Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's plasma membrane. According to the trigger that opens the channel for such ions, they can be classified into Voltage-gated sodium channels and ligand-gated sodium channels. Sodium channels are highly selective for the transport of sodium ions across cell membranes. In excitable cells such as neurons, myocytes, and certain types of glia, sodium channels are responsible for the rising phase of action potentials. Many of the most common neurological disorders, such as epilepsy, migraine, neurodegenerative diseases, and neuropathic pain, involve abnormalities of neuronal excitability. There is a growing body of data that implicates abnormal expression and function of voltage-gated sodium channels (VGSCs) in these disorders.

Pharmacological inhibitors of VGSCs have been used for decades to treat epileptic seizures, the most common disease of neuronal excitability, and arrhythmia, and it is becoming increasingly evident that these antiepileptic VGSC blockers might also be efficacious against a broad range of neurological disorders. Sodium channels serve as specific target for a large variety of chemically distinct neurotoxins produced by many different animals and plants. The development of drugs with enhanced selectivity for specific VGSC isoforms might be an effective and novel approach for the treatment of several neurological diseases.

TargetMol’s Sodium Channel Blocker Library collects 118 reported sodium channel blockers and agonists, and is an ideal tool for screening more selective and efficient drugs targeting potassium channels.