Date published: 2025-9-16

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KCNT1 Activators

Quinidine, traditionally viewed as an antiarrhythmic due to its sodium channel blockage, exerts an inhibitory action on KCNT1 channels, which results in an atypical activation effect under specific conditions. Muscle relaxant Chlorzoxazone, on the other hand, directly activates KCNT1, leading to a boost in channel activity. In a similar vein, Riluzole, recognized for its neuroprotective effects, promotes the surface expression of KCNT1, thereby increasing channel activity.

Calcium channel blocker Bepridil and antifungal Ciclopirox both share the ability to activate KCNT1 channels, albeit via different binding interactions, resulting in increased potassium conductance. Bithionol, another activator, also modulates potassium ion flow through KCNT1 activation. Haloperidol activates KCNT1, which implicates potassium ion efflux. Anthelmintic agents like Niclosamide, by enhancing KCNT1 channel activation, impact the movement of potassium ions, an effect shared by the paradoxical activator Clofilium Tosylate. Diuretic Ethacrynic Acid's interaction with KCNT1 leads to a modulation of potassium transport, a function similarly altered by the NSAID Diclofenac through its activation of KCNT1 channels.

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