Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo [2, 3-b] pyridines are potent 5-HT 6 agonists

…, Q Lin, P Li, J Coupet, S Rosenzweig-Lipson…

Index: Bernotas, Ronald C.; Lenicek, Steven; Antane, Schuyler; Cole, Derek C.; Harrison, Boyd L.; Robichaud, Albert J.; Zhang, Guo Ming; Smith, Deborah; Platt, Brian; Lin, Qian; Li, Ping; Coupet, Joseph; Rosenzweig-Lipson, Sharon; Beyer, Chad E.; Schechter, Lee E. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 14 p. 5153 - 5163

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Citation Number: 13

Abstract

A series of 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo [2, 3-b] pyridines 10a–z was prepared as novel 5-HT6 ligands. The best compounds were high affinity, full agonists at 5-HT6 receptors. Several agonists demonstrated good selectivity over other serotonergic and dopaminergic receptors. Acute administration of selective agonist 10e significantly increased extracellular GABA concentrations in rat frontal cortex. This compound also ...