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二氮平,一种用于钙通道二氢吡啶受体的新型光亲和探针。

Diazipine, a novel photoaffinity probe for dihydropyridine receptors of calcium channels.

作者信息

Taki M, Nakayama H, Kanaoka Y

机构信息

Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan.

出版信息

FEBS Lett. 1991 Jun 3;283(2):259-62. doi: 10.1016/0014-5793(91)80602-y.

Abstract

A new 1,4-dihydropyridine photoaffinity ligand, [3H]diazipine, has been assessed by binding and photolabeling, and compared with a currently used [3H]azidopine. [3H]Diazipine reversibly binds to skeletal muscle Ca2+ channels with a similar affinity to [3H]azidopine, but [3H]diazipine labels the channel two times more efficiently and no release of the incorported amount is observed after dithiothreitol treatment.

摘要

一种新型的1,4 - 二氢吡啶光亲和配体[3H]二氮平,已通过结合和光标记进行评估,并与目前使用的[3H]叠氮平进行比较。[3H]二氮平以与[3H]叠氮平相似的亲和力可逆地结合到骨骼肌Ca2+通道上,但[3H]二氮平标记通道的效率高出两倍,并且在二硫苏糖醇处理后未观察到掺入量的释放。

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