Author/Authors :
David R. Adams، نويسنده , , Jonathan M. Bentley، نويسنده , , Karen R. Benwell، نويسنده , , Michael J. Bickerdike، نويسنده , , Corinna D. Bodkin، نويسنده , , Ian A. Cliffe، نويسنده , , Colin T. Dourish، نويسنده , , Ashley R. George، نويسنده , , Guy A. Kennett، نويسنده , , Antony R. Knight، نويسنده , , Craig S. Malcolm، نويسنده , , Howard L. Mansell، نويسنده , , Anil Misra، نويسنده , , Kathleen Quirk، نويسنده , , Jonathan R.A. Roffey، نويسنده , , Steven P. Vickers، نويسنده ,
Abstract :
A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for the compounds at 5-HT2 receptor subtypes are reported. The analogue which showed the highest 5-HT2C binding affinity (27, 1.6 nM) was found to be successful in reducing food intake in rats.
Keywords :
Obesity , Serotonin , 5-HT2C , agonist
