| Literature DB >> 19523834 |
Ronald C Bernotas1, Steven Lenicek, Schuyler Antane, Derek C Cole, Boyd L Harrison, Albert J Robichaud, Guo Ming Zhang, Deborah Smith, Brian Platt, Qian Lin, Ping Li, Joseph Coupet, Sharon Rosenzweig-Lipson, Chad E Beyer, Lee E Schechter.
Abstract
A series of 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines 10a-z was prepared as novel 5-HT(6) ligands. The best compounds were high affinity, full agonists at 5-HT(6) 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 reduced adjunctive drinking behavior in the rat schedule-induced polydipsia assay, possibly predictive of efficacy in obsessive compulsive disorder and other anxiety related disorders.Entities:
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Year: 2009 PMID： 19523834 DOI： 10.1016/j.bmc.2009.05.055
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641