Amino Acids and Peptides. LII. Design and Synthesis of Opioid Mimetics Containing a Pyrazinone Ring and Examinaiton of Their Opioid Receptor Binding Activity

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概要

• 論文の詳細を見る

• An amino group was introduced to the 3 or 6 position of a pyrazinone ring by cyclization of dipeptidyl chloromethyl ketones. Boc-Tyr-OH was coupled with the amino funciton, followed by removal of the Boc group to give pyrazinone ring-containing tyrosine derivatives. Of the various tyrosine derivatives prepared, 5-methyl-6-β-phenethyl-3-tyrosylaminobutyl-2(1H)-pyrazinone exhibited strong binding to the μ-opioid receptor with a K_i value of 55.8 nM and to the δ-opioid receptor with a K_i value of 2165 nM and with a K_iμ/K_iδ value of 0.026.

• 公益社団法人日本薬学会の論文
• 1998-09-15

著者

• Taguchi Hiroyuki

  College Of Pharmacy Nihon University

• OKADA Yoshio

  Faculty of Pharmaceutical Sciences, Kobe Gakuin University

• Lazarus L

  Medicinal Chemistry Group Lpc National Institute Of Environmental Health Sciences

• Okada Yoshio

  Faculty Of Pharmaceutical Sciences Kobe Gakuin University

• Takahashi M

  Research Center For Medicinal Plant Resources National Institute Of Biomedical Innovation

• YOKOI Toshio

  Faculty of Pharmaceutical Sciences, Kobe Gakuin University

• BRYANT Sharon

  Peptide Neurochemistry, LCBRA, National Institute of Environmental Health Sciences, Research Triangl

• LAZARUS Lawrence

  Peptide Neurochemistry, LCBRA, National Institute of Environmental Health Sciences, Research Triangl

• YOKOI Toshio

  The Graduate School of Food and Medicinal Sciences, Kobe Gakuin University

• BRYANT Sharon

  Medicinal Chemistry Group, LPC, National Institute of Environmental Health Sciences

• TSUKATANI Masaki

  Faculty of Pharmaceutical Sciences, Kobe Gakuin University

• TAGUCHI Hiroaki

  Faculty of Pharmaceutical Sciences, Kobe Gakuin University

• Bryant Sharon

  Medicinal Chemistry Group Lpc National Institute Of Environmental Health Sciences

• Yokoi T

  Kobe‐gakuin Univ. Hyogo Jpn

• Lazarus Lawrence

  Peptide Neurochemistry Lcbra National Institute Of Environmental Health Sciences Research Triangle P

• Yamamoto T

  R&d Laboratories Nippon Organon K.k.

• Taguchi H

  Kobe Pharmaceutical Univ. Kobe Jpn

• Taguchi Hiroaki

  Faculty Of Pharmaceutical Sciences Kobe-gakuin University

• Bryant Sharon

  Peptide Neurochemistry Lcbra National Institute Of Environmental Health Sciences Research Triangle P

• Yokoi Toshio

  Faculty Of Pharmaceutical Sciences And High-technology Research Center Kobe-gakuin University

• Tsuda Y

  Faculty Of Pharmaceutical Sciences And High Technology Research Center Kobe Gakuin University

• Tsukatani Masaki

  Faculty Of Pharmaceutical Science Kobe Gakuin University

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