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苯二氮䓬拮抗剂的致焦虑作用。

The anxiogenic action of benzodiazepine antagonists.

作者信息

File S E, Lister R G, Nutt D J

出版信息

Neuropharmacology. 1982 Oct;21(10):1033-7. doi: 10.1016/0028-3908(82)90118-6.

DOI:10.1016/0028-3908(82)90118-6
PMID:6815546
Abstract

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.

摘要

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。

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1
The anxiogenic action of benzodiazepine antagonists.苯二氮䓬拮抗剂的致焦虑作用。
Neuropharmacology. 1982 Oct;21(10):1033-7. doi: 10.1016/0028-3908(82)90118-6.
2
Anxiogenic and non-anxiogenic benzodiazepine antagonists.致焦虑和非致焦虑的苯二氮䓬拮抗剂。
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3
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4
Blockade of the diazepam-induced increase in rat striatal acetylcholine content by the specific benzodiazepine antagonists ethyl-beta-carboline-3-carboxylate and Ro 15-1788.
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A three-state model of the benzodiazepine receptor explains the interactions between the benzodiazepine antagonist Ro 15-1788, benzodiazepine tranquilizers, beta-carbolines, and phenobarbitone.苯二氮䓬受体的三态模型解释了苯二氮䓬拮抗剂Ro 15 - 1788、苯二氮䓬类镇静剂、β-咔啉和苯巴比妥之间的相互作用。
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The benzodiazepine antagonist Ro 15-1788 reverses the effect of methyl-beta-carboline-3-carboxylate but not of harmaline on cerebellar cGMP and motor performance in mice.苯二氮䓬拮抗剂Ro 15 - 1788可逆转甲基-β-咔啉-3-羧酸酯对小鼠小脑环磷酸鸟苷和运动能力的影响,但不能逆转哈马灵的影响。
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Eur J Pharmacol. 1982 Nov 5;85(1):93-7. doi: 10.1016/0014-2999(82)90428-9.

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