Discovery of N-{(1S,2S)-2-(3-Cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a Cannabinoid-1 Recepto

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• 作者：Ping Liu ; Linus S. Lin ; Terence G. Hamill ; James P. Jewell ; Thomas J. Lanza ; Jr ; Raymond E. Gibson ; Stephen M. Krause ; Christine Ryan ; Waisi Eng ; Sandra Sanabria ; Xinchun Tong ; Junying Wang ; Dorothy A
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：July 26, 2007
• 年：2007
• 卷：50
• 期：15
• 页码：3427 - 3430
• 全文大小：108K
• 年卷期：v.50,no.15(July 26, 2007)
• ISSN：1520-4804

文摘

The discovery of a structurally distinct cannabinoid-1receptor (CB1R) positron emission tomography tracer is described.Starting from an acyclic amide CB1R inverse agonist (1) as the leadcompound, an efficient route to introduce ¹⁸F to the molecule wasdeveloped. Further optimization focused on reducing the lipophilicityand increasing the CB1R affinity. These efforts led to the identificationof [¹⁸F]-16 that exhibited good brain uptake and an excellent signal-to-noise ratio in rhesus monkeys.