30 products were found matching "K04837"!

A conotoxin and an inhibitor of Nav1.4 receptors, inhibits Nav1.4 in HEK293 cells (IC50 = 2.3 nM for the rat channel), inhibits rat Nav1.2 channels in HEK293 cells at 500 nM and is an antagonist of a7 nAChRs and a4ß2 and a3ß2 subunit-containing nAChRs in Xenopus oocytes expressing the human receptors (IC50s = 22,...

Quinidine is a stereoisomer of the antimalarial agent quinine (Cay-23958) and a class Ia antiarrhythmic agent. Quinidine blocks the voltage-gated sodium (Nav) channel Nav1.5 in a use-dependent manner. It decreases the amplitude and duration of action potentials in isolated canine ventricular myocytes. It inhibits...

10,11-dihydro-10-hydroxy Carbamazepine is an antiepileptic agent and active metabolite of the prodrug oxcarbazepine (Cay-17340). It is a racemic mixture of (R)- and (S)-10,11-dihydro-10-hydroxy carbamazepine. (S)-10,11-dihydro-10-hydroxy Carbamazepine protects against seizures induced by maximal electroshock (MES)...

Flecainide is an inhibitor of cardiac late sodium current (INa, IC50 = 3.4 µM) and delayed-rectifier potassium current (IKr, IC50 = 1.5 µM). Formulations containing flecainide have been used in the treatment of arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart...

Fosphenytoin is a prodrug of phenytoin that is rapidly converted to phenytoin, a voltage-gated sodium channel blocker, in vivo. It induces less tissue damage compared with two other phenytoin prodrugs in rats following subcutaneous and intramuscular administration. Fosphenytoin has anticonvulsant activity in a mouse...

Lennox-Gastaut syndrome (LGS) is a severe pediatric epilepsy syndrome characterized by multiple seizure types. Rufinamide is an anticonvulsant. It inhibits the activation of voltage-gated sodium channel 1.1 (Nav1.1) when used at a concentration of 100 µM. Rufinamide inhibits Nav1.1, but not Nav1.2, Nav1.3, and...

Raxatrigine is an inhibitor of voltage-gated sodium channels (Nav, IC50s = 22, 13, 23, 10, 84, 15, 32, and 6 µM for Nav1.1-Nav1.8 channels in a FLIPR membrane potential assay using HEK293 cells). Its activity is state-dependent at the Nav1.7 channel, with a nine-fold increase in potency for the open/inactivated...

Oxcarbazepine is a prodrug form of the antiepileptic compound 10,11-dihydro-10-hydroxy carbamazepine (Cay-18467). It inhibits high-frequency repetitive firing of rat spinal cord neurons when used at a concentration of 1 µM. Oxcarbazepine protects against electroshock-induced tonic hindlimb extension (ED50 = 10-20...

Eslicarbazepine acetate is a sodium channel blocker (IC50 = 138 nM in a radioligand binding assay). It inhibits sodium uptake in a dose-dependent manner in rat cortical synaptosomes at concentrations ranging from 30-300 µM. In vivo, oral and i.p. administration of eslicarbazepine acetate is protective against...

Zonisamide is a broad-spectrum sulfonamide antiepileptic agent. It selectively blocks the repeated firing of sodium channels (IC50 = 2 µg/ml) at low concentrations in mouse embryo spinal cord neurons, and it blocks spontaneous channel firing at concentrations above 10 µg/ml. In rat cerebral cortex neurons,...

Pirmenol is a class I antiarrhythmic agent. It lengthens the final repolarization of action potentials in isolated rabbit ventricular myocytes and inhibits tachyarrhythmias induced by prolonged afterdepolarizations in isolated guinea pig papillary muscles when used at a concentration of 5 µM. Pirmenol (2.5 and 5...

Pramoxine is a local anesthetic. It reduces electrically induced peak compound action potential (CAP) amplitudes in isolated frog sciatic nerve (IC50 = 0.21 mM). Topical administration of pramoxine (0.35 and 0.6%) inhibits winking in a rabbit corneal test, indicating anesthetic activity. It inhibits the...