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OPC-1085与普萘洛尔对离体豚鼠心房作用的比较研究

A comparative study of the effects of OPC-1085 and propranolol on isolated guinea pig atrium.

作者信息

Imanaga I, Sakamoto Y, Tomita T

出版信息

Jpn J Pharmacol. 1977 Apr;27(2):227-32. doi: 10.1254/jjp.27.227.

Abstract

Effects of a newly synthesized beta-blocker, 5-(3-tert-butylamino-2-hydroxy) propoxy-3,4-dihydrocarbostyril (OPC-1085) were compared with those of propranolol. OPC-1085 had a potency about 3 times greater than that of propranolol in blocking the positive inotropic and chronotropic effects of isoprenaline on the isolated guinea pig atrium. At a concentration of over 3 X 10(-5) M OPC-1085 produced negative inotropic and chronotropic effects. However, these effects were about 10 times weaker than those of propranolol. Suppressing effects on the rate of rise and on the maximum driving frequency of action potentials were also more than 10 times less than those of propranolol. There was almost no change in the action potential of vagus nerve after a 10 min treatment with OPC-1085 (10(-5) M), while the action potential was reduced to 60-70% with propranolol (10(-5) M).

摘要

将一种新合成的β受体阻滞剂5-(3-叔丁基氨基-2-羟基)丙氧基-3,4-二氢卡巴唑(OPC-1085)的作用与普萘洛尔的作用进行了比较。在阻断异丙肾上腺素对离体豚鼠心房的正性肌力和变时作用方面,OPC-1085的效力约为普萘洛尔的3倍。在浓度超过3×10⁻⁵M时,OPC-1085产生负性肌力和变时作用。然而,这些作用比普萘洛尔的作用弱约10倍。对动作电位上升速率和最大驱动频率的抑制作用也比普萘洛尔小10倍以上。用OPC-1085(10⁻⁵M)处理10分钟后,迷走神经动作电位几乎没有变化,而用普萘洛尔(10⁻⁵M)处理后,动作电位降低至60%-70%。

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