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Pharmacological blockers of INaP are used clinically in many of these disorders. Amiodarone, while primarily blocking the human Ether-a-go-go-Related Gene potassium channel, has shown to significantly reduce persistent sodium current by 50% in cortical neurons [14] as well as in cardiac sodium channel NaV1.5 and is used to treat arrhythmia. [15]
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]
Ion channels are typically categorised by gating mechanism and by the ion they conduct. 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
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 ...
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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 ]
Flecainide works by blocking the Nav1.5 sodium channel in the heart, slowing the upstroke of the cardiac action potential. [32] This thereby slows conduction of the electrical impulse within the heart, i.e. it "reduces excitability". The greatest effect is on the His-Purkinje system and ventricular myocardium. The effect of flecainide on the ...