Ikeda S, Tamaoki H, Akahane M, Nebashi Y
Jpn J Pharmacol. 1984 Jul;35(3):319-26. doi: 10.1254/jjp.35.319.
Ritodrine hydrochloride (ritodrine) is a beta 2-adrenoceptor stimulant which has been effectively prescribed for the prevention of premature labor. The present studies were carried out to investigate the effects of ritodrine on uterine motility in rats and rabbits during gestation, as compared with those of isoproterenol and isoxsuprine. The results were as follows: 1) Spontaneous movements and evoked contractile responses of isolated rat uterus (19-20th days of gestation) were suppressed by 10(-9) - 10(-6) M ritodrine. The potency of ritodrine was approximately 10 times more than that of isoxsuprine and 100 - 1,000 times less than that of isoproterenol. 2) When these drugs were administered to pregnant rats or rabbits intravenously, the tocolytic potency was in the following order: isoproterenol greater than ritodrine greater than isoxsuprine. 3) Ritodrine induced hypotension and tachycardia, but these effects were less than those of isoproterenol and isoxsuprine. 4) The effects of isoproterenol and ritodrine were almost prevented by pretreatment with propranolol, but those of isoxsuprine were only partially or not affected. These results suggest that ritodrine is effective in preventing the uterine contractions in rats and rabbits and that it has less effect on the circulatory system than isoproterenol and isoxsuprine. It is also concluded that ritodrine produces these effects through activation of beta-adrenoceptors.
盐酸利托君(利托君)是一种β2肾上腺素能受体激动剂,已被有效地用于预防早产。本研究旨在探讨利托君与异丙肾上腺素和异克舒令相比,对妊娠大鼠和家兔子宫运动的影响。结果如下:1)10(-9)-10(-6)M的利托君可抑制离体大鼠子宫(妊娠19 - 20天)的自发运动和诱发的收缩反应。利托君的效力约为异克舒令的10倍,比异丙肾上腺素低100 - 1000倍。2)当将这些药物静脉注射给妊娠大鼠或家兔时,其保胎效力顺序如下:异丙肾上腺素>利托君>异克舒令。3)利托君可引起低血压和心动过速,但这些作用比异丙肾上腺素和异克舒令小。4)普萘洛尔预处理几乎可完全阻断异丙肾上腺素和利托君的作用,但只能部分阻断或不影响异克舒令的作用。这些结果表明,利托君在预防大鼠和家兔子宫收缩方面有效,且对循环系统的影响比异丙肾上腺素和异克舒令小。还得出结论,利托君通过激活β肾上腺素能受体产生这些作用。