File S E, Lister R G, Nutt D J
Neuropharmacology. 1982 Oct;21(10):1033-7. doi: 10.1016/0028-3908(82)90118-6.
Two benzodiazepine antagonists were tested in an animal model of anxiety, the social interaction test. Ethyl beta-carboline-3-carboxylate (1 and 2 mg/kg) had a potent anxiogenic action; the imidazodiazepine RO 15-1788 (4-10 mg/kg) had a weak anxiogenic effect that with a larger dose (20 mg/kg) disappeared and RO 15-1788 (10 mg/kg) significantly counteracted the anxiogenic effect of the beta-carboline (1 mg/kg). The implications of these results for the understanding of the pharmacological basis of anxiety and for the existence and nature of an endogenous ligand for the benzodiazepine binding site are discussed.
在焦虑动物模型社交互动试验中对两种苯二氮䓬拮抗剂进行了测试。β-咔啉-3-羧酸乙酯(1和2毫克/千克)具有强效致焦虑作用;咪唑二氮䓬RO 15 - 1788(4 - 10毫克/千克)有微弱致焦虑效应,大剂量(20毫克/千克)时此效应消失,且RO 15 - 1788(10毫克/千克)能显著对抗β-咔啉(1毫克/千克)的致焦虑效应。讨论了这些结果对于理解焦虑药理学基础以及苯二氮䓬结合位点内源性配体的存在和性质的意义。