Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Adams DR., Bentley JM., Benwell KR., Bickerdike MJ., Bodkin CD., Cliffe IA., Dourish CT., George AR., Kennett GA., Knight AR., Malcolm CS., Mansell HL., Misra A., Quirk K., Roffey JRA., Vickers SP.
A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) 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-HT(2) receptor subtypes are reported. The analogue which showed the highest 5-HT(2C) binding affinity (27, 1.6nM) was found to be successful in reducing food intake in rats.