THE STRETCH-ACTIVATED ION-CHANNEL BLOCKER GADOLINIUM ALSO BLOCKS L-TYPE CALCIUM CHANNELS IN ISOLATED VENTRICULAR MYOCYTES OF THE GUINEA-PIG
THE STRETCH-ACTIVATED ION-CHANNEL BLOCKER GADOLINIUM ALSO BLOCKS L-TYPE CALCIUM CHANNELS IN ISOLATED VENTRICULAR MYOCYTES OF THE GUINEA-PIG
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DOI：
10.1016/0005-2736(94)90250-x
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发表时间：
1994-04-20
影响因子：
3.4
通讯作者：
LEGUENNEC, JY
中科院分区：
文献类型：
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作者：
LACAMPAGNE, A;GANNIER, F;LEGUENNEC, JY
我们证明钆 (Gd3(+)) 是豚鼠离体心室肌细胞中有效的钙通道阻滞剂。 I-CaL 的剂量依赖性抑制。发现 EC(50) 为 1.4 muM，并且在 10 muM Gd3(+) 下完全抑制。与 Cd2+ 相比，I-CaL 似乎被阻断。是一种复杂现象，可能涉及多个位点，可能涉及多个相互作用位点（Gd3+ 的希尔系数为 1.6，而 Cd2+ 的希尔系数为 1.0）。结论是Gd3+离子完全阻断I-CaL。在用于阻断拉伸激活通道 (SAC) 的浓度下，使其作为特定 SAC 抑制剂的使用存在问题。
We show that gadolinium (Gd3(+)) is a potent calcium channel blocker in guinea-pig isolated ventricular myocytes. A dose-dependent inhibition of I-CaL. was found with an EC(50) of 1.4 mu M and a complete inhibition at 10 mu M Gd3(+). When compared with Cd2+, it appeared that the blockade of I-CaL. is a complex phenomenon probably involving more than one sitphenomenon probably involving more than one site of interaction (a Hill coefficient of 1.6 was found for Gd3+ vs. 1.0 for Cd2+). It is concluded that Gd3+ ions completely block I-CaL. at concentrations used to block stretch-activated channels (SAC), rendering its use as a specific SAC inhibitor problematic.