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

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)...

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Published inBioorganic & medicinal chemistry letters Vol. 16; no. 3; pp. 677 - 680
Main Authors 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
Format Journal Article
LanguageEnglish
Published England 01.02.2006
Subjects
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
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Summary: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.
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ISSN:0960-894X
1464-3405