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.
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 | €120.00 | |
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) | €120.00 | |
1308 | (±)-BMS 204352 | Potassium channel opener; racemate of Axon 1112 | Inquire | |
1076 | (±)-Epibatidine dihydrochloride | Nicotinic acetylcholine receptor agonist | €95.00 | |
4114 | (±)-trans-ML-SI3 | TRPML1/3 inhibitor and TRPML2 activator | Recently added | €120.00 |
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 | €120.00 | |
1097 | Alosetron hydrochloride | 5-HT3 antagonist | €85.00 | |
1113 | AM 36 dihydrochloride | Na+ channel blocker | €145.00 |