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Discovery of a Novel Kv7 Channel Opener as a Treatment for Epilepsy

Discovery of a Novel Kv7 Channel Opener as a Treatment for Epilepsy

Jennifer E Davoren, Michelle M Claffey, Sheri L Snow, Matthew R Reese, Gaurav Arora, Christopher R Butler, Brian P Boscoe, Lois Chenard, Shari L DeNinno, Susan E Drozda, Allen J Duplantier, Ludivine Moine, etc.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944.

PMID: 25987375

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1354712927	PF-05020182		1354712-92-7	Price

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