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
3415 AMPA Highly selective AMPA receptor agonist €110.00
3335 AZD6765 dihydrochloride Noncompetitive NMDA antagonist €90.00
1217 CFM 2 AMPA antagonist €115.00
2079 CMPDA Positive allosteric modulator of AMPA receptor €85.00
1200 CNQX AMPA/Kainate antagonist €85.00
2522 CNQX disodium salt AMPA/Kainate antagonist €90.00
2254 CP 101606 NMDA NR2B antagonist €120.00
1406 CP 101606 mesylate NMDA NR2B antagonist €85.00
3089 CX516 Positive allosteric modulator of AMPA receptor €70.00
3090 CX546 Positive allosteric modulator of AMPA receptor €95.00
1201 DNQX AMPA/Kainate antagonist €50.00
1246 Eliprodil NMDA antagonist €90.00
2687 Farampator Second-generation ampakine that potentiates AMPA receptor function €99.00
1262 Gavestinel NMDA antagonist (glycine site) €110.00
1374 GYKI 53655 AMPA antagonist €85.00
1156 Ifenprodil L-(+)-tartrate NMDA antagonist €55.00
2793 JNJ 55511118 Negative modulator of AMPA receptor (TARP-γ8 selective) €95.00
1353 Lamotrigine Glutamate antagonist; Na+ channel blocker €60.00
1249 N 20C hydrochloride NMDA antagonist €85.00
3472 NMDA Selective NMDA agonist €60.00
3349 NMDAR-TRPM4 blocker C19 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €130.00
3348 NMDAR-TRPM4 blocker C8 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €120.00
1434 RGH 896 NMDA NR2B antagonist €95.00
3499 Riluzole Glutamatergic neurotransmission blocker; neuroprotectant €80.00
3576 Riluzole hydrochloride Glutamatergic neurotransmission blocker; neuroprotectant €80.00
1314 RO 25-6981 hydrochloride NMDA NR2B antagonist €110.00
2601 RO 25-6981 maleate NMDA NR2B antagonist €110.00
1788 S 18986 Positive allosteric modulator of AMPA receptor €105.00
2708 TCN-201 NMDA NR2A antagonist €105.00

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