Sodium Channel

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S1614

Riluzole

Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

S2454

Bupivacaine HCl

Bupivacaine HCl binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, used for treating cardiac arrhythmias.

S1811

Amiloride HCl

Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).

S1256

Rufinamide

Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

S1603

Furosemide

Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used in the treatment of congestive heart failure and edema.

S4669New

Benzocaine hydrochloride

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

S4668New

Procaine

Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses.

S1445

Zonisamide

Zonisamide is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.

S2524

Phenytoin Sodium

Phenytoin Sodium is an inactive voltage-gated sodium channel stabilizer.

S1693

Carbamazepine

Carbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.

S2785

A-803467

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.

S2560

Amiloride HCl dihydrate

Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.

S2525

Phenytoin

Phenytoin is an inactive voltage-gated sodium channel stabilizer.

S2874

Camostat Mesilate

Camostat is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.

S2114

Dronedarone HCl

Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).

S3024

Lamotrigine

Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.

S4016

Ouabain

Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.

S1965

Primidone

Primidone is an anticonvulsant of the pyrimidinedione class.

S3064

Ambroxol HCl

AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.

S2500

Propafenone HCl

Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.

S4023

Procaine HCl

Procaine is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.

S4038

Dibucaine HCl

Dibucaine HCl is a local anesthetics.

S1391

Oxcarbazepine

Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.

S4058

Ropivacaine HCl

Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.

S4180

Nefopam HCl

Nefopam HCl is a centrally-acting but non-opioid analgesic drug by blocking voltage-gated sodium channel and inhibition of serotonin, dopamine and noradrenaline reuptake.

S4061

Levobupivacaine HCl

Levobupivacaine HCl, the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.

S4080

Triamterene

Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.

S4200

Tolperisone HCl

Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.

S4210

Benzocaine

Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.

S4225

Mexiletine HCl

Mexiletine HCl belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.

S2110

Vinpocetine

Vinpocetine is a selective inhibitor of voltage-sensitive sodium channel for the treatment of stroke, vascular dementia and Alzheimer's disease.

S4290

Digoxin

Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.

S2118

Ibutilide Fumarate

Ibutilide Fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current, which prolongs action potential and refractory period of myocardial cells.

S4294

Procainamide HCl

Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.

S1828

Proparacaine HCl

Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.

Catalog No. Information Product Use Citations Product Validations
S1614

Riluzole

Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

S2454

Bupivacaine HCl

Bupivacaine HCl binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, used for treating cardiac arrhythmias.

S1811

Amiloride HCl

Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).

S1256

Rufinamide

Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

S1603

Furosemide

Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used in the treatment of congestive heart failure and edema.

S4669New

Benzocaine hydrochloride

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

S4668New

Procaine

Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses.

S1445

Zonisamide

Zonisamide is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.

S2524

Phenytoin Sodium

Phenytoin Sodium is an inactive voltage-gated sodium channel stabilizer.

S1693

Carbamazepine

Carbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.

S2785

A-803467

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.

S2560

Amiloride HCl dihydrate

Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.

S2525

Phenytoin

Phenytoin is an inactive voltage-gated sodium channel stabilizer.

S2874

Camostat Mesilate

Camostat is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.

S2114

Dronedarone HCl

Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).

S3024

Lamotrigine

Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.

S4016

Ouabain

Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.

S1965

Primidone

Primidone is an anticonvulsant of the pyrimidinedione class.

S3064

Ambroxol HCl

AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.

S2500

Propafenone HCl

Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.

S4023

Procaine HCl

Procaine is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.

S4038

Dibucaine HCl

Dibucaine HCl is a local anesthetics.

S1391

Oxcarbazepine

Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.

S4058

Ropivacaine HCl

Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.

S4180

Nefopam HCl

Nefopam HCl is a centrally-acting but non-opioid analgesic drug by blocking voltage-gated sodium channel and inhibition of serotonin, dopamine and noradrenaline reuptake.

S4061

Levobupivacaine HCl

Levobupivacaine HCl, the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.

S4080

Triamterene

Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.

S4200

Tolperisone HCl

Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.

S4210

Benzocaine

Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.

S4225

Mexiletine HCl

Mexiletine HCl belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.

S2110

Vinpocetine

Vinpocetine is a selective inhibitor of voltage-sensitive sodium channel for the treatment of stroke, vascular dementia and Alzheimer's disease.

S4290

Digoxin

Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.

S2118

Ibutilide Fumarate

Ibutilide Fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current, which prolongs action potential and refractory period of myocardial cells.

S4294

Procainamide HCl

Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.

Catalog No. Information Product Use Citations Product Validations
S1828

Proparacaine HCl

Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.