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尼立替林:高血压大鼠中的一种强效抗高血压药物。

Nylidrin: a potent anti-hypertensive agent in hypertensive rats.

作者信息

Yen T T, Pearson D V

出版信息

Res Commun Chem Pathol Pharmacol. 1979 Jan;23(1):11-28.

PMID:441505
Abstract

Nylidrin HCl lowered the blood pressure and increased the heart rate of conscious, spontaneously hypertensive rats (SHR), Goldblatt hypertensive rats, and DOCA hypertensive rates. In SHR, the minimum effective dose was 0.5 mg/kg, s.c. At that dose, the anti-hypertensive activity of nylidrin lasted more than 3 hours. Propranolol reversed both effects on blood pressure and heart rate by nylidrin, whereas atenolol, a specific cardiac beta 1 blocker, only blocked or reversed the tachycardia caused by nylidrin but did not block the anti-hypertensive effect of the compound. In normotensive rats of Wistar/Kyoto strain (WKY) and Holtzman strain, nylidrin at 5 or 10 mg/kg, s.c., produced a transient hypotensive effect which lasted less than an hour and tachycardia that persisted for several hours. In WKY, atenolol prolonged the hypotensive activity of the compound by partially reversing the tachycardia. These observations indicate that SHR is more sensitive than WKY to the anti-hypertensive activity of nylidrin, which is probably caused by vasodilatation mediated by beta 2 receptors.

摘要

盐酸尼立替林降低清醒的自发性高血压大鼠(SHR)、戈德布拉特高血压大鼠和去氧皮质酮高血压大鼠的血压并增加其心率。在SHR中,最小有效剂量为0.5mg/kg,皮下注射。在该剂量下,尼立替林的抗高血压活性持续超过3小时。普萘洛尔可逆转尼立替林对血压和心率的两种作用,而阿替洛尔,一种特异性心脏β1受体阻滞剂,仅阻断或逆转尼立替林引起的心动过速,但不阻断该化合物的抗高血压作用。在Wistar/Kyoto品系(WKY)和霍尔兹曼品系的正常血压大鼠中,皮下注射5或10mg/kg的尼立替林产生短暂的降压作用,持续时间不到1小时,心动过速持续数小时。在WKY中,阿替洛尔通过部分逆转心动过速延长了该化合物的降压活性。这些观察结果表明,SHR对尼立替林的抗高血压活性比WKY更敏感,这可能是由β2受体介导的血管舒张引起的。

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Nylidrin: a potent anti-hypertensive agent in hypertensive rats.
Res Commun Chem Pathol Pharmacol. 1979 Jan;23(1):11-28.
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