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海人酸可使培养神经元中的谷氨酸释放呈浓度依赖性升高,但不会使环磷酸鸟苷水平升高。

Kainate produces concentration-dependent elevation of glutamate release but not cGMP levels in cultured neuron.

作者信息

Oh S, McCaslin P P

机构信息

Department of Pharmacology and Toxicology, University of Mississippi Medical Center, Jackson 39216-4045, USA.

出版信息

Gen Pharmacol. 1996 Jan;27(1):83-7. doi: 10.1016/0306-3623(95)00079-8.

Abstract
  1. Treatment of cultured cerebellar granule cells for 3 min with N-methyl-D-aspartate (NMDA) resulted in a concentration-dependent elevation of cyclic GMP. However, neither kainate (KA) nor NMDA produced a concentration-dependent elevation of this nucleotide after exposing cells to the agonist for 60 min. 2. Unlike the case for cGMP, both KA and NMDA produced concentration-dependent elevations of glutamate for 60 min incubation. 3. The NMDA-induced elevations of cGMP and glutamate were blocked by selective NMDA receptor antagonists. 4. The selective KA/alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) receptor antagonist, 6,7-nitroquinoxaline-2,3-dione (DNQX), blocked the KA-induced elevations of cGMP with 3-min exposures, but it augmented the response with 60-min exposures. However, the KA-induced release of glutamate was prevented by DNQX. 5. The KA/AMPA receptor antagonist, GYKI 52466, blocked all KA-induced responses regardless of the incubation times.
摘要
  1. 用N-甲基-D-天冬氨酸(NMDA)处理培养的小脑颗粒细胞3分钟,可导致环磷酸鸟苷(cGMP)浓度依赖性升高。然而,在将细胞暴露于激动剂60分钟后,红藻氨酸(KA)和NMDA均未产生该核苷酸的浓度依赖性升高。2. 与cGMP的情况不同,KA和NMDA在孵育60分钟时均产生谷氨酸浓度依赖性升高。3. NMDA诱导的cGMP和谷氨酸升高被选择性NMDA受体拮抗剂阻断。4. 选择性KA/α-氨基-3-羟基-5-甲基异恶唑-4-丙酸(AMPA)受体拮抗剂6,7-二硝基喹喔啉-2,3-二酮(DNQX)在暴露3分钟时可阻断KA诱导的cGMP升高,但在暴露60分钟时会增强该反应。然而,DNQX可阻止KA诱导的谷氨酸释放。5. KA/AMPA受体拮抗剂GYKI 52466无论孵育时间如何,均可阻断所有KA诱导的反应。

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