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普萘洛尔和美托洛尔对去氧皮质酮处理大鼠的降压效果比较

Comparative antihypertensive effects of propranolol and metoprolol in DOC-treated rats.

作者信息

Wendt R L, Much D R, Bergey J L, Wicks T C

出版信息

Arch Int Pharmacodyn Ther. 1981 Sep;253(1):110-20.

PMID:7325751
Abstract

The effects of chronic twice daily s.c. injections of dlpropranolol, metoprolol and d-propranolol on systolic blood pressure and heart rate were assessed in conscious DOC-saline hypertensive rats. Measurements were taken (tail-cuff) 4 hr after the morning injection and 16-18 hr after the afternoon injection during 11 of 19 consecutive treatment days. Only dl-propranolol and metoprolol at 5 mg/kg lowered blood pressure and heart rate significantly relative to the changes occurring in control saline-injected animals. At the lower dose of 0.2 mg/kg, both agents tended to decrease heart rate while having little or no effect on blood pressure. The overall blood pressure and heart rate changes produced by propranolol at 5 mg/kg differed significantly from those of the control group at both the 4 and 16-18 hr post-dosing intervals. Metoprolol at 5 mg/kg produced significant overall changes in blood pressure and heart rate only at the 4 hr post-doing interval. D-propranolol had no effect on either blood pressure or heart rate. The results indicate tha s.c. propranolol and metoprolol lower systolic blood pressure in conscious DOC-saline hypertensive rats only at the higher dose of 5 mg/kg and that cardioselectivity does not afford increased antihypertensive activity in this model.

摘要

在清醒的地塞米松-生理盐水诱导的高血压大鼠中,评估了每日两次皮下注射dl-普萘洛尔、美托洛尔和d-普萘洛尔对收缩压和心率的影响。在连续19天的治疗中,于11天的上午注射后4小时和下午注射后16 - 18小时(采用尾套法)进行测量。只有5mg/kg的dl-普萘洛尔和美托洛尔相对于注射生理盐水的对照动物的变化,能显著降低血压和心率。在0.2mg/kg的较低剂量下,两种药物都倾向于降低心率,而对血压几乎没有影响或没有影响。5mg/kg的普萘洛尔在给药后4小时和16 - 18小时产生的总体血压和心率变化与对照组均有显著差异。5mg/kg的美托洛尔仅在给药后4小时产生了显著的血压和心率总体变化。d-普萘洛尔对血压和心率均无影响。结果表明,皮下注射普萘洛尔和美托洛尔仅在5mg/kg的较高剂量下能降低清醒的地塞米松-生理盐水诱导的高血压大鼠的收缩压,并且在该模型中,心脏选择性并未带来增强的抗高血压活性。

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