Wua Yong-Jin, Dworetzky Steven I
Department of Neuroscience Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA.
Curr Med Chem. 2005;12(4):453-60. doi: 10.2174/0929867053363045.
During the past five years, several members of the KCNQ potassium channel gene family have been identified with a high degree of CNS specificity. Within the KCNQ family, the combination of the KCNQ2/KCNQ3 proteins, and the KCNQ5/KCNQ3 arrangement has been identified as the molecular correlates of the different M-currents. Several lines of evidence are emerging demonstrating the importance of these channels in regulating neuronal excitability; for example, determination of the excitability threshold, firing properties, and responsiveness of neurons to synaptic inputs. Recent studies have shown that KCNQ openers have potential for the treatment of several CNS disorders characterized by neuronal hyperexcitability, such as migraine, epilepsy and neuropathic pain. This article reviews the recent developments of KCNQ potassium channel openers.
在过去五年中，已鉴定出几个具有高度中枢神经系统（CNS）特异性的KCNQ钾通道基因家族成员。在KCNQ家族中，KCNQ2/KCNQ3蛋白的组合以及KCNQ5/KCNQ3排列已被确定为不同M电流的分子相关物。越来越多的证据表明这些通道在调节神经元兴奋性方面的重要性；例如，确定神经元的兴奋阈值、放电特性以及对突触输入的反应性。最近的研究表明，KCNQ开放剂有潜力治疗几种以神经元过度兴奋为特征的中枢神经系统疾病，如偏头痛、癫痫和神经性疼痛。本文综述了KCNQ钾通道开放剂的最新进展。
