Ion Channels

Ion channels are pore-forming membrane proteins that act as gated pathways for the movement of ions across cell membranes. They are found in both surface and intracellular membranes, and play essential roles in the physiology of all cell types. Ion channels are especially prominent components of the nervous system as they underlie the nerve impulse and because "transmitter-activated" channels mediate conduction across the synapses of a nerve cell’s axon. In addition, ion channels are key components in a wide variety of biological processes that involve rapid changes in cells, such as cardiac, skeletal, and smooth-muscle contraction, epithelial transport of nutrients and ions, T-cell activation and pancreatic beta-cell insulin release. Many human diseases are caused by defects in ion channel function, which can lead to disease in a number of different ways: Gain, or loss, of channel function (channel-pathies), defective regulation of channel activity by intracellular or extracellular ligands or by channel modulators, by autoantibodies binding to ion channel proteins, or even by ion channels that act as lethal agents[1]. Ion channels can be categorized based upon multiple characteristics, e.g. their selectivity in permeability for a certain type of ion, the number of pores, or by their mechanism of activation.  The wide range of Axon Ligands™  targeting ion channels has been categorized into ligand gated ion channels and voltage gated ion channels (and more). Categories are subdivided on the basis of their selectivity towards activating ligand or the type of ion. In addition, sections are created for specific members of the family of potassium channels that are characterized by their deviant ways of activation (e.g. calcium-activated, and ATP-sensitive potassium channels).

[1] Taken from Oxford Textbook of Medicine, fifth edition, 2010. ISBN 9780470987261.

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Axon ID Name Description From price
3088 1-BCP Brain-penetrant modulator of AMPA receptor €75.00
3042 AZD 6280 Selective, orally active, allosteric GABA-A α2/3 receptor modulator €125.00
3087 AZD7325 Potent, selective GABAA-α2 and GABAA-α3 modulator €90.00
1763 CoPo 22 Modulator of CFTR (δ-F508 Selective) €120.00
1825 Erastin VDAC2 modulator €90.00
1301 Gabapentin GABA modulator; Anti-convulsant €65.00
1823 Pregabalin Reduces synaptic signaling by binding to α2δ subunits €85.00
2169 VX 661 Corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) €80.00

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