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尼群地平、阿罗洛尔和拉贝洛尔在脊髓麻醉大鼠中诱导的α受体阻滞和血管舒张作用。

Alpha-blockade and vasodilatation induced by nipradilol, arotinolol and labetalol in pithed rats.

作者信息

Nakagawa Y, Nakahara H, Chin W P, Imai S

出版信息

Jpn J Pharmacol. 1985 Dec;39(4):481-5. doi: 10.1254/jjp.39.481.

Abstract

In pithed rats two recently-introduced beta-blockers, nipradilol and arotinolol, as well as labetalol shifted the pressor dose-response curve for phenylephrine to the right. Labetalol and arotinolol did not modify the pressor dose-response curve for clonidine, while nipradilol induced a definite rightward shift. These results indicate that labetalol and arotinolol are selective alpha 1-blockers, while nipradilol is a non-selective one. In addition, all the three beta-blockers produced complex changes in the blood pressure in pithed rats. A fall of the diastolic blood pressure induced by labetalol and nipradilol was preceded by a slight rise, while arotinolol produced a fall at lower doses and a rise at higher ones. The hypotension by labetalol was abolished after propranolol, while the hypertension was suppressed by prazosin, indicating that labetalol has an intrinsic beta- and alpha 1-sympathomimetic effect. The hypertension and the hypotension produced by nipradilol and arotinolol persisted even in the presence of propranolol and prazosin or propranolol and yohimbine.

摘要

在脊髓毁损大鼠中,两种新引入的β受体阻滞剂——尼普地洛和阿罗洛尔,以及拉贝洛尔,均使去氧肾上腺素的升压剂量-反应曲线右移。拉贝洛尔和阿罗洛尔未改变可乐定的升压剂量-反应曲线,而尼普地洛则引起明显的右移。这些结果表明,拉贝洛尔和阿罗洛尔是选择性α1受体阻滞剂,而尼普地洛是非选择性的。此外,所有这三种β受体阻滞剂均使脊髓毁损大鼠的血压产生复杂变化。拉贝洛尔和尼普地洛引起的舒张压下降之前有轻微升高,而阿罗洛尔在较低剂量时引起血压下降,在较高剂量时引起血压升高。拉贝洛尔引起的低血压在给予普萘洛尔后消失,而高血压则被哌唑嗪抑制,这表明拉贝洛尔具有内在的β和α1拟交感神经效应。即使存在普萘洛尔和哌唑嗪或普萘洛尔和育亨宾,尼普地洛和阿罗洛尔引起的高血压和低血压仍然存在。

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