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首页> 外文期刊>Expert opinion on therapeutic targets >The therapeutic potential of neuronal KCNQ channel modulators.
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The therapeutic potential of neuronal KCNQ channel modulators.

机译：神经元KCNQ通道调节剂的治疗潜力。

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Neuronal KCNQ (Kv7) channels (KCNQ2 - 5 or Kv7.2 - 7.5, disclosed to date) were discovered by virtue of their homology with a known cardiac channel involved in long QT syndrome (KvLQT or KCNQ1, Kv7.1) and first disclosed in 1998. The involvement of KCNQ2 (Kv7.2) and KCNQ3 (Kv7.3) in a benign idiopathic neonatal epilepsy, KCNQ4 (Kv7.4) in a form of congenital deafness, and the discovery that neuronal KCNQ heteromultimers were among the molecular substrates of M-channels, resulted in a high level of interest for potential drug development strategies. A number of small-molecule modulators were quickly identified, including openers or activators such as the antiepileptic drug candidate retigabine and the structurally-related analgesic drug flupirtine (Katadolon trade mark Asta Medica), and a group of KCNQ channel inhibitors/blockers originally developed for cognition enhancement. All of these data have suggested a rich target profile for modulators of neuronal KCNQ channels, including a variety of neuronalhyperexcitability disorders and conditions for openers, such as the epilepsies, acute pain, neuropathic pain, migraine pain and some neurodegenerative and psychiatric disorders. KCNQ blockers could likewise have utility in disorders characterised by neuronal hypoactivity, including cognition enhancement and perhaps disorders of mood. Emerging patent literature suggests significant interest in neuronal KCNQ modulation in the pharmaceutical industry and significant chemical diversity concerning KCNQ modulation.
机译：神经元KCNQ（Kv7）通道（迄今为止已公开的KCNQ2-5或Kv7.2-7.5）是通过与参与长QT综合征的已知心脏通道（KvLQT或KCNQ1，Kv7.1）的同源性发现的，并首次公开1998年。KCNQ2（Kv7.2）和KCNQ3（Kv7.3）参与良性特发性新生儿癫痫，先天性耳聋形式的KCNQ4（Kv7.4），并且发现神经元KCNQ异源多聚体属于分子M通道的底物引起了对潜在药物开发策略的高度关注。很快发现了许多小分子调节剂，包括开环剂或激活剂，例如抗癫痫药候选药物瑞替加滨和与结构相关的止痛药氟吡汀（Katadolon商标Asta Medica），以及最初开发用于以下用途的一组KCNQ通道抑制剂/阻滞剂认知增强。所有这些数据表明，神经元KCNQ通道的调节剂具有丰富的靶标，包括多种神经元过度兴奋性疾病和开放性疾病，例如癫痫，急性疼痛，神经性疼痛，偏头痛和某些神经变性和精神疾病。 KCNQ阻滞剂同样可用于以神经元功能低下为特征的疾病，包括认知能力增强，甚至可能是情绪障碍。新兴的专利文献表明，制药行业对神经元KCNQ调节非常感兴趣，并且涉及KCNQ调节也涉及大量化学多样性。

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