  
Metabotropic Glutamate ◽  
In Vivo Characterization
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