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 ,
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.
