Author(s): Bromidge SM, Clarke SE, Gager T, Griffith K, Jeffrey P,
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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.
This article was published in Bioorg Med Chem Lett
and referenced in Journal of Genetic Syndromes & Gene Therapy