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奥昔福林对交感神经系统活性的影响(作者译)

[Effects of oxilofrine on the activity of the sympathetic nervous system (author's transl)].

作者信息

Rapin J R, Jacquot C

出版信息

Arzneimittelforschung. 1980;30(7):1077-9.

PMID:6106499
Abstract

The effects of 1-(4-hydroxyphenyl)-2-methylamin-propanol- (1) (oxilofrine, 4-HMP) on the catecholamine metabolism were investigated in vitro in isolated rat hearts and spleen sections. Investigations were conducted in vivo to determine the influence exerted by the sympathomimetic agent on the noradrenaline biosynthesis in the heart and on the oxygen-dependent enzymes tyrosine hy droxylase and dopamine-beta-hydroxylase. Oxilofrine is an excellent inhibitor of the noradrenaline storage in the heart (DI = 1.5 X 10(-6) mol/l). At the same time, the sympathomimetic agent releases noradrenaline from the storage compartments. In this process, preferably newly synthetised noradrenaline is released both from the heart and from the spleen. This double mechanism of action is associated with an acceleration of the noradrenaline biosynthesis and an increase in enzymal activity of tyrosine hydroxylase and dopamine-beta-hydroxylase. The transmitter concentrations in the region of the postsynaptic receptors are enhanced by oxilofrine.

摘要

在离体大鼠心脏和脾脏切片中对1-(4-羟苯基)-2-甲氨基丙醇-(1)(奥昔福林,4-HMP)对儿茶酚胺代谢的影响进行了体外研究。进行了体内研究以确定拟交感神经药对心脏中去甲肾上腺素生物合成以及对氧依赖性酶酪氨酸羟化酶和多巴胺-β-羟化酶的影响。奥昔福林是心脏中去甲肾上腺素储存的优良抑制剂(抑制常数=1.5×10⁻⁶mol/L)。同时,拟交感神经药从储存区释放去甲肾上腺素。在此过程中,优选新合成的去甲肾上腺素从心脏和脾脏中释放出来。这种双重作用机制与去甲肾上腺素生物合成的加速以及酪氨酸羟化酶和多巴胺-β-羟化酶的酶活性增加有关。奥昔福林可提高突触后受体区域的递质浓度。

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