ENDOTHELIN ANTAGONIST

内皮素拮抗剂

• 批准号: 3501653
• 负责人: MARTHA KNIGHT
• 金额: $ 5万
• 依托单位: PEPTIDE TECHNOLOGIES CORPORATION
• 依托单位国家: 美国
• 财政年份: 1989
• 资助国家: 美国
• 起止时间: 1989-09-01 至 1990-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3501653
• 关键词: blood flow measurement; cardiovascular pharmacology; cats; drug design /synthesis /production; growth factor; inhibitor /antagonist; protein biosynthesis; protein sequence; protein structure function; vasoconstriction; vasodilation

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.

内皮素，一种有效的血管活性多肽，刚刚被发现是一种 先前描述的内皮细胞衍生收缩因子涉及 在调节血管张力方面。尽管内皮素拥有 在体外具有强大的血管收缩活性，在体内的作用似乎 要复杂一点。在全身和肾脏血管床上，血管扩张似乎 才是最初的效果。在肺和血管肠系膜 循环区内皮素引起的阻力增加是由于 血管收缩。内皮素还能刺激生长顺畅 肌肉细胞。一种内皮素的拮抗剂将用于表征 其受体相互作用和生理效应。类似物将是 内皮素的合成及其对血管作用的抑制试验 电导。一种可能治疗动脉粥样硬化，高血压， 以及严重的损伤和休克情况也可能因此而发展。