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新型β2 选择性拮抗剂 IPS 339 对气管平滑肌和慢收缩骨骼肌的肾上腺素能受体阻断特性。

The adrenoceptor blocking properties of the new beta 2-selective antagonist, IPS 339 on tracheal smooth muscle and on slow contracting skeletal muscle.

作者信息

Holmberg E, Jeppsson A B, Lamm C J, Waldeck B

出版信息

Acta Pharmacol Toxicol (Copenh). 1980 Feb;46(2):150-5. doi: 10.1111/j.1600-0773.1980.tb02435.x.

Abstract

The beta-adrenoceptor blocking properties of IPS 339 and propranolol were studied on isolated preparations of trachea and of the slow-contracting soleus muscle from the guinea-pig. Both compounds antagonized the relaxation of the trachea and the depression of subtetanic contractions of the soleus produced by the beta2-selective agonist, terbutaline. On the soleus muscle the pA2-values for IPS 339 and propranolol were similar and close to those obtained for propranolol on the trachea. However, on the trachea the slope of the Schildplot for IPS 339 against terbutaline became less than one and a reliable pA2-value could not be calculated.

摘要

在豚鼠气管和慢收缩比目鱼肌的离体标本上研究了IPS 339和普萘洛尔的β-肾上腺素受体阻断特性。两种化合物均拮抗了β2选择性激动剂特布他林引起的气管舒张和比目鱼肌不完全强直收缩的抑制。在比目鱼肌上,IPS 339和普萘洛尔的pA2值相似,且与普萘洛尔在气管上获得的值相近。然而,在气管上,IPS 339对特布他林的Schild图斜率小于1,无法计算出可靠的pA2值。

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