voltage-gated potassium

Amifampridine (3,4-Diaminopyridine) is primarily used to treat rare muscle diseases. It blocks potassium channel efflux in nerve terminals, increasing action potential duration, which allows Ca2+ channels to remain open longer and enhances acetylcholine release to stimulate muscles at the end plate.

RY785 is a potent and selective inhibitor of voltage-gated potassium channels, such as KV2.2 (IC50 = 50 nM). This compound may be used in pain relief studies.

Kv3 modulator 1 is an imidazolidinedione-type orthosteric modulator of Kv3 voltage-gated potassium channels. Kv3 modulator 1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and sustained, dose-dependent effects. Kv3 modulator 1 can be used to study the mechanisms underlying inflammatory pain and neurological disorders such as epilepsy and schizophrenia.

Hymenidin, an alkaloid isolated from the Okinawan sponge Hymeniacidon sp. is a 5-hydroxytryptaminergic receptor antagonist and voltage-gated potassium channel inhibitor with potential antiprotozoal effects.It selectively binds to FOXO1 DNA and reduces depolarization-induced elevation of cellular calcium.

Amiodarone hydrochloride is an anti-anginal agent and a class III antiarrhythmic drug that inhibits potassium channels (including wild-type hERG channels and their tail currents, with an IC₅₀ of approximately 45 nM) as well as voltage-gated sodium channels. This leads to prolonged action potential duration in ventricular and atrial myocytes, resulting in reduced heart rate and vascular resistance. It activates ERK1/2 and p38 MAPK signaling pathways in fibroblasts, promoting cell proliferation and myofibroblast differentiation. Amiodarone hydrochloride is widely used in the study of supraventricular and ventricular arrhythmias and can also be used to establish pulmonary fibrosis animal models.

Tetrandrine (Sinomenine A) is a naturally occurring biphenylisoquinoline alkaloid, a calcium channel inhibitor. Tetrandrine inhibits voltage-gated calcium channels (ICa) and Ca2+-activated potassium channels.

Hymenidin HCl is a natural alkaloid isolated from Hymeniacidon sp. and acts as a serotonin (5-HT) receptor antagonist. Hymenidin HCl inhibits voltage-gated potassium channels (Kv), exhibits selective inhibition of CDK5, affects cellular signaling, and induces apoptosis in cancer cells.

UK 78282 hydrochloride, a novel potent and selective Kv1.3 blocker.UK 78282 hydrochloride inhibits Kv1.3 voltage-gated potassium channels and suppresses human T cell activation.

Meclofenamic acid (Meclofenamate) is a non-selective gap-junction blocker and a selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, with notable anti-inflammatory activities.

RY796 is a selective voltage-gated potassium (KV2) channel inhibitor that inhibits KV2.1 and KV2.2, used in research on neurological disorders.

D-myo-Inositol-1,3,4,5-tetrakisphosphate potassium enhances extracellular calcium (Ca2+) influx by upregulating voltage-gated calcium channels.

(S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide (N-Docosahexacnoylethanolamide(22:6)) is a homologue of dehydroepiandrosterone (DHEA). This compound can block Shaker-related voltage-gated potassium channels and inhibits Kv1.2 K+ currents with an IC50 value of 1.5 μM.

Quinidine methiodide is a quaternized derivative of quinidine and a classical ion channel blocker. Unable to penetrate the blood-brain barrier, it prolongs action potential duration by exclusively blocking voltage-gated sodium and potassium channels on peripheral membranes, acting as a benchmark tool in neuromuscular and cardiovascular electrophysiology research.

QO-83, a retigabine analog, is an activator of the voltage-gated potassium channel KCNQ2 (Kv7.2) with an EC50 of 0.56 μM. It binds to a single hydrophobic pocket of the KCNQ2-CaM complex in a closed conformation. QO-83 shifts the voltage-dependent activation curve of the KCNQ2 channel negatively, enhancing the channel's voltage sensitivity, and can be utilized in epilepsy research.

KV7 (KCNQ) voltage-gated potassium channels blocker

β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014)

Water-soluble salt of lamotrigine . Displays anticonvulsant effects and inhibits glutamate release, possibly through inhibition of Na+, K+ and Ca2+ currents. Leach et al (1991) Neurochemical and behavioral aspects of lamotr. Epilepsia 32 S4 PMID:1685439 |Smith and Meldrum (1995) Cardioprotective effect of lamotr. after focal ischemia in rats. Stroke 26 117 PMID:7839380 |Zona and Avoli (1997) Lamotrigine reduces voltage-gated sodium currents in rat central neurons in culture. Epilepsia 38 522 PMID:9184596 |Grunze et al (1998) Modulation of calcium and potassium currents by lamotr. Neuropsychobiology 38 131 PMID:9778600

Photoswitchable Kv channel blocker (IC50 values are 2 and 64 μM at 500 nm and 380 nm respectively). Switches conformation from cis to trans at 500 nm and trans to cis at 380 nm. Exhibits minimal activity at Nav1.2 and L-type Ca2+ channels. Stimulates action potential firing of hippocampal neurons in vitro at 500 nm and restores visual responsiveness in blind mice at 380 nm. Fortin et al (2008) Photochemical control of endogenous ion channels and cellular excitability. Nat.Methods 5 331 PMID:18311146 |Polosukhina et al (2012) Photochemical restoration of visual responses in blind mice. Neuron 75 271 PMID:22841312 |Banghart et al (2009) Photochromic blockers of voltage-gated potassium channels. Angew.Chem.Int.Ed. 48 9097 PMID:19882609

DAD is an ion channel blocker (blocks voltage-gated potassium channels) and is a third generation photoelectric switch that responds to visible light.

DAD dichloride is an ion channel blocker that blocks voltage-gated potassium channels, a third-generation photoelectric switch that responds to visible light, and can be used to study visual function.

PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-typ

Huwentoxin XVI TFA, a potent analgesic derived from the Chinese tarantula Ornithoctonus huwena, acts as a highly reversible and selective antagonist of mammalian N-type calcium channels (IC 50 of ~60 nM), with no impact on voltage-gated T-type calcium channels, potassium channels, or sodium channels [1].

Dendrotoxin-I, a neurotoxin from Dendroaspis snake venom, potently blocks K⁺ channels, specifically targeting voltage-gated potassium channel subunits KV1.1 and KV1.2 [1] [2] [3].

Jingzhaotoxin-IX is a C-terminally amidated peptide neurotoxin consisting of 35 amino acid residues. It inhibits both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms of voltage-gated sodium channels, as well as the Kv2.1 channel. However, Jingzhaotoxin-IX does not affect the delayed rectifier potassium channels Kv1.1, Kv1.2, and Kv1.3 [1].