3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake

A series of 3-(4-piperidinylalkyl)indoles was synthesized and tested as uptake inhibitors of biogenic amines. Some of these compounds are potent and very selective in blocking the 5-hydroxytryptamine (5-HT) uptake, as evidenced by biochemical data and behavioral tests. A discussion on structure-acti...

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Veröffentlicht in:Journal of medicinal chemistry 1980-12, Vol.23 (12), p.1306-1310
Hauptverfasser: Gueremy, Claude, Audiau, Francois, Champseix, Alain, Uzan, Andre, Le Fur, Gerard, Rataud, Jean
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Sprache:eng
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Zusammenfassung:A series of 3-(4-piperidinylalkyl)indoles was synthesized and tested as uptake inhibitors of biogenic amines. Some of these compounds are potent and very selective in blocking the 5-hydroxytryptamine (5-HT) uptake, as evidenced by biochemical data and behavioral tests. A discussion on structure-activity relationships is given. The most interesting member of the series, indalpine, 3-[2-(4-piperidinyl)ethyl]indole (1), was selected for clinical studies.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00186a005