1996 Fiscal Year Final Research Report Summary
Development of selective agonists and antagonists of the endothelin receptors
| Project/Area Number |
06556050
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| Research Category |
Grant-in-Aid for Scientific Research (A)
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| Allocation Type | Single-year Grants |
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| Section | 試験 |
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| Research Field |
Basic veterinary science/Basic zootechnical science
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| Research Institution | THE UNIVERSITY OF TOKYO |
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Principal Investigator |
KARAKI Hideaki The University of Tokyo, Graduate School of Agricultural and Life Sciences, Faculty of Agriculture, Professor, 大学院・農学生命科学研究科, 教授 (60011912)
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| Co-Investigator(Kenkyū-buntansha) |
OKADA Toshikazu Ciba Geigy Japan Ltd., International Research Laboratory, Chief Investigator, 国際科学研究所, 研究員
MATSUDA Yuzuru Kyowa Hakko Kogyo Company, Tokyo research Institute, Chief Investigator, 東京研究所, 研究員
TSUBONE Hirokazu The University of Tokyo, Graduate School of Agricultural and Life Sciences, Facu, 大学院・農学生命科学研究科, 助教授 (30142095)
SUGANO Shigeru The University of Tokyo, Graduate School of Agricultural and Life Sciences, Facu, 大学院・農学生命科学研究科, 教授 (70111482)
OZAKI Hiroshi The University of Tokyo, Graduate School of Agricultural and Life Sciences, Facu, 大学院・農学生命科学研究科, 助教授 (30134505)
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| Project Period (FY) |
1994 – 1996
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| Keywords | Endothelin / Endothelin receptor / Endothelin receptor antagonists / IRL 1620 / RES-701-1 |
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| Research Abstract |
Endothelin (ET) is a potent vasoconstrictor peptide derived from vascular endothelium and other tissues. There are two types of ET receptors, the ETA and the ETB receptors. Because ET has various effects on isolated tissues at very low concentrations, and many tissues produce ET,it is expected that ET has variety of effects in out body. However, physiological and pathophysiological roles of ET have not been identified mainly because we do not have selective agonists and antagonists of these ET reseptors. The major purpose of our project was to find out such agonists and antagonists. We found that a selective agonist of the ETB receptor, IRL 1620, from the C-terminal peptides of ET-1. IRL 1620 is more selective than other ETB agonists and is more easily labeled by I125. We also found a selective ETB antagonist, RES-701-1 from bacterial products. This antagonist showed different characteristics from other ETB antagonist, BQ788, indicating the presence of the ETB receptor subtypes.
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Research Products
(8 results)
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[Publications] SUDJARWO,S.A., HORI,M., TANAKA,T., MATSUDA,Y., OKADA,T.AND KARAKI,H.: "Subtypes of Endothelin ET_A and ET_B receptors mediating venous smooth muscle contraction" Biochem. Biophys. Res. Commun.200. 627-633 (1994)
Description
「研究成果報告書概要(欧文)」より
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[Publications] KARAKI,H., SUDJARWO,S.A., HORI,M., TANAKA,T., AND MATSUDA,Y.: "Effects of endothelin ET_B receptor antagonist, RES-101-1, on isolated blood vessel and small intestine" Eur. J.Pharmacol.262. 255-259 (1994)
Description
「研究成果報告書概要(欧文)」より
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[Publications] JAMES,A.F., URADE,Y., WEBB,R.L., KARAKI,H., UMEMURA,I., FUJITANI,Y., ODA,K., OKADA,T., LAPPE,R.W.AND TAKAI,M.: "IRL 1620, succinyl-[Glu^9, Ala^<11,15>]-endothelin-1 (8-21), a highly specific agonist of the ET_B receptor" Cardiovasc. Drug Rev.11. 253-270 (1993)
Description
「研究成果報告書概要(欧文)」より
