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2001 Fiscal Year Final Research Report Summary

Design and synthesis of μ-selective opioidomimetic peptides

Research Project

Project/Area Number 11694326
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field 医薬分子機能学
Research InstitutionKobe Gakuin University

Principal Investigator

OKADA Yoshio  Kobe Gakuin University, Faculty of Pharmaceutical Sciences, Professor, 薬学部, 教授 (60068236)

Co-Investigator(Kenkyū-buntansha) TSUDA Yuko  Kobe Gakuin University, Faculty of Pharmaceutical Sciences, Assistant Professor, 薬学部, 講師 (10098478)
YOKOI Toshio  Kobe Gakuin University, Faculty of Pharmaceutical Sciences, Professor, 薬学部, 教授 (50122255)
Project Period (FY) 1999 – 2001
Keywordsopioid mimetics / pyrazinone derivatives / endomorphine derivatives / diamine derivartives / dimethyltyrosine / μ-opioid receptor agoniat / 鎮痛薬 / 皮下投与
Research Abstract

This project started as International Scientific Research by The Ministry of Education, Culture, Sports, Science and Technology in 1999 and then as Grant-in-Aid for Scientific Research (C) in 2000 and 2001. Therefore, Dr. Lawrence H. Lazarus and Ms. Sharon D. Bryant of National Institute of Environmental Health Sciences, USA were investigators in this project. Dr. Yoshio Okada has been engaged in synthesis of peptides based on the peptide synthesis we made a plan of this project with objective to develop novel type of anti-pain medicine, and obtained following results. 1) We could develop synthetic methodologies ofpeptides. 2) We designed and synthesized endomorphin derivatives and obtained compounds which exhibited potent μ-opioid receptor agonistic activity and δ-opioid receptor antagonistic activity. We designated them as bifunctional opioid mimetics. 3) Employing new method to synthesize pyrazinones from dipeptidyl chloromethyl ketones, novel type opioid memetics containing pyrazinone ring were prepared. 4) Instead of pyrazinone ring, NH_2(CH_2)nNH_2 (n=2-8)were employed to prepare novel types of anti-pain drugs. 5) Compounds obtained above exhibited more potent in vitro and in vivo activity than morphine.6) International conference Annual ' Conference on Opioid Mimetic Analgesics 2002" was successfully held from 17 to 19 of March, 2002 at Awaji Yumebutai International Conference Center and we exchanged our mutual interest concerning the developme t of anti-pain medicines."

  • Research Products

    (11 results)

All Other

All Publications (11 results)

  • [Publications] Yoshio Okada et al.: "Amino Acids and Peptides. LVI. Synthesis of pyrazinone ring-containing opioid mimetics and examination of their opioid receptor binding activity"Tetrahedron. 55. 14391-14406 (1999)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yoshio Okada et al.: "Synthesis of pyrazinone ring-containing opioid mimetics and examination of their opioid receptor binding activity"Chem.Pharm.Bull.. 47. 1193-1195 (1999)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yoshio Okada et al.: "Synthesis of Stereoisomeric Analogues of Endomorphin-2, H-Tyr-Pro-Phe Phe-NH_2, and Examination of Their Opioid Receptor Binding Acitivities"Biocheim.Biophys.Res.Commun.. 276. 7-11 (2000)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yoshio Okada: "Synthesis of Peptides by Solution Methods"Current Organic Chemistry. 5. 1-43 (2001)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yoshio Okada: "Huben-Weyl Methods of Organic Chemistry, Volume E 22a : Synthesis of Peptides and Peptidomimetics"Thieme Stuttgart-New York. 901 (2001)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yoshio Okada, Atsuko Fukumizu, Motohiro Takahashi, Junpei Yamazaki, Toshio Yokoi, Yuko Tsuda, Sharon D.Bryant, Lawrence H.Lazarus: "Amino Acids and Peptides.LVI.Synthesis of pyrazinone ring-containing opioid mimetics and examination of their opioid receptor binding activity"Tetrahedron. 55. 14391-14406 (1999)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshio Okada, Atsuko Fukumizu, Motohiro Takahashi, Junpei Yamazaki, Toshio Yokoi, Yuko Tsuda, Sharon D.Bryant, Lawrence H.Lazarus: "Synthesis of Pyazinone ring-containing Opioid Mimetics and Examination of their Opioid Receptor Bbinding activity"Chem. Pharm. Bull. 47. 1193-1195 (1999)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshio Okada, Atsuko Fukumizu, Motohiro Takahashi, Yoshiro Shimizu, Yuko Tsuda, Toshio Yokoi, Sharon D.Bryant, Lawrence H.Lazarus: "Synthesis of Stereoismeric Analogues of Enfomorphin-2, H-Tyr-Pro-Phe-Phe-NH_2, and Examination of Their Opioid Receptor Binding Activities and Solution Conformation"Biochem. Biophys. Res. Commun. 276. 7-11 (2000)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshio Okada: "Synthesis of Peptides by Solution methods"Current Organic Chemistry. 5. 1-43 (2001)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshio Okada: "Synthesis of Peptides in Solution"Huben-Weyl Methods of Chemistry, Volume E22a : Synthesis of Peptides and Peptidomimetics Thieme Stuttgart-New York. 591-626 (2001)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Tadashi Okamoto, Takashi Matsuya, Takeo Kishi, and Kiyota Goshima: I Experimental Methods of Cultured Cells, 5 Experimental Method of Cultured Cardiac myocytes. Experimental Methods of Cell Biology Hirokawa Publishing Co.. 59-71 (1999)

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 2003-09-17  

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