PF-05020182(PF-05020182) - 药物靶点：KCNQ5 x Kv7.2 x Kv7.3 x Kv7.4_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

KCNQ5 x Kv7.2 x Kv7.3 x Kv7.4

作用机制

KCNQ5 modulators(KCNQ voltage-gated potassium channel-5 modulators)、Kv7.2调节剂(电压门控性钾通道蛋白亚型Kv7.2调节剂)、Kv7.3调节剂(KCNQ3通道调节剂)

+ [1]

治疗领域

神经系统疾病

在研适应症-

非在研适应症

癫痫

原研机构

Pfizer Inc.

在研机构-

非在研机构

Pfizer Inc.

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 PF-05020182 相关的临床结果

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100 项与 PF-05020182 相关的转化医学

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100 项与 PF-05020182 相关的专利（医药）

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1

项与 PF-05020182 相关的文献（医药）

2015-11-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Discovery of a novel Kv7 channel opener as a treatment for epilepsy

4区 · 医学

Article

作者: Serpa, Kevin A ; Arora, Gaurav ; Rogers, Bruce N ; Stolyar, Polina ; Baker, Karen ; Claffey, Michelle M ; Duplantier, Allen J ; Wright, Ann S ; Butler, Christopher R ; Boscoe, Brian P ; Rong, SuoBao ; Reese, Matthew R ; DeNinno, Shari L ; Tse, Karen ; Snow, Sheri L ; Zhang, Lei ; Drozda, Susan E ; Schuyten, Katherine ; Moine, Ludivine ; Whisman, Tammy L ; Clark, Alan J ; Weber, Mark L ; Rong, Haojing ; Lowe, John A ; Mather, Robert J ; Davoren, Jennifer E ; Chenard, Lois

Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures. In an effort to identify a compound with such properties, the structure-activity relationship (SAR) and in vitro ADME for a series of heterocyclic Kv7.2-7.5 channel openers was explored. PF-05020182 (2) demonstrated suitable properties for further testing in vivo where it dose-dependently decreased the number of animals exhibiting full tonic extension convulsions in response to corneal stimulation in the maximal electroshock (MES) assay. In addition, PF-05020182 (2) significantly inhibited convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 (2) support further development as an adjunctive treatment of refractory epilepsy.

100 项与 PF-05020182 相关的药物交易

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