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Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.

Adams, David R; Bentley, Jonathan M; Benwell, Karen R; Bickerdike, Michael J; Bodkin, Corinna D; Cliffe, Ian A; Dourish, Colin T; George, Ashley R; Kennett, Guy A; Knight, Antony R; Malcolm, Craig S; Mansell, Howard L; Misra, Anil; Quirk, Kathleen; Roffey, Jonathan R A; Vickers, Steven P.

Bioorg Med Chem Lett ; 16(3): 677-80, 2006 Feb.

Article in English | MEDLINE | ID: mdl-16257207

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.

Subject(s)

Eating/drug effects , Isoquinolines/pharmacology , Quinolines/pharmacology , Serotonin 5-HT2 Receptor Agonists , Serotonin Receptor Agonists/pharmacology , Animals , Anti-Obesity Agents/pharmacology , Disease Models, Animal , Isoquinolines/chemistry , Pyrroles/chemistry , Quinolines/chemistry , Radioligand Assay , Rats

ABSTRACT

Subject(s)

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