voltage-gated na+ channel

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.

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.

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

Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na+ channel(IC50 of 0.8 mM tested with a potential of +30 mV).

QAQ dichloride is a photoswitchable compound that blocks voltage-gated Na v and K v channels. Its channel-blocking activity is observed in the trans form of the azobenzene photoswitch, while the cis form does not exhibit this effect. This compound is membrane-impermeant and selectively enters pain-sensing neurons expressing endogenous import channels. QAQ dichloride functions as a light-sensitive analgesic and provides a valuable tool for investigating signaling mechanisms involved in acute and chronic pain [1] [2].

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.

Brevetoxin-3 (PbTx-3) is a potent allosteric activator of voltage-gated Na+ channels, exhibiting a high affinity for site 5 and inhibiting the inactivation of these channels.

Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca2+ channel gating inhibitor with a dissociation constant (Kd) of 15 nM for the Cav3.1 (α1G T-type) Ca2+ channel. It exhibits high-affinity interactions with native neuronal high-threshold L-type, N-type, and P-type Ca2+ channels in both central and peripheral neurons and displays cross-reactivity with the voltage-gated Na+ channel [1].

ProTx-III, a spider venom peptide derived from the Peruvian green velvet tarantula, functions as a selective and potent inhibitor of the voltage-gated sodium channel Na v 1.7, exhibiting an IC 50 of 2.1 nM. Characterized by its inhibitor cystine knot motif (ICK), ProTx-III can attenuate the pain response and is applicable in research on chronic pain, epilepsy, and arrhythmia [1].

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

Nav1.3 Channel Inhibitor 1 (Compound 15b) is a state-dependent inhibitor of the voltage-gated sodium channel Na v 1.3, with an IC50 value of 20 nM. It has the ability to cross the blood-brain barrier, making it applicable for research into nervous system disorders [1].

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM 40% & 20 μM 60% at pH 9.0, 5 nM 28% & 3 μM 72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM 39% & 10 μM 61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1 2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

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)

Licarbazepine (10,11-hydroxy-10,11 Dihydrocarbamezer) is the pharmacologically active metabolite of oxcarbazepine, a drug indicated for the treatment of partial seizures and bipolar disorders.

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