voltage-gated sodium channel

Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.

PF-06305591 is an effective and selective blocker of voltage-gated sodium channel NaV1.8 (IC50 = 15 nM).

Phenytoin sodium (Diphantoine) is an inactive stabilizer for voltage-gated sodium channel .

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

Hemin (Hemin chloride) is a chlorinated iron-containing porphyrin, a heme oxygenase (HO)-1 inducer. Hemin has therapeutic activity in porphyrias by reducing heme deficiency in patients, thereby inhibiting δ-aminolevulinic acid synthetase activity through biochemical feedback.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Rufinamide (E 2080), a triazole derivative, is used as voltage-gated sodium channel blocker for the treatment of seizure disorders.

Primidone (NCI-C56360) is a potent anticonvulsant agent. It is a neuronal voltage-gated sodium channel blocker and has value in the study of epilepsy, essential tremor, and psychiatric disorders.

Mexiletine hydrochloride (KOE-1173 hydrochloride) is a voltage-gated sodium channel blocker and a Class IB antiarrhythmic drug. Mexiletine hydrochloride exerts antiarrhythmic effects by inhibiting sodium current in myocardial cells, thereby reducing the rise rate of cardiac action potential (phase 0) and reducing the automaticity of Purkinje fibers.

Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride (Proparacaine HCl) stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, and resulting in a loss of sensation.

Etidocaine Hydrochloride (W19053) is a long-acting anesthetic and a blocker of the voltage-gated sodium channel.

Co 102862 is a voltage-gated sodium channel blocker. Co 102862 can be used for anticonvulsant studies.

1-(2,4-difluorophenyl)guanidine hydrochloride is a compound that is a potent and selective inhibitor of the voltage-gated sodium channel Nav1.7, a key player in pain signaling. It is therefore able to reduce pain signaling, resulting in an analgesic effect.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective positive modulator of Nav1.1 channels and also increases the activity of Nav1.2 and Nav1.5 channels while not affecting Nav1.4, Nav1.6, and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

KGP-25 is an inhibitor of the voltage-gated sodium channel 1.8 (Nav1.8), utilized for analgesia by targeting the peripheral nervous system (PNS). Additionally, it targets the γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for use as a general anesthetic.

Batrachotoxin (BTX), a potent neurotoxin and cardiotoxin, is found in the skin of the Colombian dart frog (Phyllobates aurotaenia). As an activator of sodium channels (sodium channel), it interferes with normal sodium channel closure by binding to voltage-gated sodium channels (sodium channel) on the cell membrane. This interaction causes a continuous influx of sodium ions into the cells, leading to persistent depolarization.

Nav1.8-IN-5 (Example 1), a voltage-gated sodium channel Nav1.8 inhibitor, is applicable in the research of Nav1.8-mediated diseases including pain, pain-related disorders, and cardiovascular diseases (such as atrial fibrillation) [1].

DPI-201-106 is a cardioselective inhibitor of the TTX-resistant h1 Na channel inactivation. DPI-201-106 inhibits the L-type calcium current, and inward and delayed rectifier potassium currents.

Ceratotoxin-2 (CcoTx2) is a voltage-gated sodium channel inhibitor with half maximal inhibitory concentrations (IC50) of 8 nM for Na v 1.2 β 1 and 88 nM for Na v 1.3 β 1 [1].

Bupivacaine is a BK SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells. It acts by binding to the intracellular portion of voltage-gated sodium channels and blocking sodium influx into nerve cells.

VSTx-3 is a potassium voltage-gated channel (K_V) blocker, which has also been shown to be a potent tetrodotoxin-sensitive (TTX-sensitive) sodium channel inhibitor, with particular efficacy against NaV1.8 channels, as evidenced by its half-maximal inhibitory concentration (IC_50) values of 0.19 μM for hNaV1.3, 0.43 μM for hNaV1.7, and 0.77 μM for hNaV1.8 channels.

Poneratoxin acetate is the acetate form of Poneratoxin. It acts as a modulator of voltage-gated sodium channels (NaV, with EC50 values for NaV1.6 of 97 nM and 2.3 µM). This compound reduces the activation voltage threshold and inhibits channel inactivation, thereby enhancing neuronal excitability and contributing to the transmission of pain signals.

voltage-gated sodium channel blocker

3'-Methoxydaidzein is a dual isoflavone and Sodium Channel inhibitor. 3'-Methoxydaidzein inhibited NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM and 505 nM, respectively. 3'-Methoxydaidzein was specific for collagen-induced platelet aggregation with IC50 values of 12.3 and 61.5µM, respectively. 3'-Methoxydaidzein acts as an analgesic by inhibiting voltage-gated sodium channels. 3'-Methoxydaidzein showed antioxidant activity and antiplatelet aggregation activity.