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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]
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
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 tissue. Over time, this mechanism leads to an overall decrease in tissue excitation.
20264 Ensembl ENSG00000185313 ENSMUSG00000034533 UniProt Q9Y5Y9 Q6QIY3 RefSeq (mRNA) NM_001293306 NM_001293307 NM_006514 NM_001205321 NM_009134 RefSeq (protein) NP_001280235 NP_001280236 NP_006505 NP_001192250 NP_033160 Location (UCSC) Chr 3: 38.7 – 38.82 Mb Chr 9: 119.44 – 119.55 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Na v 1.8 is a sodium ion channel subtype that in ...
DPH-362 is a simplified amitriptyline analog created by omission of the two-carbon dibenzosuberane bridge (the seven membered ring). The resulting compound still had activity in a test to explore TCA sodium channel blockers with analgesic properties.
As the cardiac sodium channel is the most pH-sensitive sodium channel, most of what is known is based on this channel. Reduction in extracellular pH has been shown to depolarize the voltage-dependence of activation and inactivation to more positive potentials.
DSP-2230 is a selective small-molecule Na v 1.7 and Na v 1.8 voltage-gated sodium channel blocker which is under development by Dainippon Sumitomo Pharma for the treatment of neuropathic pain. [1] [2] As of June 2014, it is in phase I/phase II clinical trials. [1] [2]
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