The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT_2C receptor agonists

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• 作者：Bayard R. Huck ; Luis Llamas ; Michael J. Robarge ; Thomas C. Dent ; Jianping Song ; William F. Hodnick ; Chris Crumrine ; Alain Stricker-Krongrad ; John Harrington ; Kurt R. Brunden and Youssef L. Bennani
• 关键词：5-HT2C ; Obesity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 June 2006
• 年：2006
• 卷：16
• 期：11
• 页码：2891-2894
• 全文大小：147 K

文摘

The 5-HT_2C receptor has been implicated in the regulation of appetite. As such, small molecule agonists to this receptor may serve as novel therapies to combat obesity. We describe here the identification, synthesis, and SAR of a 5-HT_2C agonist from a unique pyrimidine-diazabicyclo[3.3.0]octane series. This compound displayed good potency at the 5-HT_2C receptor, modest selectivity relative to other 5-HT2 receptors, and was efficacious in an acute feeding study in rats.