Benzenesulfonamides act as open-channel blockers on KV3.1 potassium channel

Bassetto, Carlos Alberto Z.; Passianoto, Luana Vitorino Gushiken; Gonzalez, E R; Varanda, Wamberto Antônio

doi:10.1007/s00726-018-2669-5

Cited by 1 publication

(2 citation statements)

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“…The fast inactivation of VGSCs may mask or even prevent an open state blockade by ANE. This problem is elegantly featured in previous works [25][26][27][28]. Our data indicate related acceleration of the I Na+ inactivation process, but in that case, we can more safely interpret these data as indicating stronger binding to the inactive states of the VGSCs, as discussed below.…”

Section: Discussionsupporting

confidence: 81%

“…The blockade induced by ANE on these currents is fully reversible and strongly concentration-dependent, as seen in the Hill slope of ~16. These data show that ANE may modulate cell excitability with similar potency to other terpenes and terpenoids of similarly small chemical structures, such as estragole [9], eugenol [22][23][24][25][26], and carvacrol [27,28]. Furthermore, our data show that ANE blocked I Na+ through a mechanism that is like that of lidocaine (a well-known local anesthetic), a blockade that includes binding to the resting and inactive states of the VGSCs [29].…”

Section: Discussionsupporting

confidence: 62%

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State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na+ Channels by Anethole

Moreira-Junior,

Leal-Cardoso,

Cassola

et al. 2024

IJMS

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Anethole is a phenolic compound synthesized by many aromatic plants. Anethole is a substance that humans can safely consume and has been studied for years as a biologically active molecule to treat a variety of conditions, including nerve damage, gastritis, inflammation, and nociception. Anethole is thought to carry out its biological activities through direct interaction with ion channels. Anethole is beneficial for neurodegenerative Alzheimer’s and Parkinson’s diseases. Nevertheless, nothing has been investigated regarding the effects of anethole on voltage-gated Na+ channels (VGSCs), which are major players in neuronal function. We used cultured dorsal root ganglion neurons from neonatal rats as a source of natively expressed VGSCs for electrophysiological studies using the whole-cell patch-clamp technique. Our data show that anethole interacts directly with VGSCs. Anethole quickly blocks and unblocks (when removed) voltage-activated Na+ currents in this preparation in a fully reversible manner. Anethole’s binding affinity to these channels increases when the inactive states of these channels are populated, similar to lidocaine’s effect on the same channels. Our data show that anethole inhibits neuronal activity by blocking VGSCs in a state-dependent manner. These findings relate to the putative anesthetic activity attributable to anethole, in addition to its potential benefit in neurodegenerative diseases.

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Section: Discussionsupporting

confidence: 81%