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Characterization of a novel high-potency positive modulator of K v 7 channels

W Dalby-Brown, C Jessen, C Hougaard…

文献索引:Dalby-Brown, William; Jessen, Carsten; Hougaard, Charlotte; Jensen, Marianne L.; Jacobsen, Thomas A.; Nielsen, Karin S.; Erichsen, Helle K.; Grunnet, Morten; Ahring, Philip K.; Christophersen, Palle; Strobaek, Dorte; Jorgensen, Susanne European Journal of Pharmacology, 2013 , vol. 709, # 1-3 p. 52 - 63

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被引用次数: 9

摘要

Kv7 channel activators decrease neuronal excitability and might potentially treat neuronal hyperexcitability disorders like epilepsy and mania. Here we introduce NS15370 ((2-(3, 5- difluorophenyl)-N-[6-[(4-fluorophenyl) methylamino]-2-morpholino-3-pyridyl] acetamide) hydrochloride, an in vitro high-potency chemical analogue of retigabine, without effects on GABAA receptors. NS15370 activates recombinant homo-and heteromeric Kv7. 2–Kv7. 5 ...