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Suzetrigine (developmental code name VX-548) is a non-opioid, small-molecule analgesic that works as a selective inhibitor of Na v 1.8-dependent pain-signaling pathways in the peripheral nervous system. [1] [2] It is being developed by Vertex Pharmaceuticals and has completed two phase 3 clinical trials. [1] [3]
Note that an ion channel may overlap between different categories. Some channels conduct multiple ion currents and some are gated by multiple mechanisms. Examples of targets for modulators include: Voltage-gated ion channels. Calcium channel: see also Calcium channel blocker, Calcium channel opener
Although the early studies on the biophysics of Na V 1.8 channels were carried out in rodent channels, more recent studies have examined the properties of human Na V 1.8 channels. Notably, human Na V 1.8 channels exhibit an inactivation voltage-dependence that is even more depolarized than that in rodents, and it also exhibits a larger ...
A channel opener, also known as a channel activator, is a type of drug which facilitates ion flow through ion channels. They include the following: Potassium channel openers; Calcium channel openers; Sodium channel openers; Chloride channel openers
Sodium channel blockers are also used as local anesthetics and anticonvulsants. [5] Sodium channel blockers have been proposed for use in the treatment of cystic fibrosis, [6] but current evidence is mixed. [7] It has been suggested that the analgesic effects of some antidepressants may be mediated in part via sodium channel blockade. [8]
A sodium channel opener is a type of drug which facilitates ion transmission through sodium channels.. Examples include toxins, such as aconitine, veratridine, batrachotoxin, robustoxin, palytoxin and ciguatoxins and insecticides (DDT and pyrethroids), which activate voltage-gated sodium channels (VGSCs), and solnatide (AP301), which activates the epithelial sodium channel (ENaC).
Sodium channel inhibitors are used as both antiepileptics and antiarrhythmics, as they can inhibit the hyper-excitable tissues in a patient. [22] Introducing specific sodium channel blockers into a tissue allows for the preferential binding of the blocker to sodium channels, which results in an ultimate inhibition of the flow of sodium into the ...
The epithelial sodium channel (ENaC), (also known as amiloride-sensitive sodium channel) is a membrane-bound ion channel that is selectively permeable to sodium ions (Na +).It is assembled as a heterotrimer composed of three homologous subunits α or δ, β, and γ, [2] These subunits are encoded by four genes: SCNN1A, SCNN1B, SCNN1G, and SCNN1D.