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索他洛尔、氧烯洛尔、普萘洛尔和吲哚洛尔对兔肠平滑肌β-肾上腺素能受体阻断特性的比较。

Comparison of beta-adrenoceptor blocking properties of sotalol, oxprenolol, propranolol and pindolol on rabbit intestinal smooth muscle.

作者信息

Salimi M

出版信息

Pharmacology. 1975;13(5):441-7. doi: 10.1159/000136936.

Abstract

Adrenergic agonists produced a characteristic and definite decrease in the amplitude of spontaneous contractions and tone of the isolated rabbit jejunum. Effect of phenylephrine was abolished either by phenoxybenzamine or phentolamine. Relaxation induced by epinephrine and by norepinephrine was inhibited after combined treatment with phentolamine and propranolol. Phentolamine alone diminished the response to epinephrine and to norepinephrine, but the diminution for epinephrine was greater, indicating that epinephrine has a greater affinity for alpha- than for beta-receptors in the rabbit jejunum. Stimulation of the beta-receptors by isoproterenol was inhibited by propranolol, oxprenolol, sotalol and pindolol, but the block was incomplete. The activity of these four beta-blockers in preventing the inhibitory response to isoproterenol was as follows: inidolol greater than or equal to oxprenolol greater than propranolol greater than sotalol. This demonstrates the fact that not all beta-adrenergic blocking agents possess an identical pharmacologic spectrum of activity. Also it can be suggested that the beta-receptors of jejunum differ in specificity from those of other organs.

摘要

肾上腺素能激动剂使离体兔空肠的自发收缩幅度和张力出现特征性且明确的降低。苯氧苄胺或酚妥拉明可消除去氧肾上腺素的作用。酚妥拉明和普萘洛尔联合处理后,肾上腺素和去甲肾上腺素诱导的舒张作用受到抑制。单独使用酚妥拉明可减弱对肾上腺素和去甲肾上腺素的反应,但对肾上腺素的减弱作用更大,这表明在兔空肠中,肾上腺素对α受体的亲和力比对β受体的亲和力更大。异丙肾上腺素对β受体的刺激作用被普萘洛尔、氧烯洛尔、索他洛尔和吲哚洛尔抑制,但这种阻断并不完全。这四种β受体阻滞剂在预防对异丙肾上腺素的抑制反应方面的活性如下:吲哚洛尔≥氧烯洛尔>普萘洛尔>索他洛尔。这证明了并非所有β肾上腺素能阻滞剂都具有相同的药理活性谱这一事实。也可以认为空肠β受体在特异性上与其他器官的β受体不同。

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