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尼鲁地平(Bay a 7168)对清醒肾性高血压犬的降压作用。

Antihypertensive effect of Niludipine (Bay a 7168) on conscious renal-hypertensive dogs.

作者信息

Hiwatari M, Taira N

出版信息

Arzneimittelforschung. 1979;29(9):1373-6.

PMID:583244
Abstract

In conscious renal-hypertensive dogs (one kidney Grollman type) oral administration of 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid-bis-(2-propoxyethyl)-ester (niludipine, Bay a 7168) (1 and 3 mg/kg) produced a rather prompt fall of blood pressure and an increase in heart rate. With 3 mg/kg p.o. of niludipine a fall of blood pressure was marked at its peak effect attained about 45 min after dosing and lasted about 3 h. Prior administration of propranolol (30 mg/kg p.o.) greatly prevented an increase in heart rate accompanying the fall of blood pressure produced by 3 mg/kg p.o. of niludipine but was of no effect on the antihypertensive action. These results, taken together with previous results indicating niludipine to have a potent coronary vasodilator action, suggest that niludipine will be useful as an antihypertensive drug, especially when hypertension is associated with ischemic heart disease or when the reduction of blood pressure is urgent. Combined use of niludipine with a beta-adrenergic blocking agent is recommended.

摘要

在清醒的肾性高血压犬(单肾Grollman型)中,口服1,4 - 二氢 - 2,6 - 二甲基 - 4 -(3 - 硝基苯基)- 3,5 - 吡啶二羧酸 - 双 -(2 - 丙氧基乙基)酯(尼鲁地平,Bay a 7168)(1和3毫克/千克)可使血压迅速下降并使心率增加。口服3毫克/千克尼鲁地平后,在给药后约45分钟达到峰值效应时血压明显下降,并持续约3小时。预先口服普萘洛尔(30毫克/千克)可极大地预防因口服3毫克/千克尼鲁地平导致的血压下降所伴随的心率增加,但对其降压作用无影响。这些结果与之前表明尼鲁地平具有强大冠状动脉舒张作用的结果相结合,提示尼鲁地平将作为一种降压药物有用,特别是当高血压与缺血性心脏病相关或血压降低紧急时。建议将尼鲁地平与β - 肾上腺素能阻滞剂联合使用。

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