Author/Authors :
Steven M. Bromidge، نويسنده , , Stephen E. Clarke، نويسنده , , Tracey Gager، نويسنده , , Kerry Griffith، نويسنده , , Phillip Jeffrey، نويسنده , , Andrew J. Jennings، نويسنده , , Graham F. Joiner، نويسنده , , Frank D. King، نويسنده , , Peter J. Lovell، نويسنده , , Stephen F. Moss، نويسنده , , Helen Newman-Gage، نويسنده , , Graham Riley، نويسنده , , Derek Rogers، نويسنده , , Carol Routledge، نويسنده , , Halina Serafinowska، نويسنده , , Douglas R. Smith، نويسنده ,
Abstract :
Substituted N-phenyl-4-methoxy-3-piperazin-1-ylbenzenesulfonamides and conformationally restricted analogues have been identified as high affinity and selective 5-HT6 antagonists. Compounds from this series had a range of pharmacokinetic profiles in rat and in general there was a correlation between clearance and CNS penetration. Based on its overall biological profile 2 (SB-357134) was selected for further pre-clinical evaluation.
