na channels

Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

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

λ-Cyhalothrin (Icon) is a type II synthetic pyrethroid insecticide featuring a high-efficiency, broad-spectrum formula with an α-cyano group. It is employed across various applications for controlling a wide array of pests. As a neurotoxin, λ-Cyhalothrin acts on sodium channels in neuron membranes within the central nervous system.

Mebeverine hydrochloride (Colofac Hydrochloride), a β-phenylethylamine derivative, is a potent α1 repector inhibitor, relaxing the muscles in and around the gut.

Ropivacaine (LEA-103 HCl) is a local anaesthetic drug belonging to the amino amide group.

E 0747 (E0747) is a new antiarrhythmic compound that inhibits arrhythmias by inhibiting Na channels in cardiac cells.

SM-6586 is a potent calcium channel antagonist with inhibitory effects on Na+/H+ and Na+/Ca2+ exchange channels, and can be used in the study of cerebrovascular disease and hypertension, among other diseases.

Raxatrigine (CNV 1014802) has been investigated for the treatment of Bipolar Disorder and Bipolar Depression.

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

Ralfinamide mesylate (FCE-26742A (mesylate)) is an orally available Na+ channel blocker.

Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.

Bepridil hydrochloride (CERM 1978) is a calcium channel blocker and also inhibits Na+/Ca2+ exchange (NCX), sodium channels and cardiac sarcolemmal KATP channels.

A-803467 is a selective NaV1.8 channel blocker.

EIPA (L593754) (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Ranolazine (RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level.

Carbamazepine (NSC-169864) is a tricyclic compound chemically related to tricyclic antidepressants (TCA) with anticonvulsant and analgesic properties. Carbamazepine exerts its anticonvulsant activity by reducing polysynaptic responses and blocking post-tetanic potentiation. Its analgesic activity is not understood; however, carbamazepine is commonly used to treat pain associated with trigeminal neuralgia.

Articaine hydrochloride (Hoe-045) is a thiophene-containing local anesthetic pharmacologically similar to MEPIVACAINE.

ATX-II TFA, a specific Na+ channel modulator toxin, is derived from the venom of the sea anemone (Anemonia sulcata). This compound impedes the inactivation of Na+ channels and has been associated with arrhythmogenesis in the pulmonary vein and atrial fibrillation [1] [2]. It interacts with halothane, caffeine, and ryanodine in this modulation.

Benzocaine is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.

Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator. Brevetoxin-3 has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels.

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

Iota-conotoxin RXIA, an agonist of voltage-gated sodium channels (Na v 1.2, 1.6, 1.7), has been shown to induce repetitive action potentials and seizure in the motor axons of frogs following intracranial injection in mice [1].

Cd1a, a β-toxin from the African spider Ceratogyrus darlingi, modulates calcium ion channels and inhibits human calcium ion channels (Ca v 2.2)(IC 50 2.6 μM) as well as mouse sodium ion channels (Na v 1.7). This compound has potential applications in creating drugs for the treatment of peripheral pain [1].

Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain.

Ralfinamide (Priralfinamide) is an orally available Na-channel blocker for the treatment of neuropathic pain and other pain conditions.

Sodium ionophore III (ETH2120) is a Na+ ionophore suitable for the test of sodium activity in plasma, serum, and blood.

Prilocaine hydrochloride (Prilocaine HCl) is a local anesthetic of the amino amide type, binds to voltage-gated sodium ion channels in the neuronal membrane, thereby preventing the permeability of sodium ions.

ATX-II, an Na+ channel modulator toxin derived from the sea anemone (Anemonia sulcata), causes delayed inactivation of the Na+ channels and has been linked to pulmonary vein arrhythmogenesis and atrial fibrillation [1] [2]. It exhibits interaction with halothane, caffeine, and ryanodine.

6-Benzoylheteratisine (Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth) is a Aconitum alkaloid. It can inhibits voltage-gated Na+ channels in rat brain synaptosomes

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

QX-222 chloride (Lidocaine N-Methyl Hydrochloride) is a sodium channel blocker.

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

Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor, which is the pure S(-)-enantiomer of bupivacaine. It was utilized as a long-acting local anesthetic.

E 0747 FA is an antiarrhythmic compound that inhibits the voltage of action potential Vmax in Purkinje fibers of porcine heart.E 0747 FA inhibits Na channels in cardiac cells.

Nicainoprol (RU-42924) is a fast-sodium-channel blocking drug. Nicainoprol is a potent antiarrhythmic agent.

Triamterene is a pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.

Phenamil is an irreversible inhibitor of amiloride-sensitive Na channels; derivative of amiloride, synergizing bone formation with BMP2 and inhibits BMP2 induced cyst-like bone formation.

GS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ).

LY393615 (NCC1048) is a novel blocker of both neuronal Ca²⁺ (calcium) and Na⁺ (sodium) channels, exhibiting half-maximal inhibitory concentrations (IC₅₀) of 1.9 µM and 5.2 µM against α1A and α1B calcium channel subunits, respectively. This compound demonstrates effective brain penetration and has shown neuroprotective effects in cerebral ischemia models, suggesting its utility in neurological disease research [1].

Ajmaline (Cardiorythmine) is a class Ia anti-arrhythmic compound that is widely used for the diagnosis of Brugada syndrome and the acute treatment of atrial or ventricular tachycardia. Ajmaline inhibits cardiac Kv1.5 and Kv4.3 channels at therapeutic concentrations.

Dibucaine hydrochloride (Cinchocaine hydrochloride), a long-acting local amide anestheticsis, is usually used for surface anesthesia.

Ranolazine dihydrochloride (Ranolazine 2HCl) , an antianginal agent, can treat arrhythmia via a novel mechanism of action (inhibition of the late phase of the inward sodium current), and do not affect blood pressure or heart rate.

3',4'-Dichlorobenzamil HCl is an inhibitor of Na+ transport, Na+/Ca2+ exchanger, sarcoplasmic reticulum Ca2+ release channels.