1,10-菲咯啉镍（II）螯合物及其组成金属离子和配体对豚鼠离体心房的比较作用。

Comparative actions of 1,10-phenanthroline nickel(II) chelates and their constituent metal ion and ligands on the guinea-pig isolated atrium.

作者信息

Shulman A, Grossman H

出版信息

Chem Biol Interact. 1978 Sep;22(2-3):281-6. doi: 10.1016/0009-2797(78)90132-1.

Abstract

The actions of fully co-ordinated, inert nickel(II) chelates of 1,10-phenanthroline and 3,4,7,8-tetramethyl-1,10-phenanthroline have been compared on the guinea-pig isolated atrium with those of their constituent metal ion and ligands. In general, each test substance showed distinctive actions suggesting that the effects of the metal chelates are mediated by the intact chelate cation and not by liberated metal ion or ligand. Differences in the actions of the unsubstituted and the highly methylated compounds may result from the greater capacity of the methylated chelate and ligand to induce more profound and sustained conformational changes in the responsive atrial pre- and postsynaptic membranes thereby promoting more rapid and prolonged influx of Ca2+.

摘要

在豚鼠离体心房上，比较了1,10 - 菲啰啉和3,4,7,8 - 四甲基 - 1,10 - 菲啰啉的完全配位、惰性镍（II）螯合物与其组成的金属离子和配体的作用。一般来说，每种测试物质都表现出独特的作用，这表明金属螯合物的作用是由完整的螯合阳离子介导的，而不是由游离的金属离子或配体介导的。未取代和高度甲基化化合物作用的差异可能是由于甲基化螯合物和配体在诱导反应性心房突触前和突触后膜中更深刻和持续的构象变化方面具有更大的能力，从而促进Ca2+更快速和持久的内流。