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Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor |
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| Authors: | Bromidge S M Griffith K Heightman T D Jennings A King F D Moss S F Newman H Riley G Routledge C Serafinowska H T Thomas D R |
| Affiliation: | Discovery Chemistry Europe, GlaxoSmithKline, Discovery Research, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK |
| Abstract: | The discovery of (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides and their binding affinities for a selection of 5-HT and dopamine subreceptors is described. Many compounds show high affinity (pK(i)>8) for the 5-HT(6) receptor and >100-fold selectivity against a range of other receptors. Structure-activity relationships of these compounds are discussed. |
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