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
2742 GSK 2193874 Orally active TRPV4 antagonist €120.00
2860 GTS 21 dihydrochloride Selective α7 nicotinic acetylcholine receptor (nAChR) partial agonist €90.00
1967 GW 791343 hydrochloride P2X7 receptor antagonist and allosteric modulator Inquire
1374 GYKI 53655 AMPA antagonist €85.00
1757 HMR 1098 K+ channel blocker (SUR1/Kir6.2 selective) €115.00
2724 ICA-069673 KCNQ2/KCNQ3 channel opener; Anti-convulsant €90.00
1156 Ifenprodil L-(+)-tartrate NMDA antagonist €55.00
2890 JNJ 47965567 Potent, brain-penetrant P2X7 antagonist €135.00
2793 JNJ 55511118 Negative modulator of AMPA receptor (TARP-γ8 selective) €95.00
1735 Kv1.3 Channel blocker 42 Kv1.3 potassium channel blocker €110.00
1196 L 838417 GABAA-α1 antagonist €95.00
1444 Lacosamide Na+ channel blocker; anti-convulsant €75.00
1353 Lamotrigine Glutamate antagonist; Na+ channel blocker €60.00
2423 M8-B hydrochloride Selective and potent antagonist of the TRPM8 channel €115.00
2747 ML 213 KCNQ2/KCNQ4 channel opener €75.00

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