[2-(ω-Phenylalkyl)phenoxy]alkylamines II : Synthesis and Selective Serotonin-2-Receptor Binding

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概要

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• A series of [2-(ω-phenylalkyl)phenoxy]alkylamines was synthesized and thir receptor binding affinity was examined in vitro. These compounds showed an affinity for serotonin-2 (5-HT_2) and dopamine-2 (D_2) receptors. [2-(2-phenylethyl)phenoxy]alkylamine derivatives with a pyrrolidine or piperidine moiety in the structure showed higher affinity for 5-HT_2 receptors but lower affinity for D_2 receptors. Among these compounds, (S)-2-[2-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]ethyl]1-methylpyrrolidine, (S)-27,exhibited the most potent and selective affinity for 5-HT_2 receptors. Furthermore, (S)-27 was effective in inhibiting 5-HT-induced vasoconstriction in vitro and platelet aggregation both in vitro and ex vivo.

• 公益社団法人日本薬学会の論文
• 2000-02-01

著者

• Tanaka N

  Department Of Pharmacology School Of Pharmaceutical Sciences Mukogawa Women's University

• Tanaka Naoko

  武庫川女子大学 薬学部薬理学

• Tanaka Naoki

  Medical ProteoScope Co., Ltd.

• 中西 務

  Faculty Of Pharmaceutical Sciences Setsunan University

• Ito Rie

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

• Tanaka N

  School Of Pharmaceutical Sciences Mukogawa Women S University

• Ogawa T

  R & D Division Daiichi Sankyo Co. Ltd.

• GOTO Riki

  Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.

• HAYAKAWA Miho

  Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.

• FUJIMOTO Koichi

  Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.

• SUGIDACHI Atsuhiro

  Pharmacology and Molecular Biology Research Laboratories, Sankyo Co., Ltd.

• OGAWA Taketoshi

  Pharmacology and Molecular Biology Research Laboratories, Sankyo Co., Ltd.

• ASAI Fumitoshi

  Pharmacology and Molecular Biology Research Laboratories, Sankyo Co., Ltd.

• Goto R

  R & D Division Daiichi Sankyo Co. Ltd.

• Hayakawa Miho

  R & D Division Daiichi Sankyo Co. Ltd.

• Asai Fumitoshi

  R & D Division Daiichi Sankyo Co. Ltd.

• Fujimoto K

  R & D Division Daiichi Sankyo Co. Ltd.

• Sugidachi Atsuhiro

  R & D Division Daiichi Sankyo Co. Ltd.

• Nishimata Toyoki

  R & D Division Daiichi Sankyo Co. Ltd.

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