Ischemic stroke together with ischemic heart disease and oncopathology continues to hold leading position among causes of morbidity, mortality and invalidization of population both in Ukraine and in the whole world. Endothelial dysfunction is an early feature of a stroke. That is why knowing of mechanisms that are the basis of its development is very significant. The most important function of endothelium is vasomor tone regulation which is made by means of correlation between vasodilators and vasoconstrictors. During endothelial dysfunction the bioavailability of nitrogen oxide is decreased, thus vasodilatory effect of endothelium is violated. An important change is increasing of products and biological activity – endothelin-1. It performs its influence through activation of specific ETA and ETBreceptors. Effect of endothelin-1 is determined by localization of receptors and correlations between them. The basic action principle of endothelin-1 is increasing of internal cellular concentration of calcium. It causes strong contraction of unstriated muscles as well as coagulants activation.