[2-(ω-Phenylalkyl)phenoxy]alkylamines : Synthesis and Dual Dopamine2 (D2) and 5-Hydroxytryptamine2 (5-HT2) Receptor Antagonistic Activities

Naoki TANAKA; Riki GOTO; Rie ITO; Miho HAYAKAWA; Taketoshi OGAWA; Koichi FUJIMOTO

doi:10.1248/cpb.46.639

[2-(ω-Phenylalkyl)phenoxy]alkylamines : Synthesis and Dual Dopamine₂ (D₂) and 5-Hydroxytryptamine₂ (5-HT₂) Receptor Antagonistic Activities

Naoki TANAKA, Riki GOTO, Rie ITO, Miho HAYAKAWA, Taketoshi OGAWA, Koichi FUJIMOTO

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Keywords: 5-hydroxytryptamine₂ (5-HT₂), dopamine₂ (D₂), dual antagonist, antagonistic activity, [2-(4-phenylbutyl)phenoxy]alkylamine

JOURNAL FREE ACCESS

1998 Volume 46 Issue 4 Pages 639-646

DOI https://doi.org/10.1248/cpb.46.639

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Abstract

A series of [2-(ω-phenylalkyl)phenoxy]alkylamines was synthesized and their 5-hydroxytryptamine₂ (5-HT₂) and/or dopamine₂ (D₂) receptor antagonistic activities were examined in vitro. [2-(4-Phenylbutyl)phenoxy]alkylamines showed strong inhibition of both 5-HT₂ and D₂ receptors. It particular, [2-(4-phenylbutyl)phenoxy]-methylpiperidine derivatives, 10b, 10i and 10q, exhbited potent inhibition. The structure-activity relationships in this series of compounds are discussed.

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