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首页> 外文期刊>Alcohol >Ethanol increases desensitization of recombinant GluR-D AMPA receptor and TARP combinations.
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Ethanol increases desensitization of recombinant GluR-D AMPA receptor and TARP combinations.

机译：乙醇会增加重组GluR-D AMPA受体和TARP组合的脱敏作用。

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摘要

Glutamate receptors are important target molecules of the acute effect of ethanol. We studied ethanol sensitivity of homomeric GluR-D receptors expressed in human embryonic kidney 293 cells and examined whether recently discovered transmembrane alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor regulatory proteins (TARPs) affect ethanol sensitivity. Coexpression of the TARPs, stargazin, and gamma4 increased the time constant (tau-value) of current decay in the presence of agonist, thus slowing the onset of desensitization and increasing the steady-state current. Ethanol produced less inhibition of the peak current than the steady-state current for all types of the GluR-D receptors. In addition, ethanol concentration-dependently accelerated the rate of desensitization, measured as the tau-value of fast decay of peak current. This effect was enhanced with coexpression of TARPs. The recovery from desensitization was slowed down by coexpression of gamma4 but ethanol did not affect this process in any GluR-D combination. The results support the idea that increased desensitization is an important mechanism in the ethanol inhibition of AMPA receptors and indicate that coexpression of TARPs can alter this effect of ethanol.
机译：谷氨酸受体是乙醇急性作用的重要靶分子。我们研究了人类胚胎肾293细胞中表达的同型GluR-D受体的乙醇敏感性，并研究了最近发现的跨膜α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体调节蛋白（TARP）是否影响乙醇灵敏度。 TARP，stargazin和gamma4的共表达增加了在存在激动剂的情况下电流衰减的时间常数（tau值），从而减慢了脱敏的发生并增加了稳态电流。对于所有类型的GluR-D受体，乙醇对峰值电流的抑制作用均小于稳态电流。此外，乙醇浓度依赖于加速脱敏速率，以峰值电流快速衰减的tau值表示。 TARPs的共表达增强了这种效果。脱敏的恢复由于共表达gamma4而减慢，但是乙醇在任何GluR-D组合中均不影响该过程。结果支持以下想法：增加的脱敏作用是AMPA受体的乙醇抑制作用的重要机制，并表明TARPs的共表达可以改变乙醇的这种作用。

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