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 |
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| container_end_page | 260 |
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| container_issue | 3 |
| container_start_page | 251 |
| container_title | Journal of enzyme inhibition and medicinal chemistry |
| container_volume | 21 |
| creator | Raoul, Marion Patigny, Dominique Fabis, Frédréic Dauphin, FranÇis Rault, Sylvain Sapi, Janos Laronze, Jean-Yves |
| description | 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. |
| doi_str_mv | 10.1080/14756360600700285 |
| format | Article |
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| identifier | ISSN: 1475-6366 |
| ispartof | Journal of enzyme inhibition and medicinal chemistry, 2006-06, Vol.21 (3), p.251-260 |
| issn | 1475-6366 1475-6374 |
| language | eng |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Taylor & Francis Journals Complete |
| subjects | 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 |
| title | N-Arylsulfonyl-2-vinyltryptamines as new 5-HT6 serotonin receptor Ligands |
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