加兰他敏可阻断克隆的Kv2.1通道，但不影响Kv1.5钾通道。
Galantamine blocks cloned Kv2.1, but not Kv1.5 potassium channels.
作者信息
Zhang Hai-Xia, Zhang Wei, Jin Hong-Wei, Wang Xiao-Liang
机构信息
Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, PR China.
出版信息
Brain Res Mol Brain Res. 2004 Nov 24;131(1-2):136-40. doi: 10.1016/j.molbrainres.2004.08.010.
Galantamine is a cholinesterase inhibitor (AChEI) currently used in treatment of Alzheimer's disease (AD). In the present study, the effects of galantamine on currents of cloned Kv2.1 and Kv1.5 potassium channels were investigated by using patch-clamp whole cell recording techniques. Kv2.1 and Kv1.5 were stably expressed in HEK293 cells. Galantamine blocked Kv2.1 current in a concentration-dependent manner. When depolarizing from -50 to +40 mV, the IC50 of galantamine for inhibition of Kv2.1 was 5.6 microM. Galantamine 10 microM shifted the activation curve of Kv2.1 to negative potential by 4.0 mV. At the same concentration, galantamine shifted the inactivation curve to negative potential by 25.2 mV. While Kv1.5 was not sensitive to galantamine, Kv1.5 current was not changed by galantamine at concentration of 10 microM. Our data suggest that galantamine potently blocks Kv2.1, but not Kv1.5 channels.
加兰他敏是一种胆碱酯酶抑制剂（AChEI），目前用于治疗阿尔茨海默病（AD）。在本研究中，采用膜片钳全细胞记录技术研究了加兰他敏对克隆的Kv2.1和Kv1.5钾通道电流的影响。Kv2.1和Kv1.5在HEK293细胞中稳定表达。加兰他敏以浓度依赖性方式阻断Kv2.1电流。当从-50 mV去极化至+40 mV时，加兰他敏抑制Kv2.1的IC50为5.6 microM。10 microM的加兰他敏使Kv2.1的激活曲线向负电位移动4.0 mV。在相同浓度下，加兰他敏使失活曲线向负电位移动25.2 mV。而Kv1.5对加兰他敏不敏感，10 microM浓度的加兰他敏对Kv1.5电流无影响。我们的数据表明，加兰他敏可有效阻断Kv2.1通道，但不能阻断Kv1.5通道。
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