A Positron Emission Tomography Radioligand for the in Vivo Labeling of Metabotropic Glutamate 1 Receptor:  (3-Ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone

A selective metabotropic glutamate 1 receptor (mGlu1) antagonist was labeled with the positron-emitting radioisotope carbon-11 and evaluated in ex vivo biodistribution studies and micro-positron emission tomography (micro-PET) imaging experiments in rats. Results from animal experiments demonstrate...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2005-08, Vol.48 (16), p.5096-5099
Main Authors: Huang, Yiyun, Narendran, Raj, Bischoff, François, Guo, Ningning, Zhu, Zhihong, Bae, Sung-A, Lesage, Anne S, Laruelle, Marc
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Brain - diagnostic imaging
Brain - metabolism
Carbon Radioisotopes
Contrast media. Radiopharmaceuticals
Glutamatergic system (aspartate and other excitatory aminoacids)
Ligands
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Positron-Emission Tomography
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - pharmacology
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - pharmacology
Rats
Receptors, Metabotropic Glutamate - antagonists & inhibitors
Receptors, Metabotropic Glutamate - metabolism
Structure-Activity Relationship
Tissue Distribution
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Description
Summary:A selective metabotropic glutamate 1 receptor (mGlu1) antagonist was labeled with the positron-emitting radioisotope carbon-11 and evaluated in ex vivo biodistribution studies and micro-positron emission tomography (micro-PET) imaging experiments in rats. Results from animal experiments demonstrate that the radioligand [11C]2 is the first PET tracer capable of labeling the rat mGlu1 receptor in vivo.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm050263+