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

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

2019 ◽  
Vol 12 ◽  
pp. 175628641984741 ◽  
Author(s):  
Monika Christ ◽  
Torsten Müller ◽  
Corinna Bien ◽  
Thomas Hagen ◽  
Markus Naumann ◽  
...  

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.


2016 ◽  
Vol 37 (6) ◽  
pp. 2283-2293 ◽  
Author(s):  
Boeun Lee ◽  
Yu Kyeong Kim ◽  
Ji Youn Lee ◽  
Young Joo Kim ◽  
Yun-Sang Lee ◽  
...  

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.


2010 ◽  
Vol 67 (5) ◽  
Author(s):  
Romain Marignier ◽  
Florian Chenevier ◽  
Veronique Rogemond ◽  
Peter Sillevis Smitt ◽  
Christel Renoux ◽  
...  

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