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

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Gueremy C, Audiau F, Champseix, Uzan A, Le Fur G, Rataud J

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

J Med Chem. 1980 Dec;23(12):1306-10.

PubMed ID

7452682 [ View in PubMed

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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.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clomipramine	Sodium-dependent serotonin transporter	IC 50 (nM)	70	N/A	N/A	Details