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
2534 (+)-Azasetron hydrochloride 5-HT3 antagonist €135.00
1077 (+)-Epibatidine dihydrochloride Nicotinic acetylcholine receptor agonist €155.00
1594 (+)-Pagoclone GABAA-α2 and GABAA-α3 agonist €135.00
2535 (-)-Azasetron hydrochloride 5-HT3 antagonist €135.00
1078 (-)-Epibatidine dihydrochloride Nicotinic acetylcholine receptor agonist €155.00
1758 (R)-(+)-BAY K 8644 Calcium (Ca2+) channel modulator €115.00
1309 (R)-(-)-BMS 204352 Potassium channel opener; Less active enantiomer of Axon 1112 €145.00
2784 (R)-(-)-N-Desmethyl-PK 11195 Radioligand precursor of the benzodiazepine antagonist (R)-(-)-PK 11195 €150.00
2785 (R)-(-)-PK 11195 Benzodiazepine antagonist. €130.00
1759 (S)-(-)-BAY K 8644 Calcium (Ca2+) channel activator (L-type voltage-gated) €115.00
1308 (±)-BMS 204352 Potassium channel opener; racemate of Axon 1112 Inquire
1076 (±)-Epibatidine dihydrochloride Nicotinic acetylcholine receptor agonist €95.00
3088 1-BCP Brain-penetrant modulator of AMPA receptor €75.00
1313 1-EBIO K+ channel opener (Ca2+ activated) €50.00
2694 4BP-TQS Allosteric agonist of α7 nAChR €110.00
1816 A 784168 TRPV1 receptor antagonist €95.00
1915 A 803467 Blocker of the voltage-gated Nav1.8 channel €95.00
2182 A 804598 Potent and selective P2X7 antagonist €125.00
3835 A-438079 hydrochloride Competitive P2X7 antagonist €110.00
3019 A2764 dihydrochloride Selective inhibitor of the TRESK potassium channel €105.00
3060 A2793 Inhibitor of the TRESK and TASK-1 potassium channel €95.00
1504 ABT 102 TRPV1 antagonist €90.00
3785 ABT-639 Peripherally acting, selective and orally bioavailable T-type Ca2+ channel blocker €115.00
3698 AC-5216 Selective translocator protein (TSPO) ligand €90.00
3026 AC1903 Selective TRPC5 inhibitor €95.00
2552 Adjudin Non-hormonal male contraceptive with anti-proliferative activity €125.00
3524 AKOS-022 VDAC1 inhibitor  Recently added €120.00
1097 Alosetron hydrochloride 5-HT3 antagonist €85.00
1113 AM 36 dihydrochloride Na+ channel blocker €145.00
3356 AMG 9810 Potent and selective vanilloid receptor-1 (TRPV1) antagonist €90.00

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