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[洛普拉明的药理特性]

[Pharmacological properties of lopramine].

作者信息

Akashi A, Hashizume T, Tanaka M, Naka S, Suzuki I

出版信息

Nihon Yakurigaku Zasshi. 1976 May;72(4):417-31.

PMID:987974
Abstract

Pharmacological properties of LOP were compared with those of imipramine(IMP). LOP had little or no effect on electroconvulsive shock and chemoconvulsions in mice, conditioned avoidance response in rats, pain threshold in mice and rats and body temperature in rabbits. LOP, unlike IMP, showed relatively weak effects on general behavior in mice, spontaneous EEG in cats and spontaneous motor activity in mice. LOP prevented oxotremorine-induced hypothermia but not tremor, while IMP antagonized both the responses in mice. In anesthetized dogs, LOP caused a respiratory stimulation and a fall in blood pressure, left ventribular pressure and left ventricular dp/dt without a noticeable effect on heart rate. LOP was less potent than IMP in the depressor and cardiodepressing effects, antispasmogenic activity and in antagonizing the depressor response to acetylcholine. LOP, like IMP, potentiated pressor response to norepinephrine and reduced that to tyramine in anesthetized dogs, but neither antidepressant produced norepinephrine potentiation in isolated guinea-pig vas deferens. Both drugs inhibited spontaneous motility of the jejunum without reducing the gastric motility in anesthetized dogs. These results indicate that, compared with IMP, LOP is characterized by weak general pharmacological activities.

摘要

将洛匹那韦(LOP)的药理特性与丙咪嗪(IMP)进行了比较。洛匹那韦对小鼠的电惊厥休克和化学惊厥、大鼠的条件回避反应、小鼠和大鼠的痛阈以及家兔的体温几乎没有影响或没有影响。与丙咪嗪不同,洛匹那韦对小鼠的一般行为、猫的自发脑电图和小鼠的自发运动活动的影响相对较弱。洛匹那韦可预防氧化震颤素引起的体温过低,但不能预防震颤,而丙咪嗪可拮抗小鼠的这两种反应。在麻醉犬中,洛匹那韦引起呼吸刺激、血压下降、左心室压力和左心室dp/dt下降,对心率无明显影响。在降压、心脏抑制作用、抗痉挛活性以及拮抗对乙酰胆碱的降压反应方面,洛匹那韦的效力低于丙咪嗪。与丙咪嗪一样,洛匹那韦可增强麻醉犬对去甲肾上腺素的升压反应,并降低对酪胺的升压反应,但两种抗抑郁药在离体豚鼠输精管中均未产生去甲肾上腺素增强作用。两种药物均抑制麻醉犬空肠的自发运动,但不降低胃的运动。这些结果表明,与丙咪嗪相比,洛匹那韦的特点是一般药理活性较弱。

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