从传统抗抑郁药抑制 GABA-A 受体介导的突触传递到 α5-GABA-A 受体的负变构调节剂作为潜在的快速作用抗抑郁药物：闭环？
From Inhibition of GABA-A Receptor-Mediated Synaptic Transmission by Conventional Antidepressants to Negative Allosteric Modulators of Alpha5- GABA-A Receptors as Putative Fast-Acting Antidepressant Drugs: Closing the Circle?
机构信息
Department of Psychiatry & Forensic Medicine, Institute of Neurosciences, Autonomous University of Barcelona, 08193-Bellaterra, Barcelona, Spain.
出版信息
Curr Neuropharmacol. 2022;20(1):85-89. doi: 10.2174/1570159X19666211104144650.
Abstract
The present perspective paper shortly and specifically addresses the issues of whether inhibition of GABA-A receptor-mediated synaptic transmission may be involved in antidepressantlike actions and the therapeutic effects of conventional antidepressant (AD) drugs, and whether the recent development of negative allosteric modulators (NAMs) of the alpha5-GABA-A receptor may constitute significant progress in our knowledge on the neurobiology and the treatment of depression.
摘要
本文简要而具体地探讨了 GABA-A 受体介导的突触传递抑制是否可能参与抗抑郁作用和传统抗抑郁药 (AD) 的治疗效果，以及最近开发的 α5-GABA-A 受体负变构调节剂 (NAM) 是否可能代表我们在抑郁症神经生物学和治疗方面的知识取得了重大进展。
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From Inhibition of GABA-A Receptor-Mediated Synaptic Transmission by Conventional Antidepressants to Negative Allosteric Modulators of Alpha5- GABA-A Receptors as Putative Fast-Acting Antidepressant Drugs: Closing the Circle?从传统抗抑郁药抑制 GABA-A 受体介导的突触传递到 α5-GABA-A 受体的负变构调节剂作为潜在的快速作用抗抑郁药物：闭环？
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Convergent Mechanisms Underlying Rapid Antidepressant Action.快速抗抑郁作用的潜在汇聚机制。
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GABA receptor: Positive and negative allosteric modulators.GABA 受体：正变构调节剂和负变构调节剂。
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Negative allosteric modulation of alpha 5-containing GABA receptors engenders antidepressant-like effects and selectively prevents age-associated hyperactivity in tau-depositing mice.负变构调节含 alpha5 型 GABA 受体产生抗抑郁样作用，并选择性预防tau 沉积小鼠与年龄相关的过度活跃。
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Selective Pharmacological Augmentation of Hippocampal Activity Produces a Sustained Antidepressant-Like Response without Abuse-Related or Psychotomimetic Effects.海马体活动的选择性药理学增强产生持续的抗抑郁样反应，且无滥用相关或拟精神病效应。
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