Paper
3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake.
Published Dec 1, 1980 · C. Guérémy, F. Audiau, Champseix
Journal of medicinal chemistry
16
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0
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Abstract
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.
3-(4-piperidinylalkyl)indoles show potent and selective inhibition of neuronal 5-hydroxytryptamine uptake, with indalpine selected for clinical studies.
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