A NOVEL NONPEPTIDE ENDOTHELIN ANTAGONIST ISOLATED FROM BAYBERRY, MYRICA-CERIFERA

被引：82

作者：

FUJIMOTO, M

MIHARA, S

NAKAJIMA, S

UEDA, M

NAKAMURA, M

SAKURAI, K

机构：

[1] Shionogi Research Laboratories, Shionogi and Co., Fukushima-ku, Osaka, 553

来源：

FEBS LETTERS | 1992年 / 305卷 / 01期

关键词：

ENDOTHELIN ANTAGONIST; MYRICERON CAFFEOYL ESTER; RECEPTOR BINDING; CYTOSOLIC FREE CALCIUM; VASOCONSTRICTION;

D O I：

10.1016/0014-5793(92)80651-V

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A potent non-peptide ET receptor antagonist, myriceron caffeoyl ester (50-235), was isolated from the bayberry, Myrica cerifera. This compound selectively antagonized specific binding of [I-125]ET-1, but not of [I-125]ET-3, to rat cardiac membranes, ET-1-induced increase in the intracellular free calcium concentration in Swiss 3T3 fibroblasts, and ET-1-induced contraction of rat aortic strips. Thus, 50-235 is the first non-peptide ET(A) receptor antagonist. This compound can be useful for studying the physiological role of endothelin and exploring its role in various diseases.

引用

页码：41 / 44

页数：4

共 28 条

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