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SCH 58261对喹啉酸在纹状体切片和海马体切片中诱导产生的效应有不同影响。

SCH 58261 differentially influences quinolinic acid-induced effects in striatal and in hippocampal slices.

作者信息

Tebano Maria Teresa, Domenici Maria Rosaria, Popoli Patrizia

机构信息

Department of Pharmacology, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy.

出版信息

Eur J Pharmacol. 2002 Aug 30;450(3):253-7. doi: 10.1016/s0014-2999(02)02148-9.

DOI:10.1016/s0014-2999(02)02148-9
PMID:12208317
Abstract

The influence of the adenosine A(2A) receptor antagonist SCH 58261 (7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4-trizolo[1,5-c] pyrimidine) (50, 200 nM, 1 microM) on quinolinic acid effects has been studied in rat striatal and hippocampal slices. Quinolinic acid induced disappearance of field potentials at concentrations of 500 microM and 2 mM in hippocampal and corticostriatal slices, respectively. We found that 1 microM SCH 58261 prevented quinolinic acid-induced field potential disappearance in corticostriatal but not in hippocampal slices. This finding demonstrates that the peculiar binding profile of SCH 58261 and the predominance in the hippocampus of "atypical" adenosine A(2A) receptor population (not recognized by SCH 58261) could have a functional relevance in the occurrence of region-specific neuroprotective effects.

摘要

在大鼠纹状体和海马切片中,研究了腺苷A(2A)受体拮抗剂SCH 58261(7-(2-苯乙基)-5-氨基-2-(2-呋喃基)-吡唑并-[4,3-e]-1,2,4-三唑并[1,5-c]嘧啶)(50、200 nM、1 microM)对喹啉酸作用的影响。喹啉酸分别在海马切片和皮质纹状体切片中浓度为500 microM和2 mM时诱导场电位消失。我们发现,1 microM的SCH 58261可防止喹啉酸诱导皮质纹状体切片中场电位消失,但不能防止海马切片中的场电位消失。这一发现表明,SCH 58261独特的结合特性以及海马中“非典型”腺苷A(2A)受体群体(不被SCH 58261识别)的优势可能与区域特异性神经保护作用的发生具有功能相关性。

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SCH 58261 differentially influences quinolinic acid-induced effects in striatal and in hippocampal slices.SCH 58261对喹啉酸在纹状体切片和海马体切片中诱导产生的效应有不同影响。
Eur J Pharmacol. 2002 Aug 30;450(3):253-7. doi: 10.1016/s0014-2999(02)02148-9.
2
Blockade of striatal adenosine A2A receptor reduces, through a presynaptic mechanism, quinolinic acid-induced excitotoxicity: possible relevance to neuroprotective interventions in neurodegenerative diseases of the striatum.纹状体腺苷A2A受体的阻断通过一种突触前机制减轻喹啉酸诱导的兴奋性毒性:可能与纹状体神经退行性疾病的神经保护干预有关。
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Adenosine A2A receptor blockade differentially influences excitotoxic mechanisms at pre- and postsynaptic sites in the rat striatum.腺苷A2A受体阻断对大鼠纹状体突触前和突触后位点的兴奋毒性机制有不同影响。
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Adenosine A(2A) antagonism increases striatal glutamate outflow in the quinolinic acid rat model of Huntington's disease.在喹啉酸诱导的亨廷顿病大鼠模型中,腺苷A(2A)拮抗剂可增加纹状体谷氨酸外流。
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SCH 58261 (an adenosine A(2A) receptor antagonist) reduces, only at low doses, K(+)-evoked glutamate release in the striatum.SCH 58261(一种腺苷A(2A)受体拮抗剂)仅在低剂量时可减少纹状体中钾离子诱发的谷氨酸释放。
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Transducing system operated by adenosine A(2A) receptors to facilitate acetylcholine release in the rat hippocampus.由腺苷A(2A)受体操纵的转导系统促进大鼠海马体中乙酰胆碱的释放。
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Effect of A2A adenosine receptor stimulation and antagonism on synaptic depression induced by in vitro ischaemia in rat hippocampal slices.A2A 腺苷受体激动和拮抗对大鼠海马切片体外缺血诱导的突触抑制的影响。
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The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist.非黄嘌呤类杂环化合物SCH 58261是一种新型强效选择性A2a腺苷受体拮抗剂。
J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.
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Different synaptic and subsynaptic localization of adenosine A2A receptors in the hippocampus and striatum of the rat.大鼠海马体和纹状体中腺苷A2A受体的不同突触及亚突触定位。
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