El-Tahir K E, Al-Khamees H A, Bayomi S M
Department of Pharmacology, King Saud University, Riyadh, Saudi Arabia.
Boll Chim Farm. 1995 Dec;134(11):604-8.
The cardiovascular effects of a series of 2-substituted- 1,2,4-triazolo[1,5-a]-pyrimidine derivatives (compounds 1-6) were examined in anaesthetized rats. Of these compounds only compounds 3 and 4 in dose of (15-60 mumole/Kg) induced dose-dependent decreases in the arterial blood pressure and heart rate. The induced cardiovascular changes were not antagonised by histaminergic, cholinergic, serotoninergic receptor blockers, prostaglandin synthesis inhibitors or Cacl2. Treatment of the animals with the compounds (20-30 mumole/Kg) competitively antagonised noradrenaline-induced increase in the arterial blood pressure and significantly antagonised isoprenaline-induced tachycardia but not the induced hypotension. The compounds seemed to possess both alpha 1- and, beta 1-adrenoceptor blocking activities.
在麻醉大鼠中检测了一系列2-取代-1,2,4-三唑并[1,5-a]嘧啶衍生物(化合物1-6)的心血管效应。在这些化合物中,只有化合物3和4在剂量为(15-60微摩尔/千克)时可引起动脉血压和心率的剂量依赖性降低。组胺能、胆碱能、5-羟色胺能受体阻滞剂、前列腺素合成抑制剂或氯化钙均不能拮抗所诱导的心血管变化。用这些化合物(20-30微摩尔/千克)处理动物可竞争性拮抗去甲肾上腺素诱导的动脉血压升高,并显著拮抗异丙肾上腺素诱导的心动过速,但不能拮抗所诱导的低血压。这些化合物似乎同时具有α1和β1肾上腺素能受体阻断活性。