AMPA受体异质性在鼠海马神经元cyclothiazide揭示了微分灵敏度。

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斑点兆瓦,巴尔R, Patneau DK,梅耶尔毫升

AMPA受体异质性在鼠海马神经元cyclothiazide揭示了微分灵敏度。

J Neurophysiol。1996年6月,75(6):2322 - 33所示。

PubMed ID

8793745 (在PubMed

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文摘

1。发病的动力学alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic酸(AMPA)由谷氨酸受体脱敏和衰减的程度由cyclothiazide AMPA受体脱敏,显示明显的大鼠海马神经元的细胞间文化的差异。文化由CA1区地层radiatum倾向于显示弱调制比文化cyclothiazide准备从整个海马。2。动力学分析浓度跳对谷氨酸的反应显示多个受体的数量与快(大约400毫秒),中间(大约2 - 4 s)和(> 20年代)时间常数复苏缓慢由cyclothiazide调制。这些组件的振幅细胞之间的差异很大,建议至少存在三个种群的AMPA受体亚型,相对密度的变化从细胞到细胞。3所示。cyclothiazide敏感性的复杂的模式出现在海马神经元可以通过组装重组的重组AMPA受体亚基产生互补编码flip (i)和失败(o)拼接的变体GluR-A GluR-B子单元。恢复从调制cyclothiazide慢了GluR-AiBi和比GluR-AiBo GluR-AoBi GluR-AoBo。4所示。 Coexpression of the flip and flop splice variants of GluR-A, in the absence of GluR-B, revealed that heteromeric AMPA receptors with intermediate sensitivity to cyclothiazide, similar to responses observed for the combinations GluR-AoBi or GluR-AiBo, could be generated independently of the presence of the GluR-B subunit. However, recovery from modulation by cyclothiazide was twofold slower for GluR-AiBi than for homomeric GluR-Ai, indicating that the GluR-A and GluR-B subunits are not functionally equivalent in controlling sensitivity to cyclothiazide. 5. These results demonstrate that AMPA receptors expressed in hippocampal neurons are assembled in a variety of subunit and splice variant combinations that might serve as a mechanism to fine-tune the kinetics of synaptic transmission.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Cyclothiazide	碳酸酐酶1	蛋白质	人类	未知的	抑制剂	细节