title: Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
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.
authors.affiliation: Vernalis plc, Oakdene Court, 613 Reading Road, Winnersh, Wokingham, Berkshire RG41 5UA, UK.
authors.forename: David R
authors.initials: DR
authors.lastname: Adams
authors.forename: Jonathan M
authors.initials: JM
authors.lastname: Bentley
authors.forename: Karen R
authors.initials: KR
authors.lastname: Benwell
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Bickerdike
authors.forename: Corinna D
authors.initials: CD
authors.lastname: Bodkin
authors.forename: Ian A
authors.initials: IA
authors.lastname: Cliffe
authors.forename: Colin T
authors.initials: CT
authors.lastname: Dourish
authors.forename: Ashley R
authors.initials: AR
authors.lastname: George
authors.forename: Guy A
authors.initials: GA
authors.lastname: Kennett
authors.forename: Antony R
authors.initials: AR
authors.lastname: Knight
authors.forename: Craig S
authors.initials: CS
authors.lastname: Malcolm
authors.forename: Howard L
authors.initials: HL
authors.lastname: Mansell
authors.forename: Anil
authors.initials: A
authors.lastname: Misra
authors.forename: Kathleen
authors.initials: K
authors.lastname: Quirk
authors.forename: Jonathan R A
authors.initials: JR
authors.lastname: Roffey
authors.forename: Steven P
authors.initials: SP
authors.lastname: Vickers
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology; D004195:Disease Models, Animal; D004435:Eating / Q000187:drug effects*; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D058826:Serotonin 5-HT2 Receptor Agonists; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*
chemical_list: D019440:Anti-Obesity Agents; D007546:Isoquinolines; D011758:Pyrroles; D011804:Quinolines; D058826:Serotonin 5-HT2 Receptor Agonists; D017366:Serotonin Receptor Agonists; C039109:isoquinoline