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盐酸利托君(一种β2 -肾上腺素能受体激动剂)的药理学研究。

Pharmacological investigation of ritodrine hydrochloride, a beta 2-adrenoceptor stimulant.

作者信息

Ikeda S, Tamaoki H

出版信息

Jpn J Pharmacol. 1984 Dec;36(4):477-84. doi: 10.1254/jjp.36.477.

Abstract

Ritodrine hydrochloride (ritodrine) has been effectively prescribed for the prevention of premature labor. The present study was carried out to investigate the mode of action of ritodrine on the uterus and heart in comparison with those of isoxsuprine and isoproterenol. 1) Ritodrine (10(-8)-10(-6) M) suppressed the spontaneous motility of pregnant rat uterus and showed positive chronotropic action at the doses of 10(-6)-10(-4) M in guinea-pig atria. 2) In the Ca2+-free, K+-rich Tyrode solution, ritodrine suppressed the Ca2+ induced contracture of pregnant rat uterus, while it potentiated the carbachol induced contraction. 3) Ritodrine increased the amount of cyclic AMP in the uterus but not in heart. This action of ritodrine was suppressed by pretreatment with propranolol (10(-6) M). 4) These results suggest that ritodrine causes actions through activation of cyclic AMP production, as in the case of isoproterenol, and it acts more selectively on beta 2-adrenoceptors than on beta 1-adrenoceptors.

摘要

盐酸利托君(利托君)已被有效地用于预防早产。本研究旨在比较利托君与异克舒令和异丙肾上腺素相比,对子宫和心脏的作用方式。1)利托君(10⁻⁸ - 10⁻⁶M)抑制妊娠大鼠子宫的自发运动,并在豚鼠心房中,在10⁻⁶ - 10⁻⁴M剂量下显示出正性变时作用。2)在无钙、富钾的台氏液中,利托君抑制妊娠大鼠子宫的钙诱导挛缩,而增强卡巴胆碱诱导的收缩。3)利托君增加子宫中环磷酸腺苷(cAMP)的量,但不增加心脏中的量。利托君的这一作用被普萘洛尔(10⁻⁶M)预处理所抑制。4)这些结果表明,利托君与异丙肾上腺素一样,通过激活环磷酸腺苷的产生而发挥作用,并且它对β₂肾上腺素能受体的作用比对β₁肾上腺素能受体的作用更具选择性。

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