ENDOTHELIN ANTAGONIST

内皮素是一种有效的血管活性肽， 以前描述的内皮细胞衍生的收缩因子涉及 在调节血管张力方面。 虽然内皮素具有 在体外具有有效的血管收缩活性，其在体内的作用似乎 要复杂。 在全身和肾血管床血管舒张似乎 这是最初的效果。 在肺和血管肠系膜 循环区域内皮素导致阻力增加， 血管收缩 内皮素也刺激平滑的生长 肌肉细胞 内皮素拮抗剂将用于表征 其受体相互作用和生理效应。 类比将是 合成并测试内皮素对血管内皮细胞的抑制作用， 电导 一种可能的治疗动脉粥样硬化，高血压， 以及因此可能发展成急性损伤和休克状况。

Endothelin, a potent vasoactive peptide, has just been discovered as the formerly described endothelial cell-derived contracting factor involved in the regulation of vascular tone. Although endothelin possesses potent vasoconstricter activity in vitro, its actions in vivo appear to be complex. In the systemic and renal vascular beds vasodilation seems to be the initial effect. In the pulmonary and vascular mesenteric circulatory regions endothelin causes an increase in resistance due to vasoconstriction. Endothelin also stimulates the growth of smooth muscle cells. An antagonist of endothelin will serve to characterize its receptor interaction and physiological effects. Analogues will be synthesized and tested for inhibition of endothelin actions on vascular conductance. A possible therapeutic for atherosclerosis, hypertension, as well as acute conditions of jury and shock may thus be developed.