Voltage-Gated Sodium Channel Blockers Library
The voltage-gated sodium channels (VGSCs) are a family of membrane proteins forming a pore, through which they selectively conduct sodium ions inward and outward cell’s plasma membranes in response to variations of membrane potentials.
Many of the most common neurological disorders, such as epilepsy, migraine, neurodegeneration, and chronic pain, involve abnormalities in neuronal excitability. VGSCs play a fundamental role in originating the rising phase of cell membrane action potential and many experimental data indicate that the functional VGSCs could be implicated in the pathogenesis and/or the progression of such disorders. VGSC-interfering drugs have been used for decades to treat epileptic seizures, the most common disease related to abnormal neuronal excitability, and it has become evident that VGSC blockers could also be beneﬁcial in the therapy of a broad range of disorders.
Our new Voltage-Gated Sodium Channel Blockers Library (1477 compounds in total)
was designed as a special screening library containing compounds with predicted sodium channels blocking activity and selectivity. The compounds have been selected by pharmacophore screening of OTAVAchemicals Drug-like Green Collection
against three ligand-based pharmacophore models. The models were built based on the known sodium channel blockers divided into three groups according to their structural features.
This library comprises drug-like compounds only.
All the compounds are in stock, cherry-picking is available.
The library (DB, SD, XLS, PDF format) as well as the price-list is available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain this library or if you need more information.
Catterall WA (2000) From ionic currents to molecular mechanisms: the structure and function of voltage-gated sodium channels. Neuron 26:13–25
Mantegazza M, Curia G, Biagini G, Ragsdale DS, Avoli M (2010) Voltage-gated sodium channels as therapeutic targets in epilepsy and other neurological disorders. Lancet Neurol 9:413–424
Lampert A, O’Reilly AO, Reeh P, Lefﬂer A (2010) Sodium channelopathies and pain. Pﬂugers Arch Eur J Physiol 460:249–263