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…

文献索引：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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被引用次数: 13

摘要

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 ...