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  • Title: 3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.
    Author: Bernotas RC, Antane S, Shenoy R, Le VD, Chen P, Harrison BL, Robichaud AJ, Zhang GM, Smith D, Schechter LE.
    Journal: Bioorg Med Chem Lett; 2010 Mar 01; 20(5):1657-60. PubMed ID: 20138763.
    Abstract:
    Novel 3-(arylsulfonyl)-1-(azacyclyl)-1H-indoles 6 were synthesized as potential 5-HT(6) receptor ligands, based on constraining a basic side chain as either a piperidine or a pyrrolidine. Many of these compounds had good 5-HT(6) binding affinity with K(i) values <10nM. Depending on substitution, both agonists (e.g., 6o: EC(50)=60nM, E(max)=70%) and antagonists (6y: IC(50)=17 nM, I(max)=86%) were identified in a 5-HT(6) adenylyl cyclase assay.
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