Ion Channel Modulators

Ion channel modulators

The concentration of ions (like sodium, potassium, calcium, magnesium or chloride) in the bloodstream, other fluids and inside the cells of our body is extremely important to maintain our vital physiological functions. In general, the movement (inflow or outflow) of ions across cell membranes occurs through pores created by ion channels. This ionic movement is tightly regulated by ions concentration, cell membrane potential, cellular factors or drugs. Consequently, ion channels play a critical role in a wide variety of processes in the human body, including the maintenance of fluid balance, signal transduction within and among cells (e.g. immune system cells) and the generation and propagation of electric signals along nerves, heart and other organs.

Ion channels are immensely molecularly diverse; for example, there are more than 50 potassium channel subtypes, for many of which there are no specific pharmacological agents known. There is indeed a huge demand for activators and inhibitors (i.e. modulators) for specific ion channels that are key players in certain diseases or syndromes.

There are several drugs in the market that function trough the modulation of specific ion channels. For example, Norvasc and verapamil (calcium channel blockers), which are used for the treatment of hypertension and various other cardiovascular disorders; Lamictal (sodium channel blocker), which is used for the treatment of epilepsy; Glipizide (potassium channel blocker), which is used in the treatment of diabetes; and lidocaine (sodium channel blocker), a local anesthetic.

Ion channels represent an important pharmaceutical target for a broad range of unmet clinical needs.

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