Discovery of [18F]N-(2-(Diethylamino)ethyl)-6-fluoronicotinamide: A Melanoma Positron Emission Tomography Imaging Radiotracer with High Tumor to Body Contrast Ratio and Rapid Renal C

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• 作者：Ivan Greguric ; Stephen R. Taylor ; Delphine Denoyer ; Patrice Ballantyne ; Paula Berghofer ; Peter Roselt ; Tien Q. Pham ; Filomena Mattner ; Thomas Bourdier ; Oliver C. Neels ; Donna S. Dorow ; Christian Loc&#
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：September 10, 2009
• 年：2009
• 卷：52
• 期：17
• 页码：5299-5302
• 全文大小：712K
• 年卷期：v.52,no.17(September 10, 2009)
• ISSN：1520-4804

文摘

The high melanoma uptake and rapid body clearance displayed by our series of [¹²³I]iodonicotinamides prompted the development of [¹⁸F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([¹⁸F]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [¹⁸F]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [¹⁸F]2 displayed high tumor uptake, rapid body clearance via predominantly renal excretion, and is currently being evaluated in preclinical studies for progression into clinical trials to assess the responsiveness of therapeutic agents.