Title of article
The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists
Author/Authors
Bayard R. Huck، نويسنده , , Luis Llamas، نويسنده , , Michael J. Robarge، نويسنده , , Thomas C. Dent، نويسنده , , Jianping Song، نويسنده , , William F. Hodnick، نويسنده , , Chris Crumrine، نويسنده , , Alain Stricker-Krongrad، نويسنده , , John Harrington، نويسنده , , Kurt R. Brunden، نويسنده , , Youssef L. Bennani، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
2891
To page
2894
Abstract
The 5-HT2C 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-HT2C agonist from a unique pyrimidine-diazabicyclo[3.3.0]octane series. This compound displayed good potency at the 5-HT2C receptor, modest selectivity relative to other 5-HT2 receptors, and was efficacious in an acute feeding study in rats.
Keywords
5-HT2C , obesity
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796891
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