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Behavioural pharmacology of the α5-GABA receptor antagonist S44819: Enhancement and remediation of cognitive performance in preclinical models.α5- GABA 受体拮抗剂 S44819 的行为药理学：在临床前模型中增强和改善认知表现。
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Effects of the Selective α5-GABAAR Antagonist S44819 on Excitability in the Human Brain: A TMS-EMG and TMS-EEG Phase I Study.选择性α5-γ-氨基丁酸A型受体拮抗剂S44819对人脑兴奋性的影响：一项经颅磁刺激-肌电图和经颅磁刺激-脑电图的I期研究。
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AMPA receptor antagonist, YM90K, reduces infarct volume in thrombotic distal middle cerebral artery occlusion in spontaneously hypertensive rats.AMPA受体拮抗剂YM90K可减少自发性高血压大鼠血栓性大脑中动脉远端闭塞后的梗死体积。
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Delayed treatment with YM90K, an AMPA receptor antagonist, protects against ischaemic damage after middle cerebral artery occlusion in rats.
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本文引用的文献

1
Postacute Delivery of GABA α5 Antagonist Promotes Postischemic Neurological Recovery and Peri-infarct Brain Remodeling.GABAα5 拮抗剂急性后给药促进缺血后神经功能恢复和梗死周边脑重塑。
Stroke. 2018 Oct;49(10):2495-2503. doi: 10.1161/STROKEAHA.118.021378.
2
Selective inhibition of extra-synaptic α5-GABA receptors by S44819, a new therapeutic agent.选择性抑制突触外 α5-GABA 受体的 S44819，一种新的治疗药物。
Neuropharmacology. 2017 Oct;125:353-364. doi: 10.1016/j.neuropharm.2017.08.012. Epub 2017 Aug 12.
3
Behavioural pharmacology of the α5-GABA receptor antagonist S44819: Enhancement and remediation of cognitive performance in preclinical models.α5- GABA 受体拮抗剂 S44819 的行为药理学：在临床前模型中增强和改善认知表现。
Neuropharmacology. 2017 Oct;125:30-38. doi: 10.1016/j.neuropharm.2017.07.005. Epub 2017 Jul 8.
4
Effects of the Selective α5-GABAAR Antagonist S44819 on Excitability in the Human Brain: A TMS-EMG and TMS-EEG Phase I Study.选择性α5-γ-氨基丁酸A型受体拮抗剂S44819对人脑兴奋性的影响：一项经颅磁刺激-肌电图和经颅磁刺激-脑电图的I期研究。
J Neurosci. 2016 Dec 7;36(49):12312-12320. doi: 10.1523/JNEUROSCI.1689-16.2016.
5
Neural Stem Cell Transplantation Induces Stroke Recovery by Upregulating Glutamate Transporter GLT-1 in Astrocytes.神经干细胞移植通过上调星形胶质细胞中的谷氨酸转运体GLT-1诱导中风恢复。
J Neurosci. 2016 Oct 12;36(41):10529-10544. doi: 10.1523/JNEUROSCI.1643-16.2016.
6
The effects of delayed reduction of tonic inhibition on ischemic lesion and sensorimotor function.强直抑制延迟减轻对缺血性损伤和感觉运动功能的影响。
J Cereb Blood Flow Metab. 2015 Oct;35(10):1601-9. doi: 10.1038/jcbfm.2015.86. Epub 2015 May 13.
7
Promoting brain remodelling and plasticity for stroke recovery: therapeutic promise and potential pitfalls of clinical translation.促进脑重塑和可塑性以实现中风康复：临床转化的治疗前景和潜在陷阱。
Lancet Neurol. 2012 Apr;11(4):369-80. doi: 10.1016/S1474-4422(12)70039-X. Epub 2012 Mar 19.
8
Functional regulation of GABAA receptors in nervous system pathologies.神经系统疾病中 GABA A 受体的功能调节。
Curr Opin Neurobiol. 2012 Jun;22(3):552-8. doi: 10.1016/j.conb.2011.10.007. Epub 2011 Oct 28.
9
Post-acute delivery of erythropoietin induces stroke recovery by promoting perilesional tissue remodelling and contralesional pyramidal tract plasticity.促红细胞生成素在急性后期的递送通过促进病灶周围组织重塑和对侧锥体束可塑性来诱导中风恢复。
Brain. 2011 Jan;134(Pt 1):84-99. doi: 10.1093/brain/awq344.
10
Reducing excessive GABA-mediated tonic inhibition promotes functional recovery after stroke.降低过度的 GABA 介导的紧张性抑制可促进中风后的功能恢复。
Nature. 2010 Nov 11;468(7321):305-9. doi: 10.1038/nature09511. Epub 2010 Nov 3.

Preclinical concepts and results with the GABA antagonist S44819 in a mouse model of middle cerebral artery occlusion.

作者信息

Hermann Dirk M, Saba Barbara, Sors Aurore, Bassetti Claudio L

机构信息

Departments of Neurology, University Hospital Essen, Essen, Germany.

Institut de Recherches Internationales Servier, Suresnes, France.

出版信息

Neural Regen Res. 2019 Sep;14(9):1517-1518. doi: 10.4103/1673-5374.255963.

DOI:10.4103/1673-5374.255963
PMID:31089046
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6557109/
Abstract
摘要