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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >Potentiation by calcium ions of (3H)MK-801 binding to an ion channel associated with the N-methyl-D-aspartate receptor complex in rat brain.
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Potentiation by calcium ions of (3H)MK-801 binding to an ion channel associated with the N-methyl-D-aspartate receptor complex in rat brain.

机译:(3H)MK-801的钙离子与大鼠脑中N-甲基-D-天冬氨酸受体复合物相关的离子通道结合后的增强作用。

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摘要

In vitro addition of Ca2+ ions was effective in almost doubling binding of [3H](+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imi ne (MK-801) before equilibrium to an ion channel associated with an N-methyl-D-aspartate (NMDA)-sensitive subclass of brain excitatory amino acid receptors. The addition of inhibitors for phospholipase (PLase) A2 markedly reduced binding in the absence of added Ca2+ ions, while Ca2+ ions restored the reduction to the level found in the absence of the inhibitors. Pretreatment with PLases A2 and C but not D was effective in potentiating [3H]MK-801 binding in a biphasic manner at a concentration range of 5 mU/ml-10 U/ml. Moreover, PLases A2 and C at low concentrations not only suppressed the abilities of 3 different agonists to potentiate [3H]MK-801 binding before equilibrium, but also reduced that of Ca2+ ions. These results suggest that Ca2+ ions may potentiate [3H]MK-801 binding to the NMDA channel highly permeable to Ca2+ ions through a mechanism common to that underlying potentiation by exogenous PLase A2 and/or C.
机译:体外添加Ca2 +离子可有效地使[3H](+)-5-甲基-10,11-二氢-5H-二苯并[a,d]环庚烯5,10-亚胺的结合几乎翻倍(MK-801 )平衡至与脑兴奋性氨基酸受体的N-甲基-D-天冬氨酸(NMDA)敏感亚类相关的离子通道之前。在不存在添加的Ca2 +离子的情况下,添加磷脂酶(PLase)A2抑制剂会显着降低结合,而Ca2 +离子可将还原恢复到在不存在抑制剂的情况下的水平。用PLase A2和C预处理但不使用D预处理可以有效地以双相方式在5 mU / ml-10 U / ml的浓度范围内增强[3H] MK-801的结合。此外,低浓度的PLase A2和C酶不仅抑制了3种不同激动剂在平衡前增强[3H] MK-801结合的能力,还降低了Ca2 +离子的能力。这些结果表明,Ca2 +离子可能通过与外源PLase A2和/或C潜在的增效作用共有的机制,增强[3H] MK-801与Ca2 +离子高度可渗透的NMDA通道的结合。

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