Cardiac and vascular actions of sarafotoxin S6b and endothelin-1.
Cardiac and vascular actions of sarafotoxin S6b and endothelin-1.
复制标题
sarafotoxin S6b 和内皮素-1 的心脏和血管作用。
DOI：
10.1016/0024-3205(90)90064-x
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发表时间：
1990
期刊：
影响因子：
6.1
通讯作者：
Westfall,TC
中科院分区：
文献类型：
--
作者：
Han,SP;Knuepfer,MM;Trapani,AJ;Fok,KF;Westfall,TC
蛇毒来源的 sarafotoxin S6B (SRT) 和猪内皮来源的内皮素-1 (ET) 具有惊人的结构相似性。在意识清醒、自由活动的大鼠中，ET（0.67 nmol/kg）产生短暂性心动过速和动脉血压下降，随后动脉压长期升高、心动过缓、心输出量（CO）减少和总外周阻力显着增加。相比之下，SRT（0.67 nmol/kg）仅产生持续的心血管反应。 SRT 或 ET 的持续心血管效应同样可以被硝苯地平减弱。 SRT 和 ET (30 nM) 在分离的灌注肠系膜血管床中产生血管收缩，但没有初始血管舒张。 SRT 和 ET 对离体灌注心脏具有有效的正性肌力和负性变时作用，并诱发毒性反应，包括冠状血管痉挛、心律失常、房室传导阻滞和心室颤动。除了 SRT 缺乏体内初始抑制反应外，还观察到肽活性的一些差异。 ET 在所有 3 种制剂中产生升压和血管收缩反应方面比 SRT 产生更大、更持久的作用，并且能够对心脏产生毒性作用。
Snake venom-derived sarafotoxin S6B (SRT) and porcine endothelium-derived endothelin-1 (ET) have striking structural similarities. In conscious, freely-moving rats, ET (0.67 nmol/kg) produced a transient tachycardia and fall in arterial blood pressure which was followed by a long-lasting increase in arterial pressure, bradycardia, decrease in cardiac output (CO) and marked increase in total peripheral resistance. In contrast, SRT (0.67 nmol/kg) produced only the sustained cardiovascular responses. The sustained cardiovascular effects of SRT or ET were similarly attenuated by nifedipine. SRT and ET (30 nM) produced vasoconstriction in the isolated perfused mesenteric vascular bed without initial vasodilation. SRT and ET had potent positive inotropic and negative chronotropic effects on isolated perfused hearts and induced toxic reactions including coronary vasospasm, arrhythmias, AV block and ventricular fibrillation. In addition to SRT lacking the initial depressor response in vivo, several differences in the activities of the peptides were also observed. ET produced greater and longer-lasting actions than SRT in producing pressor and vasoconstrictor responses in all 3 preparations, and in its ability to induce toxic effects on the heart.