File S E, Lister R G
Pharmacol Biochem Behav. 1983 Feb;18(2):185-8. doi: 10.1016/0091-3057(83)90361-1.
The effects of three quinoline derivatives, PK 8165 07.5 mg/kg). PK 9084 (7.5 mg/kg) and CGS 8216 (1 and 10 mg/kg), alone and in combination with chlordiazepoxide (5 mg/kg), were investigated in the social interaction test of anxiety. PK 8165 had no effect on social interaction but both PK 8165 and PK 9084 in combination with chlordiazepoxide produced sedation. PK 9084 exhibited a partial anxiolytic profile reflected by a drug x light interaction in the familiar test conditions. CGS 8216 (1 mg/kg) showed no significant effects on social interaction, but did counteract the sedative effect of chlordiazepoxide. The 10 mg/kg dose of CGS 8216 reduced social interaction between pairs of animals in familiar test conditions which is indicative of an anxiogenic effect. These intrinsic anxiogenic properties of CGS 8216 demonstrate that it cannot be considered an inert benzodiazepine antagonist.
在焦虑的社交互动测试中,研究了三种喹啉衍生物PK 8165(07.5毫克/千克)、PK 9084(7.5毫克/千克)和CGS 8216(1毫克/千克和10毫克/千克)单独使用以及与氯氮卓(5毫克/千克)联合使用的效果。PK 8165对社交互动没有影响,但PK 8165和PK 9084与氯氮卓联合使用时会产生镇静作用。在熟悉的测试条件下,PK 9084表现出部分抗焦虑作用,这通过药物与光照的相互作用得以体现。CGS 8216(1毫克/千克)对社交互动没有显著影响,但确实抵消了氯氮卓的镇静作用。CGS 8216的10毫克/千克剂量在熟悉的测试条件下减少了动物对之间的社交互动,这表明具有致焦虑作用。CGS 8216的这些内在致焦虑特性表明它不能被视为一种惰性苯二氮䓬拮抗剂。