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Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists |
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| 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 |
| Affiliation: | Vernalis plc, Oakdene Court, 613 Reading Road, Winnersh, Wokingham, Berkshire RG41 5UA, UK. |
| 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. |
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