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.
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页码：41 / 44
页数：4
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