title: Cyclopropyl-tryptamine analogues: synthesis and biological evaluation as 5-HT(6) receptor ligands.
abstract: Conformational restrictions: Based on the pharmacophore model for 5-HT(6)  receptor ligands (shown), tryptamine analogues bearing a cyclopropyl ring on the α-position of the tryptamine side chain were synthesized and evaluated against 5-HT receptors. N,N-Dimethyl-1-arylsulfonyltryptamine derivatives exhibited promising selectivity for 5-HT(6)  over 5-HT(1a)  and 5-HT(4)  receptors and interesting activity against 5-HT(6)  (K(i) =∼0.15 μM; IC(50) =∼0.20 μM).
authors.affiliation: Institut de Chimie Moléculaire de Reims, UMR CNRS 7312 (ex 6229), Faculté de Pharmacie, Université de Reims-Champagne-Ardenne, 51096 Reims Cedex and UFR Sciences, 51687, Reims Cedex 2, France.
authors.forename: Claude
authors.initials: C
authors.lastname: Szalata
authors.forename: Jan
authors.initials: J
authors.lastname: Szymoniak
authors.forename: Frédéric
authors.initials: F
authors.lastname: Fabis
authors.forename: Sabrina
authors.initials: S
authors.lastname: Butt-Gueulle
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
authors.forename: Philippe
authors.initials: P
authors.lastname: Bertus
authors.forename: Stéphane
authors.initials: S
authors.lastname: Gérard
authors.forename: Janos
authors.initials: J
authors.lastname: Sapi
mesh_terms: D000818:Animals; D003521:Cyclopropanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D003521:Cyclopropanes; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines; C097216:serotonin 6 receptor