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Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1 H -indole Derivatives as Potent, Selective 5-HT 6 Receptor Agonists and Antagonists

2004; American Chemical Society; Volume: 48; Issue: 2 Linguagem: Inglês

10.1021/jm049243i

1520-4804

Derek C. Cole, William J. Lennox, Sabrina Lombardi, John W. Ellingboe, Ronald C. Bernotas, Gregory J. Tawa, Hossein Mazandarani, Deborah L. Smith, Guoming Zhang, Joseph Coupet, Lee E. Schechter,

Nicotinic Acetylcholine Receptors Study

5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT(6) receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC(50) values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed moderate antagonist activity.