Hara Y, Sugimoto S, Ono H
Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd., Osaka, Japan.
Nihon Yakurigaku Zasshi. 1993 Aug;102(2):141-51. doi: 10.1254/fpj.102.141.
The effect of arotinolol on the incomplete tetanic contractions of the cat soleus muscle was studied. Isoproterenol and epinephrine injected intravenously decreased the tension and degree of fusion of incomplete tetanic contractions of the soleus muscle in anesthetized cats. Intravenous arotinolol (> 3 micrograms/kg), propranolol (> 30 micrograms/kg) and pindolol (> 3 micrograms/kg) blocked the effects of isoproterenol and epinephrine, but atenolol (-300 micrograms/kg), prazosin (0.1-10 micrograms/kg) and phentolamine (10, 30 micrograms/kg) did not block them. These results indicate that the receptors involved can be classified as of the beta 2-type. It is proposed that arotinolol may inhibit beta 2-adrenoceptors in the extrafusal muscle fibers of slow muscle, and thereby reduces the amplitude of tremor by changing the incomplete tetanic contractions of the muscle to the complete ones.
研究了阿罗洛尔对猫比目鱼肌不完全强直收缩的影响。静脉注射异丙肾上腺素和肾上腺素可降低麻醉猫比目鱼肌不完全强直收缩的张力和融合程度。静脉注射阿罗洛尔(>3微克/千克)、普萘洛尔(>30微克/千克)和吲哚洛尔(>3微克/千克)可阻断异丙肾上腺素和肾上腺素的作用,但阿替洛尔(-300微克/千克)、哌唑嗪(0.1 - 10微克/千克)和酚妥拉明(10、30微克/千克)则不能阻断。这些结果表明,所涉及的受体可归类为β2型。有人提出,阿罗洛尔可能抑制慢肌肌外肌纤维中的β2肾上腺素能受体,从而通过将肌肉的不完全强直收缩转变为完全强直收缩来降低震颤幅度。