从玫瑰链霉菌79089中分离得到的高选择性新型内皮素转化酶抑制剂WS79089B的生物学和药理学特性
Biological and pharmacological properties of highly selective new endothelin converting enzyme inhibitor WS79089B isolated from Streptosporangium roseum No. 79089.
作者信息
Tsurumi Y, Fujie K, Nishikawa M, Kiyoto S, Okuhara M
机构信息
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
出版信息
J Antibiot (Tokyo). 1995 Feb;48(2):169-74. doi: 10.7164/antibiotics.48.169.
WS79089B a highly specific endothelin converting enzyme (ECE) inhibitor has been isolated from the fermentation broth of Streptosporangium roseum No. 79089. WS79089B showed highly selective ECE inhibition activity with IC50 value of 0.14 microM and behaved as a competitive inhibitor of ECE, with Ki values of 8.9 x 10(-8) M. The sodium salt of WS79089B (FR901533) inhibited big endothelin-1 (big ET-1) induced pressor effect in a dose dependent manner when administered to male Sprague-Dawley rats intravenously dosed 2 minutes prior to big ET-1 challenge.
WS79089B是一种高度特异性的内皮素转化酶（ECE）抑制剂，它是从玫瑰链霉菌79089号菌株的发酵液中分离得到的。WS79089B表现出高度选择性的ECE抑制活性，IC50值为0.14微摩尔，并且作为ECE的竞争性抑制剂，Ki值为8.9×10⁻⁸ M。当在给雄性Sprague-Dawley大鼠静脉注射WS79089B的钠盐（FR901533）2分钟后再注射大内皮素-1（big ET-1）进行攻击时，它能以剂量依赖的方式抑制big ET-1诱导的升压作用。
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