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美喹他嗪(LM - 209)的药理学研究。(IV)。一般药理学作用(作者译)

[Pharmacological study of mequitazine (LM-209). (IV). General pharmacological action (author's transl)].

作者信息

Hojo M, Yoshida Y, Nagasaka Y, Katayama O, Serizawa I

出版信息

Nihon Yakurigaku Zasshi. 1981 Nov;78(5):403-29. doi: 10.1254/fpj.78.403.

Abstract

The general pharmacological actions of LM-209 were studied in rats, cats, dogs, guinea pigs and mice and the findings were compared with data on clemastine fumarate (CL). LM-209 but not CL produced a slight increase in pulse pressure and tachycardia. Inhibitory effects of LM-209 against contraction of the vas deferens and nictitating membrane, mainly dominated by sympathetic innervation, were remarkably less potent than CL. Inhibitory effects of LM-209 in the gastrointestinal tract were slightly more potent than CL. LM-209 accelerated norepinephrine-induced pressor reaction, while CL inhibited these effects at the dose level inhibiting histamine-induced depressor reaction. At the oral dose level showing anti-histaminic and anti-allergic actions, LM-209 but not CL had slight anti-tussive action, in an experimental model. Local anesthetic action of LM-209 was slightly more potent than that of lidocaine. LM-209 showed the same properties and potencies as CL, in most of the general pharmacological experiments.

摘要

在大鼠、猫、狗、豚鼠和小鼠身上研究了LM - 209的一般药理作用,并将研究结果与富马酸氯马斯汀(CL)的数据进行了比较。LM - 209而非CL会使脉压略有升高并导致心动过速。LM - 209对主要由交感神经支配的输精管和瞬膜收缩的抑制作用明显弱于CL。LM - 209在胃肠道的抑制作用略强于CL。LM - 209加速了去甲肾上腺素引起的升压反应,而CL在抑制组胺引起的降压反应的剂量水平下抑制了这些作用。在显示抗组胺和抗过敏作用的口服剂量水平下,在实验模型中,LM - 209而非CL具有轻微的镇咳作用。LM - 209的局部麻醉作用略强于利多卡因。在大多数一般药理实验中,LM - 209表现出与CL相同的性质和效力。

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