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Voltage-gated K+ channel modulators as neuroprotective agents.

机译:电压门控K +通道调节剂作为神经保护剂。

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摘要

A manifestation in neurodegeneration is apoptosis of neurons. Neurons undergoing apoptosis may lose a substantial amount of cytosolic K+ through a number of pathways including K+ efflux via voltage-gated K+ (Kv) channels. The consequent drop in cytosolic [K+] relieves inhibition of an array of pro-apoptotic enzymes such as caspases and nucleases. Blocking Kv channels has been known to prevent neuronal apoptosis by preventing K+ efflux. Some neural diseases such as epilepsy are caused by neuronal hyperexcitability, which eventually may lead to neuronal apoptosis. Reduction in activities of A-type Kv channels and Kv7 subfamily members is amongst the etiological causes of neuronal hyperexcitation; enhancing the opening of these channels may offer opportunities of remedy. This review discusses the potential uses of Kv channel modulators as neuroprotective drugs.
机译:神经变性的一种表现是神经元的凋亡。经历凋亡的神经元可能会通过许多途径(包括经由电压门控K +(Kv)通道的K +外排)丢失大量的胞质K +。随之而来的胞质[K +]的下降减轻了对一系列促凋亡酶(例如胱天蛋白酶和核酸酶)的抑制作用。已知阻断Kv通道可通过阻止K +外流来预防神经元凋亡。一些神经疾病,例如癫痫病,是由神经元过度兴奋引起的,最终可能导致神经元凋亡。 A型Kv通道和Kv7亚家族成员活动的减少是神经元过度兴奋的病因。加强这些渠道的开放可能会提供补救的机会。这篇评论讨论了Kv通道调节剂作为神经保护药物的潜在用途。

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