N-arylsulfonyl-2-vinyltryptamines as new 5-HT6 serotonin receptor ligands.
Fiche publication
Date publication
juin 2006
Auteurs
Membres identifiés du Cancéropôle Est :
Pr SAPI Janos
Tous les auteurs :
Raoul M, Patigny D, Fabis F, Dauphin F, Rault S, Sapi J, Laronze JY
Lien Pubmed
Résumé
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.
Référence
J Enzyme Inhib Med Chem. 2006 Jun;21(3):251-60.