Voltage-gated Sodium Channels and Blockers: An Overview and Where Will They Go?
Sign Up to like & getrecommendations! Published in 2019 at "Current Medical Science"
DOI: 10.1007/s11596-019-2117-0
Abstract: Voltage-gated sodium (Nav) channels are critical players in the generation and propagation of action potentials by triggering membrane depolarization. Mutations in Nav channels are associated with a variety of channelopathies, which makes them relevant targets… read more here.
Keywords: channels blockers; nav channels; gated sodium; sodium channels ... See more keywords
The tarantula toxin β/δ-TRTX-Pre1a highlights the importance of the S1-S2 voltage-sensor region for sodium channel subtype selectivity
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-01129-0
Abstract: Voltage-gated sodium (NaV) channels are essential for the transmission of pain signals in humans making them prime targets for the development of new analgesics. Spider venoms are a rich source of peptide modulators useful to… read more here.
Keywords: subtype selectivity; voltage; pre1a; nav channels ... See more keywords
Beyond lidocaine: selective voltage-gated sodium channel blockade for vaginal pain.
Sign Up to like & getrecommendations! Published in 2020 at "Pain"
DOI: 10.1097/j.pain.0000000000002037
Abstract: Female reproductive tract pain encompasses a variety of common and debilitating conditions such as vulvodynia, vaginal hyperalgesia secondary to endometriosis, pudendal neuralgia, and many others. These conditions lack effective pharmacotherapies due to a poor understanding… read more here.
Keywords: nav channels; ttx; channel; vaginal pain ... See more keywords
Structural basis of α-scorpion toxin action on Nav channels
Sign Up to like & getrecommendations! Published in 2019 at "Science"
DOI: 10.1126/science.aav8573
Abstract: How activation leads to gating Voltage-gated sodium (Nav) channels are key players in electrical signaling. Central to their function is fast inactivation, and mutants that impede this cause conditions such as epilepsy and pain syndromes.… read more here.
Keywords: nav channels; scorpion; vsd4; inactivation ... See more keywords
Development of Allosteric Modulators of Voltage-Gated Na+ Channels: A Novel Approach for an Old Target.
Sign Up to like & getrecommendations! Published in 2021 at "Current topics in medicinal chemistry"
DOI: 10.2174/1568026621666210525105359
Abstract: Given their primacy in governing the action potential (AP) of excitable cells, voltage-gated Na+ (Nav) channels are important pharmacological targets of therapeutics for a diverse array of clinical indications. Despite historically being a traditional drug… read more here.
Keywords: auxiliary proteins; nav channels; target; allosteric modulators ... See more keywords
Non-psychotropic phytocannabinoid interactions with voltage-gated sodium channels: An update on cannabidiol and cannabigerol
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Physiology"
DOI: 10.3389/fphys.2022.1066455
Abstract: Phytocannabinoids, found in the plant, Cannabis sativa, are an important class of natural compounds with physiological effects. These compounds can be generally divided into two classes: psychoactive and non-psychoactive. Those which do not impart psychoactivity… read more here.
Keywords: voltage gated; phytocannabinoid; nav channels; non psychoactive ... See more keywords
Tetrodotoxin Decreases the Contractility of Mesenteric Arteries, Revealing the Contribution of Voltage-Gated Na+ Channels in Vascular Tone Regulation
Sign Up to like & getrecommendations! Published in 2023 at "Marine Drugs"
DOI: 10.3390/md21030196
Abstract: Tetrodotoxin (TTX) poisoning through the consumption of contaminated fish leads to lethal symptoms, including severe hypotension. This TTX-induced hypotension is likely due to the downfall of peripheral arterial resistance through direct or indirect effects on… read more here.
Keywords: voltage gated; vascular tone; channels vascular; ttx ... See more keywords
Intrinsic mechanisms in the gating of resurgent Na+ currents
Sign Up to like & getrecommendations! Published in 2022 at "eLife"
DOI: 10.7554/elife.70173
Abstract: The resurgent component of the voltage-gated sodium current (INaR) is a depolarizing conductance, revealed on membrane hyperpolarizations following brief depolarizing voltage steps, which has been shown to contribute to regulating the firing properties of numerous… read more here.
Keywords: nav channels; gating resurgent; voltage; fast slow ... See more keywords