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阿替洛尔、美托洛尔和普萘洛尔对麻醉猫β-肾上腺素能受体的阻断作用。

Beta-adrenoceptor blockade by atenolol, metoprolol and propranolol in the anaesthetized cat.

作者信息

Lundgren B, Carlsson E, Herrmann I

出版信息

Eur J Pharmacol. 1979 May 1;55(3):263-8. doi: 10.1016/0014-2999(79)90193-6.

Abstract

The inhibitory effects of atenolol, metoprolol and propranolol on isoprenaline-induced tachycardia, broncho-relaxation and vasodilatation were investigated in the reserpinized and anaesthetized cat. In low doses all three antagonists inhibited the heart rate response to isoprenaline, the order of potency being propranolol greater than metoprolol greater than atenolol. While propranolol inhibited the bronchodilation and vasodilation responses to isoprenaline in the same dose range as it blocked the heart rate response, atenolol and metoprolol had to be given in considerably higher doses to block these effects. The results indicate that both metoprolol and atenolol, in contrast to propranolol, are selective beta1-adrenoceptor antagonist. No statistically significant difference in the degree of selectivity was found between metoprolol and atenolol. The three compounds were devoid of intrinsic beta-mimetic activity.

摘要

在经利血平处理并麻醉的猫身上,研究了阿替洛尔、美托洛尔和普萘洛尔对异丙肾上腺素诱发的心动过速、支气管舒张和血管舒张的抑制作用。低剂量时,所有三种拮抗剂均抑制对异丙肾上腺素的心率反应,效力顺序为普萘洛尔大于美托洛尔大于阿替洛尔。普萘洛尔在阻断心率反应的相同剂量范围内抑制对异丙肾上腺素的支气管舒张和血管舒张反应,而阿替洛尔和美托洛尔必须给予相当高的剂量才能阻断这些效应。结果表明,与普萘洛尔不同,美托洛尔和阿替洛尔都是选择性β1肾上腺素能受体拮抗剂。美托洛尔和阿替洛尔之间在选择性程度上未发现统计学上的显著差异。这三种化合物均无内在拟β活性。

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