- Record: found
- Abstract: not found
- Article: not found
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT6 agonists
Ronald C. Bernotas ,
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
July 2009
July 2009
There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.
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.