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Sedative effects of PK 9084 and PK 8165 alone and in combination with chlordiazepoxide.

机译:单独使用PK 9084和PK 8165并与氯二氮卓合用时具有镇静作用。

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摘要

1 The sedative effects in rats of two phenylquinolines, PK 9084 and PK 8165 (5-50 mg/kg), were examined in a holeboard: both when given alone and when given in conjunction with chlordiazepoxide (5 mg/kg). 2 Both phenylquinolines produced significant dose-related decreases in locomotor activity and rearing, with an ED50 about twice that for chlordiazepoxide. 3 When the phenylquinolines were combined with chlordiazepoxide the degree of sedation was equal to that seen with either drug given alone, whichever produced the greater sedation; the sedative effects of the two drugs were never additive. 4 PK 9084 (10 and 50 mg kg) significantly reduced rectal temperature, as did chlordiazepoxide (5 mg/kg), but there was no addition nor interaction of their effects. 5 Both phenylquinolines also reduced exploratory head-dipping, as did chlordiazepoxide, but in combination they antagonized each other's effects. 6 The classification of the phenylquinolines as non-sedative anxiolytics, acting as agonists at the benzodiazepine receptors needs revision.
机译:1在孔板中检查了两种苯基喹啉PK 9084和PK 8165(5-50 mg / kg)对大鼠的镇静作用:单独使用或与氯二氮卓(5 mg / kg)一起使用时。 2两种苯基喹啉在运动能力和饲养方面均引起剂量相关的显着降低,ED50约为氯二氮卓的两倍。 3当苯喹啉与氯氮卓合用时,镇静程度等于单独使用两种药物时镇静程度,两者以镇静作用较大者为准。两种药物的镇静作用从未加和。 4 PK 9084(10和50 mg kg)可以显着降低直肠温度,而氯二氮杂卓(5 mg / kg)则可以降低直肠温度,但是它们之间没有添加作用,也没有相互作用。 5两种苯喹啉都与三氯二氮杂酚一样,也减少了探索性的头浸,但两者合用时却相互拮抗。 6苯喹啉类作为非镇静性抗焦虑药的分类,在苯二氮杂pine受体上起激动剂的作用,需要修改。

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