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 …

…, AK Brown, SS Zoghbi, VM Patterson…

Index: Simeon, Fabrice G.; Brown, Amira K.; Zoghbi, Sami S.; Patterson, Velvet M.; Innis, Robert B.; Pike, Victor W. Journal of Medicinal Chemistry, 2007 , vol. 50, # 14 p. 3256 - 3266

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Citation Number: 63

Abstract

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 affinity (IC50= 36 pM) and potency in a phosphoinositol hydrolysis assay (IC50= 0.714 pM) for mGluR5. Compound 3 was labeled with fluorine-18 ...