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  • Title: Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
    Author: Bromidge SM, Clarke SE, King FD, Lovell PJ, Newman H, Riley G, Routledge C, Serafinowska HT, Smith DR, Thomas DR.
    Journal: Bioorg Med Chem Lett; 2002 May 20; 12(10):1357-60. PubMed ID: 11992776.
    Abstract:
    The synthesis of novel 3-(octahydropyrido[1,2-a]pyrazin-2-yl)- and 3-(hexahydropyrrolo[1,2-a]pyrazin-2-yl)phenyl-2-benzo[b]thiophene sulphonamide derivatives 3, (S)-4 and (R)-4 is described. The compounds show high affinity for the 5-HT6 receptor, excellent selectivity against a range of other receptors and good brain penetration.
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