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Na+ channel blocker
Amiloride hydrochloride is a Na+ channel blocker, also inhibits TRPP3 channels and Na+/H+ exchanger (NHE).- Yu Y, .et al. , Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thomas D. Williams, .et al. , J Cell Sci, 2018, Mar 15; 131(6): jcs213736 PMID: 29440238
- Bupivacaine is a more potent inhibitor of cAMP production than are chemically related local anesthetics that are less prone to produce cardiovascular toxicity.
- Carbamazepine is an anticonvulsant and mood-stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder, as well as trigeminal neuralgia.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
- Lidocaine (Alphacaine) is an anasthetic and class Ib antiarrhythmic agent. Blocks voltage-gated sodium channels in the inactivated state.
- Phenytoin sodium (Dilantin) is a sodium channel protein inhibitor.
- Riluzole preferentially blocks TTX-sensitive sodium channels, which are associated with damaged neurons.This reduces influx of calcium ions and indirectly prevents stimulation of glutamate receptors.
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SGLT2 inhibitor
PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2. -
PDE1 inhibitor
Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor. -
NMDA receptor antagonist
Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. -
Voltage-gated sodium channels antagonist
Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM. - Amiloride hydrochloride dihydrate is a potent epithelial sodium channel blocker and selective low threshold (T-type) calcium channel protein inhibitor (KD=30μM).
- Ibutilide 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. It exerts its antiarrhythmic effect by induction of slow inward sodium current, which prolongs action potential and refractory period (physiology) of myocardial cells.
- 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.
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Nav inhibitor
Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM. -
Sodium channel blocker
Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent. -
glutamate release inhibitor
Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke. -
Sodium channel blocker
Raxatrigine (GSK1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. In rats, GSK1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (PCP) in a dose-dependent way, which suggested the potential of GSK1014802 in the treatment of cognitive symptoms of schizophrenia. GSK2 was also a potent inhibitor of human MAO-B with pIC50 value of 7.96 but did not inhibit human MAO-A. -
voltage-gated sodium channel Nav1.7 inhibitor
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration. -
Sodium channel Blocker
QX 314 chloride is a membrane impermeable quaternary derivative of lidocaine, a voltage-activated Na+ channel blocker -
NaV1.3 and NaV1.1 channels inhibitor
ICA-121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). -
Sodium channel blocker
Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative. -
Sodium channel blocker
Disopyramide is an antiarrhythmic (class IA) and a sodium channel blocker.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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sodium channel protein inhibitor
Oxcarbazepine is a sodium channel protein inhibitor. -
Sodium channel blocker/DNMT inhibitor
Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor. -
sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- 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.
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Cardiac Na+ channel blocker
Flecainide is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential. -
Sodium Channel inhibitor
Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment. -
Ion channel blocker
Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.- Joe Z.Zhang, .et al. , Cell Stem Cell, 2019, 24, 1-10 PMID: 30880024
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Slows neuronal Na+ channel inactivation
beta-Pompilidotoxin is a peptide with the sequence H2N-Arg. -
sodium channel inhibitor
Levobupivacaine is a local anaesthetic drug belonging to the amino amide group. - Benzocaine hydrochloride is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.
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Sodium Channel Blocker
Pilsicainide is a water soluble selective Na+ channel blocker. -
Nav1.7 Inhibitor
PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV. -
Sodium Channel inhibitor
AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 uM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
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SChE inhibitor
Dibucaine (USAN) is an amide local anesthetic. Dibucaine reversibly binds to and inactivates sodium channels in the neuronal cell membrane. Inhibition of sodium channels prevents the depolarization of nerve cell membranes and inhibits subsequent propagation of impulses along the course of the nerve, thereby limiting the excitation of nerve endings. This results in loss of sensation. -
5-HT receptor /dopamine receptors antagonist
Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors. -
NaV1.8 blocker
PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile. -
Sodium channel blocker
Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker. -
SLC13A5 inhibitor
BI01383298 is a potent inhibitor of SLC13A5, being selective over other family members and other transporters.