THE PHARMACOLOGY OF INTRACELLULAR CA2+-RELEASE CHANNELS
THE PHARMACOLOGY OF INTRACELLULAR CA2+-RELEASE CHANNELS
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DOI：
10.1016/0165-6147(94)90074-4
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发表时间：
1994-05-01
影响因子：
13.8
通讯作者：
BEZPROZVANNY, I
中科院分区：
文献类型：
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作者：
EHRLICH, BE;KAFTAN, E;BEZPROZVANNY, I
两类细胞内钙释放通道，兰尼定受体和肌醇(1，4，5)-三磷酸(IP3)受体，在细胞内的时空钙信号传递中是必不可少的。肝素和咖啡因已被广泛用于研究这些通道。最初认为咖啡因仅作为兰尼定受体的激动剂，而肝素仅作为IP3受体的抑制剂。然而，最近的实验表明，这些化合物具有多种作用，Barbara Ehrlich和他的同事在这篇综述中对此进行了讨论。在相同的浓度范围内，咖啡因激活兰尼定受体并抑制IP3受体，肝素抑制IP3受体并激活兰尼定受体。适合研究兰尼定和IP3受体的更具体的药理学工具现在开始出现。
Two classes of intracellular Ca2+-release channels, the ryanodine receptor and the inositol (1,4,5)-trisphosphate (IP3) receptor, are essential for spatio-temporal Ca2+ signalling in cells. Heparin and caffeine have been widely used to study these channels. It was originally thought that caffeine acts solely as an agonist for the ryanodine receptor and heparin acts solely as an inhibitor for the IP3 receptor. However, recent experiments indicate that these compounds have multiple effects, and are discussed in this review by Barbara Ehrlich and colleagues. In the same concentration range, caffeine activates the ryanodine receptor and inhibits the IP3 receptor, and heparin inhibits the IP3 receptor and activates the ryanodine receptor. More specific pharmacological tools that are suitable for studies of ryanodine and IP3 receptors are now beginning to emerge.