R-type calcium channel α1E Inhibitors
Chemical inhibitors of R-type calcium channels α1E function through a variety of mechanisms to inhibit the passage of calcium ions through these channels. SNX-482 exhibits a high level of specificity for R-type calcium channels α1E, functioning by directly binding to the α1 subunit of the channel, which includes the α1E subunit, and thus obstructing the influx of calcium ions. Similarly, Nickel Chloride and Cadmium Chloride act by non-selectively binding to the extracellular side of R-type calcium channels α1E among other voltage-gated calcium channels, thereby inhibiting calcium entry. The peptide toxins ω-Conotoxin GVIA and ω-Conotoxin MVIIC also target these channels with high specificity, binding directly to R-type calcium channels α1E and impeding the flow of calcium ions, although ω-Conotoxin MVIIC has a lower affinity for R-type channels compared to P/Q-type channels. ω-Agatoxin IVA, while known to preferentially inhibit P/Q-type calcium channels, can also hinder R-type calcium channels α1E at elevated concentrations by blocking the channel.
In addition to these direct inhibitors, several other chemicals can indirectly influence the activity of R-type calcium channels α1E. Ethosuximide and Mibefradil, which are primarily T-type calcium channel blockers, may alter cellular calcium dynamics and electrical properties, which in turn can modulate the activity of R-type channels α1E. Amiloride, through its effects on sodium channels and sodium-calcium exchangers, alters intracellular calcium levels and the driving force for calcium entry, which can influence the activity of R-type channels. Lastly, the dihydropyridine compound Nifedipine, and the phenylalkylamine Verapamil, as well as the benzothiazepine Diltiazem, are all known to inhibit L-type calcium channels, but they can also indirectly affect R-type calcium channels α1E by altering overall calcium homeostasis and membrane potentials, which can modulate the contribution of R-type channels to cellular excitability.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Ethosuximide | 77-67-8 | sc-211431 | 1 g | $306.00 | ||
Ethosuximide blocks T-type calcium channels, which can indirectly inhibit R-type calcium channels α1E by altering the cellular calcium dynamics and electrical properties that could dampen the activity of R-type channels as they are part of the overall network of calcium channels regulating membrane potential and excitability. | ||||||
Mibefradil dihydrochloride | 116666-63-8 | sc-204083 sc-204083A | 10 mg 50 mg | $213.00 $865.00 | 4 | |
Mibefradil inhibits T-type calcium channels, and by modulating the intracellular calcium levels and membrane potential through this action, it can indirectly lead to a decrease in R-type calcium channel α1E activity as the two channel types can be functionally coupled in certain neuronal pathways. | ||||||
Nickel(II) chloride | 7718-54-9 | sc-236169 sc-236169A | 100 g 500 g | $68.00 $188.00 | ||
Nickel chloride non-selectively inhibits several types of voltage-gated calcium channels, including R-type. It binds to the extracellular side of the channel, causing inhibition of calcium influx through R-type calcium channel α1E. | ||||||
Amiloride | 2609-46-3 | sc-337527 | 1 g | $296.00 | 7 | |
Amiloride indirectly inhibits R-type calcium channels α1E by modulating the function of sodium channels and sodium-calcium exchangers, which in turn affects intracellular calcium levels and the driving force for calcium entry through R-type channels. | ||||||
Cadmium chloride, anhydrous | 10108-64-2 | sc-252533 sc-252533A sc-252533B | 10 g 50 g 500 g | $56.00 $183.00 $352.00 | 1 | |
Cadmium chloride is a heavy metal salt that can inhibit R-type calcium channels α1E by binding to specific sites on the channel, leading to a block of the calcium-conducting pore. | ||||||
ω-Agatoxin IVA | 145017-83-0 | sc-302015 | 100 µg | $463.00 | ||
ω-Agatoxin IVA is a toxin that preferentially blocks P/Q-type calcium channels but has also been shown to inhibit R-type calcium channels α1E at higher concentrations by binding to the channel and obstructing calcium entry. | ||||||
Nifedipine | 21829-25-4 | sc-3589 sc-3589A | 1 g 5 g | $59.00 $173.00 | 15 | |
Nifedipine is a dihydropyridine compound that predominantly inhibits L-type calcium channels but may indirectly inhibit R-type calcium channels α1E by modulating overall calcium homeostasis and membrane potentials, which could alter the activity of R-type channels. | ||||||
Verapamil | 52-53-9 | sc-507373 | 1 g | $374.00 | ||
Verapamil is a phenylalkylamine that primarily inhibits L-type calcium channels, but can also indirectly inhibit R-type calcium channels α1E by changing intracellular calcium levels and cell excitability, which could reduce the contribution of R-type channels in electrical signaling. | ||||||
Diltiazem | 42399-41-7 | sc-204726 sc-204726A | 1 g 5 g | $209.00 $464.00 | 4 | |
Diltiazem is a benzothiazepine that blocks L-type calcium channels and can indirectly inhibit R-type calcium channels α1E by influencing the overall calcium signaling and excitability of cells, which affects the functional activity of R-type channels. | ||||||