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Calcium ions are essential to contract smooth muscle cells in blood vessels. They enter these cells through voltage-dependent calcium channels, specifically L-type calcium channels in the cell membrane. These L-type calcium channels are integral to the excitation-contraction coupling process in smooth muscle. When a stimulus is received by smooth muscle cells, their membrane depolarizes. This alteration in membrane potential instigates the opening of L-type calcium channels. As a result,...
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Vasodilators, primarily affecting the smooth muscles within arterial and venous walls, are commonly used for hypertension treatment. Medications such as minoxidil and hydralazine primarily target arteries and arterioles, while sodium nitroprusside acts on arterioles and venules. Minoxidil, functioning as a prodrug, is metabolized by hepatic sulfotransferase into its active form, minoxidil sulfate, after oral administration. This metabolite binds to the sulfonylurea receptor (SUR) component of...
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The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
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拉洛西芬通过一种依赖于雌激素受体和依赖于氧化的机制在体外急性放松子冠状动脉.

G A Figtree1, Y Lu, C M Webb

  • 1Cardiac Medicine, National Heart and Lung Institute, Imperial College School of Medicine, London, UK.

Circulation
|September 8, 1999
PubMed
概括
此摘要是机器生成的。

选择性雌激素受体调节剂 (SERMs),如拉洛西芬,通过一种依赖雌激素受体的途径放松冠状动脉,涉及雄性和雌性子中的氧化.

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科学领域:

  • 心血管药理学心血管药理学
  • 内分泌学 在内分泌学.
  • 血管生物学 血管生物学

背景情况:

  • 选择性雌激素受体调节剂 (SERM) 呈现组织特异性的雌激素效应.
  • SERM在骨和脂质上提供雌激素的好处,而不会增加癌症风险.
  • 雌激素的血管保护作用已知,但SERM对冠状动脉的影响尚不清楚.

研究的目的:

  • 为了研究 SERM raloxifene 对隔离的子冠状动脉的影响.
  • 为了确定拉洛西芬是否与雌激素类似地影响冠状动脉血管.
  • 阐明拉洛西芬对冠状动脉的作用机制.

主要方法:

  • 隔离的子冠状动脉环被用于器官浴.
  • 测量了同度张力以评估放松.
  • 研究了涉及内皮,雌激素受体,氧化和对抗性的机制.

主要成果:

  • 拉洛西芬在雄性和雌性子冠状动脉中诱导了依赖内皮和依赖雌激素受体的放松.
  • 氧化和对冠状动脉肌细胞的直接抗作用参与了拉洛西芬的作用.
  • 拉洛西芬通过内皮产生了比雌激素显著更大的放松作用.

结论:

  • 拉洛西芬在冠状动脉中表现出显著的血管放松特性.
  • 在雄性和雌性子中观察到通过内皮通过拉洛西芬的雌激素受体依赖放松.
  • 拉洛西芬的血管作用超越了传统的雌激素通路.