Abstract
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.
MeSH terms
-
Cyclic AMP / agonists
-
Cyclic AMP / antagonists & inhibitors
-
Cyclic AMP / biosynthesis
-
HeLa Cells
-
Humans
-
Indoles / chemical synthesis*
-
Indoles / chemistry
-
Indoles / pharmacology
-
Pyrrolidines / chemical synthesis*
-
Pyrrolidines / chemistry
-
Pyrrolidines / pharmacology
-
Receptors, Serotonin / drug effects*
-
Stereoisomerism
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis*
-
Sulfonamides / chemistry
-
Sulfonamides / pharmacology
Substances
-
Indoles
-
Pyrrolidines
-
Receptors, Serotonin
-
Sulfonamides
-
serotonin 6 receptor
-
Cyclic AMP