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首页> 外文期刊>Journal of natural toxins >Tezosentan inhibits both equinatoxin II and endotelin-1 induced contractions of isolated porcine coronary artery in a similar way.
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Tezosentan inhibits both equinatoxin II and endotelin-1 induced contractions of isolated porcine coronary artery in a similar way.

机译:地佐生坦以相似的方式抑制马鞭毛毒素II和内皮素-1诱导的分离的猪冠状动脉的收缩。

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摘要

In the present study we examined the endothelium-dependent mechanism in the constriction of the isolated porcine coronary artery induced by Equinatoxin II (EqT II). EqT II is a polypeptide isolated from the sea anemone (Actinia equina, L.). Contractions induced by endothelin-1 (ET-1) were compared with the contractions induced by EqT II. The force of contraction induced by 100 nM EqT II reached only 30% of the force of contraction induced by 100 nM ET-1. EC50 for ET-1 was 5.14 nM, and for EqT II 101.1 nM. The effects of tezosentan, an endothelin ETA/B receptor antagonist, on contractions induced by either ET-1 or EqT II were compared. Tezosentan inhibited both ET-1 and, to a lesser extent, EqT II-induced contractions of isolated porcine coronary artery. Our present results confirm the involvement of endothelium in the EqT II-induced contractions of coronary arteries. The mode of action of tezosentan upon EqT II-induced contractions indicate that besides its pore-forming effect in the membranes, endothelium, and specifically endothelin-dependent mechanisms, are very important components of the toxin constrictory effects.
机译:在本研究中,我们研究了内皮依赖性机制在由Equinatoxin II(EqT II)诱导的分离的猪冠状动脉收缩中的作用。 EqT II是从海葵(Actinia equina,L.)分离的多肽。将内皮素-1(ET-1)诱导的收缩与EqT II诱导的收缩进行比较。 100 nM EqT II诱导的收缩力仅达到100 nM ET-1诱导的收缩力的30%。 ET-1的EC50为5.14 nM,EqT II的EC50为101.1 nM。比较了内皮素ETA / B受体拮抗剂Tezosentan对ET-1或EqT II诱导的收缩的影响。 Tezosentan抑制ET-1并在较小程度上抑制EqT II诱导的分离的猪冠状动脉收缩。我们目前的结果证实了内皮细胞参与EqT II诱导的冠状动脉收缩。 Tezosentan对EqT II诱导的收缩的作用方式表明,除了其在膜中的成孔作用外,内皮,尤其是内皮素依赖性机制,是毒素收缩作用的重要组成部分。

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