N-Arylsulfonyl-2-vinyltryptamines as new 5-HT6 serotonin receptor Ligands

Several new 2-vinyl-Nb,Nb-dimethyltryptamines were prepared using Fischer indole synthesis followed by simple functional group transformations and evaluated on 5-HT4, 5-HT5, 5-HT6 and 5-HT7 serotonin receptors. It was found that 2-vinyl substitution conferred a potent and selective 5-HT6 binding act...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2006-06, Vol.21 (3), p.251-260
Hauptverfasser:	Raoul, Marion, Patigny, Dominique, Fabis, Frédréic, Dauphin, FranÇis, Rault, Sylvain, Sapi, Janos, Laronze, Jean-Yves
Format:	Artikel
Sprache:	eng
Schlagworte:	2-vinyl-N 5-HT Animals arylsulfonyl-tryptamines Binding Sites CHO Cells Cognitive science Cricetinae dimethyltryptamines Drug Evaluation, Preclinical Guinea Pigs Humans Indoles - chemical synthesis Indoles - chemistry Ligands Male Molecular Structure Neuroscience radioligand binding tests receptor inhibitors Receptors, Serotonin - drug effects Stereoisomerism Structure-Activity Relationship Tryptamines - chemical synthesis Tryptamines - chemistry Tryptamines - pharmacology Vinyl Compounds - chemical synthesis Vinyl Compounds - chemistry Vinyl Compounds - pharmacology
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Zusammenfassung:	Several new 2-vinyl-Nb,Nb-dimethyltryptamines were prepared using Fischer indole synthesis followed by simple functional group transformations and evaluated on 5-HT4, 5-HT5, 5-HT6 and 5-HT7 serotonin receptors. It was found that 2-vinyl substitution conferred a potent and selective 5-HT6 binding activity to these molecules which could be enhanced by Na-arylsulfonyl substituents.
ISSN:	1475-6366 1475-6374
DOI:	10.1080/14756360600700285