Abstract
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.
MeSH terms
-
Animals
-
Anti-Obesity Agents / pharmacology
-
Disease Models, Animal
-
Eating / drug effects*
-
Isoquinolines / chemistry
-
Isoquinolines / pharmacology*
-
Pyrroles / chemistry
-
Quinolines / chemistry
-
Quinolines / pharmacology*
-
Radioligand Assay
-
Rats
-
Serotonin 5-HT2 Receptor Agonists*
-
Serotonin Receptor Agonists / pharmacology*
Substances
-
Anti-Obesity Agents
-
Isoquinolines
-
Pyrroles
-
Quinolines
-
Serotonin 5-HT2 Receptor Agonists
-
Serotonin Receptor Agonists
-
isoquinoline