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罗 3-4787,一种新型的β肾上腺素受体阻滞剂:在正常志愿者中的研究。

Ro 3-4787, a new β-adrenoceptor blocking agent: Studies in normal volunteers.

机构信息

Department of Clinical Research, Roche Products Limted, Welwyn Garden City, Hertfordshire.

出版信息

Br J Clin Pharmacol. 1974 Apr;1(2):143-9. doi: 10.1111/j.1365-2125.1974.tb00223.x.

DOI:10.1111/j.1365-2125.1974.tb00223.x
PMID:22454901
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1402459/
Abstract

1 A new β-adrenoceptor blocking agent, Ro 3-4787, was administered orally to resting subjects. Peak levels of 106.2 ± 15.5 ng/ml were reached after 20 mg given in the fasting state. After intravenous administration, an inverse rectilinear relationship was shown between the log dose (2 mg-20 mg) and the heart rate during vigorous exercise on a bicycle ergometer. 2 A double-blind study in five normal subjects using 0.03 mg/kg and 0.15 mg/kg showed that propranolol and Ro 3-4787 were equally effective in reducing the exercise heart rate. There was an inverse correlation between the log plasma level before exercise and the heart rate during exercise for both drugs over the range studied.

摘要
  1. 一种新的β-肾上腺素受体阻滞剂,Ro 3-4787,在空腹状态下口服给予休息的受试者。在给予 20mg 后,达到 106.2±15.5ng/ml 的峰值水平。静脉给药后,在自行车测力计上剧烈运动期间,剂量(2mg-20mg)的对数与心率呈反直线关系。

  2. 在五名正常受试者中进行的一项双盲研究,使用 0.03mg/kg 和 0.15mg/kg 表明,普萘洛尔和 Ro 3-4787 在降低运动心率方面同样有效。在研究范围内,两种药物在运动前的对数血浆水平与运动期间的心率之间存在反比关系。

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Ro 3-4787, a new β-adrenoceptor blocking agent: Studies in normal volunteers.罗 3-4787,一种新型的β肾上腺素受体阻滞剂:在正常志愿者中的研究。
Br J Clin Pharmacol. 1974 Apr;1(2):143-9. doi: 10.1111/j.1365-2125.1974.tb00223.x.
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Beta-adrenoceptor blocking effects and plasma levels of bornaprolol and propranolol in man.人体内博纳洛尔和普萘洛尔的β-肾上腺素能受体阻断作用及血浆水平
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Eur J Clin Pharmacol. 1982;23(3):189-95. doi: 10.1007/BF00547552.
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Peripheral vascular effects of bufuralol in hypertensive and normal subjects: a comparison with propranolol and pindolol.布呋洛尔对高血压患者和正常人的外周血管作用:与普萘洛尔和吲哚洛尔的比较
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本文引用的文献

1
Control of heart rate by the autonomic nervous system. Studies in man on the interrelation between baroreceptor mechanisms and exercise.自主神经系统对心率的控制。关于人体压力感受器机制与运动之间相互关系的研究。
Circ Res. 1966 Aug;19(2):400-11. doi: 10.1161/01.res.19.2.400.
2
Plasma propranolol levels in adults with observations in four children.成人血浆普萘洛尔水平及对四名儿童的观察结果
Clin Pharmacol Ther. 1970 Jan-Feb;11(1):112-20. doi: 10.1002/cpt1970111112.
3
The effects of a new beta-adrenoceptive receptor blocking drug on heart rate in man.一种新型β-肾上腺素能受体阻断药对人体心率的影响。
Br J Pharmacol Chemother. 1968 Mar;32(3):663-70. doi: 10.1111/j.1476-5381.1968.tb00465.x.
4
Comparison of some properties of pronethalol and propranolol.丙萘洛尔和普萘洛尔某些性质的比较。
Br J Pharmacol Chemother. 1965 Dec;25(3):577-91. doi: 10.1111/j.1476-5381.1965.tb01782.x.
5
Comparison of propranolol and Ro 3-3528 in hyperthyroid tachycardia and dysrhythmias.普萘洛尔与Ro 3-3528治疗甲状腺功能亢进性心动过速和心律失常的比较。
Postgrad Med J. 1973 Jan;49(567):18-23. doi: 10.1136/pgmj.49.567.18.