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An epithelial sodium channel blocker is a sodium channel blocker that is selective for the epithelial sodium channel. An example is amiloride , which is used in the treatment of hypertension . [ 1 ]
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]
For example, TTX can bind and inactivate voltage-gated sodium channels, despite the fact that TTX is much larger and chemically different than sodium ions. Given the disparities in size and chemical properties between TTX and a sodium ion, this is an example of structure being used to block usually specific channels.
Evenamide (INN Tooltip International Nonproprietary Name) (developmental code names NW-3509, NW-3509A) [1] is a selective voltage-gated sodium channel blocker, including (and not limited to) subtypes Na v 1.3, Na v 1.7, and Na v 1.8, which is described as an antipsychotic and is under development by Newron Pharmaceuticals as an add-on therapy for the treatment of schizophrenia.
A positively charged region between the III and IV domains of sodium channels is thought to act in a similar way. [9] The essential region for inactivation in sodium channels is four amino acid sequence made up of isoleucine, phenylalanine, methionine and threonine (IFMT). [13] The T and F interact directly with the docking site in the channel ...
Examples of targets for modulators include: Voltage-gated ion channels. Calcium channel: see also Calcium channel blocker, Calcium channel opener; Potassium channel: see also Potassium channel blocker, Potassium channel opener; Sodium channel: see also Sodium channel blocker, Sodium channel opener
Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects that is related to oxcarbazepine. [1] It is an active metabolite of oxcarbazepine . [ 1 ] [ 2 ] In addition, an enantiomer of licarbazepine, eslicarbazepine (( S )-(+)-licarbazepine), is an active metabolite of eslicarbazepine acetate .
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).