IEM 1754 dihydrobromide,162831-31-4

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YZ剂描述：

产品名称：IEM 1754 dihydrobromide

产品别名：IEM 1754 2HBr

英文别名：IEM 1754 2HBr

靶点：GluR1 ，GluR3

CAS：162831-31-4

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

IEM 1754 dihydrobroMide是一种选择性AMPA/kainate受体YZ剂，作用于GluR1和GluR3，IC50为6 μM。IEM 1754是一种金刚烷衍生物。IEM 1754可以引起对重组AMPA受体开放通道的使用和电压依赖性阻断。拮抗作用依赖于受体亚单位组成部分, GluR1和 GluR3门控通道对阻断的敏感性高于GluR2构成的受体门控通道。

溶解性：DMSO ：82 mg/mL (198.9 mM)
Water ：82 mg/mL (198.9 mM)

体外研究：

IEM 1754 is an adamantane derivative. IEM 1754 causes use- and voltage-dependent block of open channels of recombinant AMPA receptors. This antagonism is dependent on receptor subunit composition, channels gated by recombinant, homomeric GluR1 and GluR3 receptors exhibites a higher sensitivity to block than those gated by receptors containing edited GluR2 subunits. IEM-1754 block of GluR2-containing AMPAR is enhanced by hyperpolarization in agreement with the classical single-exponential model. In contrast, the block of GluR2-lacking AMPAR is reduced by hyperpolarization.

体内研究：

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