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[甲磺酸[对(6-胍基己酰氧基)苯甲酸乙酯](FOY)的药理作用]

[Pharmacological action of [ethyl p(6-guanidinohexanoyloxy)benzoate] methanesulfonate (FOY)].

作者信息

Okegawa T, Aishita H, Akimoto A, Makita T, Nakai H

出版信息

Nihon Yakurigaku Zasshi. 1975 Jan;71(1):71-87.

PMID:239887
Abstract

General pharmacological effects of [Ethyl p-(6-guanidinohexanoyloxy)benzoate] methanesulfonate (FOY), a new antiproteolytic agent, were studied and the following results were obtained. Acute administration of large doses of FOY in conscious dogs and rabbits caused a decrease in spontaneous motility, ataxia, cyanosis, collapse, mydriasis, and respiratory paralysis. The agent had no effect on the central nervous system and exhibited hypotensive effects in dogs in doses of more than 1 mg/kg. Hypotensive responses were not inhibited by treatment with atropine or hexamethonium. FOY had no effects on ECG in the rabbit at doses of less than 30 mg/kg and at doses from 10(-6) to 10(-4)g/ml, distinctly reduced the amplitude of the spontaneous and rhythmic contractions of the isolated rabbit ileum, guinea-pig ileum and rat uterus preparation. The contractile response to nerve stimulation, noradrenaline and barium was suppressed in isolated guinea-pig vas deferens. FOY had no effects on the twitch response of gastrocnemius muscle to sciatic nerve stimulation in rats. The drug caused local irritant effects in rabbits and rats.

摘要

对新型抗蛋白水解剂甲磺酸盐对-(6-胍基己酰氧基)苯甲酸乙酯的一般药理作用进行了研究,获得了以下结果。给清醒的狗和兔子急性大剂量给药FOY会导致自发运动减少、共济失调、发绀、虚脱、瞳孔散大及呼吸麻痹。该药物对中枢神经系统无影响,且在狗体内剂量超过1mg/kg时表现出降压作用。阿托品或六甲铵处理不能抑制降压反应。在兔子体内剂量小于30mg/kg时,FOY对心电图无影响;在剂量为10(-6)至10(-4)g/ml时,FOY可明显降低离体兔回肠、豚鼠回肠和大鼠子宫标本的自发节律性收缩幅度。在离体豚鼠输精管中,对神经刺激、去甲肾上腺素和钡的收缩反应受到抑制。FOY对大鼠腓肠肌对坐骨神经刺激的抽搐反应无影响。该药物在兔子和大鼠中引起局部刺激作用。

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