钙调素依赖性磷酸化抑制剂同时抑制骨骼肌肌浆网钙摄取和钙依赖性atp酶活性,并短暂诱导钙释放。

W Hasselbach, A Migala
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引用次数: 4

摘要

在适当的实验条件下,钙调素拮抗剂如化合物48/80不会将钙摄取与骨骼肌肌浆网膜钙依赖性ATP水解分离,而是同时抑制这两个过程。除了药物的泵抑制作用外,它们还与肌浆网中的咖啡因敏感钙通道相互作用,引起快速的瞬时钙释放。
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Inhibitors of calmodulin-dependent phosphorylation simultaneously inhibit calcium uptake and calcium-dependent ATPase activity in skeletal muscle sarcoplasmic reticulum and transiently induce calcium release.

Under adequate experimental conditions calmodulin antagonists like compound 48/80 do not dissociate calcium uptake from the calcium-dependent ATP hydrolysis of skeletal muscle sarcoplasmic reticulum membranes but simultaneously inhibit both processes. Apart from the agent's pump inhibiting effect, they interact with the caffeine sensitive calcium channel in the sarcoplasmic reticulum causing a rapid transient calcium release.

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