BRL 34915, a novel antihypertensive agent: comparison of effects on blood pressure and other haemodynamic parameters with those of nifedipine in animal models.
BRL 34915, a novel antihypertensive agent: comparison of effects on blood pressure and other haemodynamic parameters with those of nifedipine in animal models.
复制标题
BRL 34915，一种新型抗高血压药：在动物模型中比较硝苯地平对血压和其他血液动力学参数的影响。
DOI：
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发表时间：
1986
影响因子：
3
通讯作者：
R. Poyser
中科院分区：
文献类型：
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作者：
R. Buckingham;J. Clapham;T. C. Hamilton;S. Longman;J. Norton;R. Poyser
以硝苯地平为对照，研究了BRL 34915(+/-)6-cyano-3，4-dihydro-2，2-dimethyl-trans-4-(2-oxo-1-pyrrolidyl)-2H-b enzo[b]-pyran-3-ol对动物血压和其他血流动力学参数的影响。在清醒的自发性高血压大鼠和肾性高血压的猫和狗中，BRL-34915的口服降压剂量比硝苯地平的剂量低10-30倍。BRL 34915诱发的心动过速往往比硝苯地平在猫身上引起的心动过速要少，在狗身上引起的心动过速的程度也差不多。在这些模型中，对BRL 34915的降压反应在每日重复给药一次时是可重复的，在停止给药时没有反跳性高血压。在使用电磁流量探头测量麻醉猫局部血流量的研究中，与硝苯地平不同的是，静脉注射BRL 34915可显著增加肾脏血流量，但BRL 34915缺乏硝苯地平对股动脉血流量的显著影响。BRL 34915是一种结构上与现有心血管药物无关的化合物，是一种有效的新抗高血压药物，具有有趣的活性特征，使该化合物具有临床意义。
The effects of BRL 34915, (+/-) 6-cyano-3,4-dihydro-2,2-dimethyl-trans-4-(2-oxo-1-pyrrolidyl)-2H-b enzo [b]-pyran-3-ol, on blood pressure and other haemodynamic parameters in animals have been investigated in comparison with those of nifedipine. In conscious spontaneously hypertensive rats and renal hypertensive cats and dogs the oral doses of BRL 34915 lowering blood pressure are 10 to 30 times lower than those of nifedipine. Tachycardia evoked by BRL 34915 tends to be less than that produced by nifedipine in the cat and of similar magnitude in the dog. The antihypertensive response to BRL 34915 in these models is reproducible on repeat once daily dosing without rebound hypertension on cessation of dosing. In studies using electromagnetic flow probes to measure regional blood flow in anaesthetised cats the intravenous administration of BRL 34915, unlike that of nifedipine, markedly increases renal blood flow yet BRL 34915 lacks the marked effect of nifedipine on femoral blood flow. BRL 34915, a compound structurally unrelated to existing cardiovascular drugs, is a potent new antihypertensive agent having an interesting profile of activity that renders this compound of clinical interest.