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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]
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 ...
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
NKTR-171 – voltage-gated sodium channel blocker [15] PF-05089771 – selective Na v 1.7 and Na v 1.8 blocker [16] Ralfinamide (NW-1029) – non-selective voltage-gated sodium channel blocker, as well as other actions [17] Tetrodotoxin (9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocker [18]
Sodium voltage-gated channel alpha subunit 9 (also Na v 1.7) is a sodium ion channel that, in humans, is encoded by the SCN9A gene. [5] [6] [7] It is usually expressed at high levels in two types of neurons: the nociceptive (pain) neurons at the dorsal root ganglion (DRG) and trigeminal ganglion; and sympathetic ganglion neurons, which are part of the autonomic (involuntary) nervous system.
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 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]
Potassium channel: see also Potassium channel blocker, Potassium channel opener; Sodium channel: see also Sodium channel blocker, Sodium channel opener; Chloride channel: see also Chloride channel blocker, Chloride channel opener; Transient receptor potential channel; Ligand gated ion channels. 5-HT3: see also 5-HT3 antagonist,