Synthesis and Simple 18F-Labeling of 3-Fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a High Affinity Radioligand for Imaging Monkey Brain Metabotropic Glutamate Subtype-5 Receptors with Positron Emission Tomography

• Published in: Journal of medicinal chemistry Vol. 50; no. 14; pp. 3256 - 3266
• Main Authors: Siméon, Fabrice G, Brown, Amira K, Zoghbi, Sami S, Patterson, Velvet M, Innis, Robert B, Pike, Victor W
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 12.07.2007
• Subjects: Animals; Brain - diagnostic imaging; Brain - metabolism; Chromatography, High Pressure Liquid; Humans; Macaca mulatta; Nitriles - metabolism; Positron-Emission Tomography; Radioligand Assay; Rats; Receptor, Metabotropic Glutamate 5; Receptors, Metabotropic Glutamate - metabolism; Thiazoles - metabolism

2-Fluoromethyl analogs of (3-[(2-methyl-1,3-thiazol-4yl)ethynyl]pyridine) were synthesized as potential ligands for metabotropic glutamate subtype-5 receptors (mGluR5s). One of these, namely, 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile (3), was found to have exceptionally high a...