voltage-gated sodium channel

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.

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 .

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.

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.

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.

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.

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

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.

Mexiletine D6 hydrochloride is a non-selective voltage-gated sodium channel blocker,is a Class IB antianhythmic.

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

Nav1.7-IN-3 is a selective and orally bioavailable inhibitor of voltage-gated sodium channel Nav1.7(IC50 of 8 nM).

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.

Sodium Channel inhibitor1 is a novel and selective voltage-gated sodium channel for pain treatment. (IC50 Value of 0.16 uM and 0.41 uM for Na v1.7, V hold-90mV and Na v1.7, V hold-90mV)

AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.

Evenamide (NW-3509) is a sodium channel blocker. Which shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness.

Mexiletine is a non-selective voltage-gated sodium channel blocker. It is a medicine in the class of IB anti-arrhythmic. Mexiletine may also be used in patients experiencing refractory pain and is effective to treat muscle stiffness resulting from myotonic dystrophy or non-dystrophic myotonias.

Veratridine is a benzoate-cevane found in Veratrum and Schoenocaulon. It activates sodium channels to stay open longer than normal.

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

GX-674 is a highly potent and selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 value of 0.1 nM measured at -40 mV for the study of inflammatory and neuropathic pain.

voltage-gated sodium channel blocker

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.

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