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系统性内甲素受体阻塞降低了人类的外周血管抵抗和血压
W G Haynes1, C J Ferro, K P O'Kane
1Department of Medicine, University of Edinburgh, Western General Hospital, UK.
Circulation
|May 15, 1996
概括
内甲素受体对抗剂TAK-044在健康男性中引起血管扩张和低血压. 这表明内甲蛋白-1对于维持血管度和血压至关重要.
科学领域:
- 心血管药理学心血管药理学
- 人体生理学 人体生理学
背景情况:
- 局部内甲素-1抑制会导致血管扩张,但人类的系统性影响尚不清楚.
- 研究了内甲素受体阻塞对全身心血管系统的影响.
研究的目的:
- 为了评估TAK-044的心血管作用,一个强大的内甲素ETA/B受体对手,在健康的男性中.
主要方法:
- 进行了两项随机的,安慰剂控制的交叉研究.
- 在不同剂量 (10-1000毫克) 中静脉注射TAK-044并测量心血管参数.
- 评估前臂血管收缩反应对内衣林-1和TAK-044输液.
主要成果:
- TAK-044引起了剂量依赖的外周血管扩张和低血压.
- 观察到平均动脉压和总周围阻力的显著下降.
- 心率升高,心脏指数升高,以及血内甲蛋白度升高.
结论:
- TAK-044降低了外周血管阻力和血压,增加了循环内甲蛋白.
- 阻止前臂血管收缩到外源性内甲蛋白-1,表明内源性内甲蛋白-1在血管度中的作用.
- 内甲素受体对抗剂作为血管扩张剂具有潜在的治疗价值.
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