中枢给药AMPA拮抗剂增加帕金森大鼠的运动。

B Stauch Slusher, K C Rissolo, K F Anzilotti, P F Jackson
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引用次数: 13

摘要

本研究发现了3种α -氨基-3-羟基-5-甲基异恶唑-4-丙酸(AMPA)谷氨酸受体拮抗剂,包括2,3-二羟基-6-硝基-7-磺胺酰基苯并(f)喹啉(NBQX)、1-(4-氨基苯基)-4-甲基-7,8-亚甲二氧基- 5h -2,3-苯二氮卓(GYKI 52466)和6-(1H-咪唑-1-基)-7-硝基-2,3-(1H, 4H)-喹啉二酮(YM90K)。给药于双侧黑质致密部损伤的帕金森大鼠髓内核,可明显逆转运动能力。这些数据表明中枢活性AMPA拮抗剂可能在治疗特发性帕金森病中具有治疗效用。
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Centrally-administered AMPA antagonists increase locomotion in parkinsonian rats.

It was shown in the present study that three antagonists of the alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) glutamate receptor, including 2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(f)quinoxaline (NBQX), 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine (GYKI 52466) and 6-(1H-imidazole-1-yl)-7-nitro-2,3-(1H, 4H)-quinoxalinedione (YM90K), caused marked reversal of akinesia when administered into the entopeduncular nucleus of rats rendered parkinsonian by bilateral substantia nigra pars compacta lesion. These data suggest that centrally active AMPA antagonists may have therapeutic utility in the treatment of idiopathic Parkinson's disease.

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