Timmermans P B, Fluitman P H, Mackaay J C, van Zwieten P A
Arch Int Pharmacodyn Ther. 1978 Jan;231(1):98-103.
The effects of the classical alpha-sympathomimetic drugs naphazoline, tramazoline, xylometazoline, tetryzoline and oxymetazoline on blood pressure and heart rate of pentobarbitone-anaesthetized (75 mg/kg; i.p.) normotensive rats were studied following intravenous injections. With the aid of this experimental animal model a dose dependent decrease in mean arterial pressure and heart rate could be established for these agents, oxymetazoline excepted, for which only the bradycardia could be quantified. It is suggested that central alpha-adrenoceptors are involved in the mechanism of this cardiovascular inhibition in view of the most specific alpha-adrenoceptor-stimulating properties of these ddrugs. Additionally, the results indicate that the use of pentobarbitone as the anaesthetic enhances the hypotensive action of these agents, so that their pronounced peripheral vasopressive response can be overcome.
研究了经典α-拟交感神经药物萘甲唑啉、曲马唑啉、赛洛唑啉、丁苄唑啉和羟甲唑啉静脉注射后对戊巴比妥钠麻醉(75mg/kg;腹腔注射)的正常血压大鼠血压和心率的影响。借助该实验动物模型,除羟甲唑啉外,这些药物均可使平均动脉压和心率呈剂量依赖性降低,而羟甲唑啉仅能定量其引起的心动过缓。鉴于这些药物具有最特异的α-肾上腺素能受体刺激特性,提示中枢α-肾上腺素能受体参与了这种心血管抑制机制。此外,结果表明,使用戊巴比妥钠作为麻醉剂可增强这些药物的降压作用,从而克服其明显的外周血管收缩反应。