Sodium Channels

A 803467 is a selective blocker of NaV1.8 channels (IC50 values are 8, 2450, 6740, 7340 and 7380 nM for hNaV1.8, hNaV1.3, hNaV1.7, hNaV1.5 and hNaV1.2 channels respectively).

Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.

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.

Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor.

Digoxin is a sodium-potassium pump inhibitor.

GS967 is a novel, potent, and selective inhibitor of cardiac late sodium current(late INa); inhibits ATX-II-induced late I(Na) in ventricular myocytes and isolated hearts with IC(50) values of 0.13 and 0.21 uM, respectively.

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.

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.

Meticrane is a diuretic. Meticrane inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension.

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.

DSP-2230 is a selective Nav1.7/Nav1.8 blocker.

Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker.

Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.

Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.

Levobupivacaine hydrochloride is a sodium channel blocker.

Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators.