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Effect of an imidazobenzodiazepine, Ro15-4513, on the incoordination and hypothermia produced by ethanol and pentobarbital.

作者信息

Hoffman P L, Tabakoff B, Szabó G, Suzdak P D, Paul S M

出版信息

Life Sci. 1987 Aug 3;41(5):611-9. doi: 10.1016/0024-3205(87)90415-2.

DOI:10.1016/0024-3205(87)90415-2
PMID:3600196
Abstract

The imidazobenzodiazepine, Ro15-4513, which is a partial inverse agonist at brain benzodiazepine receptors, reversed the incoordinating effect of ethanol in mice, as measured on an accelerating Rotarod. This effect was blocked by benzodiazepine receptor antagonists. In contrast, Ro15-4513 had no effect on ethanol-induced hypothermia in mice. However, Ro15-4513 reversed the hypothermic effect of pentobarbital, and, at a higher dose, also reversed the incoordinating effect of pentobarbital in mice. The data support the hypothesis that certain of the pharmacological effects of ethanol are mediated by actions at the GABA-benzodiazepine receptor-coupled chloride channel.

摘要

相似文献

1
Effect of an imidazobenzodiazepine, Ro15-4513, on the incoordination and hypothermia produced by ethanol and pentobarbital.
Life Sci. 1987 Aug 3;41(5):611-9. doi: 10.1016/0024-3205(87)90415-2.
2
Ro15-4513 differentially affects ethanol-induced hypnosis and hypothermia.Ro15 - 4513对乙醇诱导的催眠和体温过低有不同影响。
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3
Effects of the imidazobenzodiazepine RO15-4513 on the stimulant and depressant actions of ethanol on spontaneous locomotor activity.咪唑并苯二氮䓬RO15 - 4513对乙醇对自发运动活性的兴奋和抑制作用的影响。
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4
A selective imidazobenzodiazepine antagonist of ethanol in the rat.
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Interactions between benzodiazepine antagonists, inverse agonists, and acute behavioral effects of ethanol in mice.
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RO15-4513 but not FG-7142 reverses anticonvulsant effects of ethanol against bicuculline- and picrotoxin-induced convulsions in rats.
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7
Antagonism of the ethanol-like discriminative stimulus effects of ethanol, pentobarbital, and midazolam in cynomolgus monkeys reveals involvement of specific GABA(A) receptor subtypes.食蟹猴中乙醇、戊巴比妥和咪达唑仑类似乙醇的辨别性刺激效应的拮抗作用揭示了特定GABA(A)受体亚型的参与。
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8
Molecular interactions of ethanol with GABAergic system and potential of RO15-4513 as an ethanol antagonist.乙醇与γ-氨基丁酸能系统的分子相互作用以及RO15-4513作为乙醇拮抗剂的潜力。
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Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-induced intoxication in the rat.
J Pharmacol Exp Ther. 1988 Jun;245(3):880-6.
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引用本文的文献

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Potentiation of Gamma Aminobutyric Acid Receptors (GABAAR) by Ethanol: How Are Inhibitory Receptors Affected?乙醇对γ-氨基丁酸受体(GABAAR)的增强作用:抑制性受体是如何受到影响的?
Front Cell Neurosci. 2016 May 6;10:114. doi: 10.3389/fncel.2016.00114. eCollection 2016.
2
α4-Containing GABA(A) Receptors are Required for Antagonism of Ethanol-Induced Motor Incoordination and Hypnosis by the Imidazobenzodiazepine Ro15-4513.α4 包含 GABA(A) 受体是咪唑并苯并二氮䓬类药物 Ro15-4513 拮抗乙醇诱导的运动不协调和催眠所必需的。
Front Pharmacol. 2011 Apr 4;2:18. doi: 10.3389/fphar.2011.00018. eCollection 2011.
3
GABAA receptors in the posterior, but not anterior, ventral tegmental area mediate Ro15-4513-induced attenuation of binge-like ethanol consumption in C57BL/6J female mice.
后腹侧被盖区而非前腹侧被盖区的 GABAA 受体介导 Ro15-4513 减轻 C57BL/6J 雌性小鼠 binge 样乙醇消耗。
Behav Brain Res. 2011 Jun 20;220(1):230-7. doi: 10.1016/j.bbr.2011.02.014. Epub 2011 Feb 12.
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Attenuation of the stimulant response to ethanol is associated with enhanced ataxia for a GABA, but not a GABA, receptor agonist.对乙醇的刺激反应减弱与共济失调增强有关,这是针对一种γ-氨基丁酸(GABA)受体激动剂而言,而非另一种GABA受体激动剂。
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Zolpidem generalization and antagonism in male and female cynomolgus monkeys trained to discriminate 1.0 or 2.0 g/kg ethanol.在经过训练以辨别1.0或2.0克/千克乙醇的雄性和雌性食蟹猴中进行唑吡坦的泛化和拮抗作用研究。
Alcohol Clin Exp Res. 2008 Jul;32(7):1197-206. doi: 10.1111/j.1530-0277.2008.00674.x.
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Physiology and pharmacology of alcohol: the imidazobenzodiazepine alcohol antagonist site on subtypes of GABAA receptors as an opportunity for drug development?酒精的生理学与药理学:GABAA受体亚型上的咪唑并苯二氮䓬类酒精拮抗剂位点——药物研发的契机?
Br J Pharmacol. 2008 May;154(2):288-98. doi: 10.1038/bjp.2008.32. Epub 2008 Feb 18.
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Tonic for what ails us? high-affinity GABAA receptors and alcohol.什么能治愈我们的病痛?高亲和力GABAA受体与酒精。
Alcohol. 2007 May;41(3):139-43. doi: 10.1016/j.alcohol.2007.03.008. Epub 2007 May 23.
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Low dose acute alcohol effects on GABA A receptor subtypes.低剂量急性酒精对GABA A受体亚型的影响。
Pharmacol Ther. 2006 Nov;112(2):513-28. doi: 10.1016/j.pharmthera.2006.05.004. Epub 2006 Jul 11.
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Low-dose alcohol actions on alpha4beta3delta GABAA receptors are reversed by the behavioral alcohol antagonist Ro15-4513.低剂量酒精对α4β3δ GABAA受体的作用可被行为性酒精拮抗剂Ro15 - 4513逆转。
Proc Natl Acad Sci U S A. 2006 May 30;103(22):8540-5. doi: 10.1073/pnas.0600194103. Epub 2006 May 12.
10
Ro 15-4513 selectively attenuates ethanol, but not sucrose, reinforced responding in a concurrent access procedure; comparison to other drugs.在同时获取程序中,Ro 15 - 4513选择性地减弱乙醇强化的反应,但不减弱蔗糖强化的反应;与其他药物的比较。
Psychopharmacology (Berl). 1995 Sep;121(2):192-203. doi: 10.1007/BF02245630.