3-(4-Piperidinylalkyl)indoles, Selective Inhibitors of Neuronal 5-Hydroxytryptamine Uptake

Article abstract of DOI:10.1021/jm00186a005

A series 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.