3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT6 receptor modulators |
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| Authors: | Ronald C Bernotas Schuyler Antane Rajesh Shenoy Van-Duc Le Ping Chen Boyd L Harrison Albert J Robichaud Guo Ming Zhang Deborah Smith Lee E Schechter |
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| Institution: | 1. Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426, USA;2. Chemical Sciences, Wyeth Pharmaceuticals, CN 8000, Princeton, NJ 08543, USA;3. Neuroscience, Wyeth Pharmaceuticals, CN 8000, Princeton, NJ 08543, USA;4. Albany Molecular Research, PO Box 15098, Albany, NY 12212, USA |
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| Abstract: | Novel 3-(arylsulfonyl)-1-(azacyclyl)-1H-indoles 6 were synthesized as potential 5-HT6 receptor ligands, based on constraining a basic side chain as either a piperidine or a pyrrolidine. Many of these compounds had good 5-HT6 binding affinity with Ki values <10 nM. Depending on substitution, both agonists (e.g., 6o: EC50 = 60 nM, Emax = 70%) and antagonists (6y: IC50 = 17 nM, Imax = 86%) were identified in a 5-HT6 adenylyl cyclase assay. |
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