New μ-Opioid Receptor Agonists with Phenoxyacetic Acid Moiety

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概要

• 論文の詳細を見る

• New μ-opioid receptor(MOR)agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, [2-[1-[3-(N, N-dimethylcarbamoyl)-3, 3-diphenylpropyl]-4-hydroxypiperidin-4-yl]phenoxy]aceitc acid(8:SS620)having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary(CHO)-K1 cells compared with the same types of δ-and κ-opioid receptors(DOR and KOR). In addition, compound 8 showed a 10 times more potent MOR agonist activity than loperamide. Furthermore, compound 8 showed a peripheral analgesic activity in vivo screening on rat.

• 公益社団法人日本薬学会の論文
• 2002-02-01

著者

• 佐藤 真悟

  Faculty of Pharmaceutical Sciences, Kanazawa University

• Sato S

  Tsitkuha Research Laboratories

• SAKAMOTO Takao

  Graduate School of Pharmaceutical Sciences, Tohoku University

• OKA Tetsuo

  Departmnet of Orthopedics, Asahikawa Medical College

• Oka Tetsuo

  Department Of Pharmacology School Of Medicine Tokai University

• Sato S

  Hisamitsu Pharmaceutical Co. Ltd. Ibaraki Jpn

• Sakamoto Takao

  Graduate School Of Pharmaceutical Sciences Tohoku University

• Miyashita Akira

  Central Research Laboratories Ssp Co. Ltd.

• SATO Susumu

  Central Research Labs., SS Pharmaceutical Co., Ltd.

• Oka Tetsuo

  Central Research Laboratories Ssp Co. Ltd.

• KOMOTO Teruo

  Central Research Laboratories SSP Co., Ltd.

• KANAMARU Yoshihiko

  Central Research Laboratories SSP Co., Ltd.

• KAWAMOTO Noriyuki

  Central Research Laboratories SSP Co., Ltd.

• OKADA Tomomi

  Central Research Laboratories SSP Co., Ltd.

• KAIHO Terumitsu

  Central Research Laboratories SSP Co., Ltd.

• MOGI Kinichi

  Central Research Laboratories SSP Co., Ltd.

• MORIMOTO Shinichi

  Central Research Laboratories SSP Co., Ltd.

• UMEHARA Norimitsu

  Central Research Laboratories SSP Co., Ltd.

• KODA Tadayuki

  Central Research Laboratories SSP Co., Ltd.

• Umehara Norimitsu

  Central Research Laboratories Ssp Co. Ltd.

• Morimoto Shinichi

  Central Research Laboratories Ssp Co. Ltd.

• Komoto Teruo

  Central Research Laboratories Ssp Co. Ltd.:graduate School Of Pharmaceutical Sciences Tohoku Univers

• Koda Tadayuki

  Central Research Laboratories Ssp Co. Ltd.

• Kanamaru Yoshihiko

  Central Research Laboratories Ssp Co. Ltd.

• Kawamoto Noriyuki

  Central Research Laboratories Ssp Co. Ltd.

• Kaiho Terumitsu

  Central Research Laboratories Ssp Co. Ltd.

• Mogi K

  Central Research Laboratories Ssp Co. Ltd.

• OKA Tetsuo

  Department of Clinical Pharmacology, School of Medicine, Tokai University

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