松弛钾通道小分子抑制剂作为儿童癫痫的潜在治疗药物。

IF 1.8 Q3 PHARMACOLOGY & PHARMACY
Alshaima'a M Qunies, Kyle A Emmitte
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引用次数: 3

摘要

松弛通道是由KCNT1基因编码的钠活化钾通道。几个KCNT1功能突变的增加与婴儿期恶性迁移性部分癫痫发作有关。奎尼丁是一种抗心律失常药物,作为松弛通道的中等有效抑制剂;然而,奎尼丁的使用受到其选择性差、安全性和药代动力学特征的限制。松弛通道代表了一个有趣的目标,开发新的治疗方法,恶性迁移部分癫痫发作的婴儿和其他儿童癫痫;因此,正在进行的努力是为了发现抑制松弛电流的小分子。本文综述了2020-2021年发表的描述新型小分子Slack抑制剂发现的专利申请。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies.

Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies.

Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies.

Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies.
Slack channels are sodium-activated potassium channels that are encoded by the KCNT1 gene. Several KCNT1 gain of function mutations have been linked to malignant migrating partial seizures of infancy. Quinidine is an anti-arrhythmic drug that functions as a moderately potent inhibitor of Slack channels; however, quinidine use is limited by its poor selectivity, safety and pharmacokinetic profile. Slack channels represent an interesting target for developing novel therapeutics for the treatment of malignant migrating partial seizures of infancy and other childhood epilepsies; thus, ongoing efforts are directed toward the discovery of small-molecules that inhibit Slack currents. This review summarizes patent applications published in 2020-2021 that describe the discovery of novel small-molecule Slack inhibitors.
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来源期刊
Pharmaceutical patent analyst
Pharmaceutical patent analyst PHARMACOLOGY & PHARMACY-
CiteScore
1.80
自引率
0.00%
发文量
22
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