Sodium Channel

Clopamide (Brinaldix) is a piperidine and sulfamoylbenzamide-based diuretic with thiazide-like diuretic activity.

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

Rufinamide (E 2080), a triazole derivative, is used as voltage-gated sodium channel blocker for the treatment of seizure disorders.

Lifarizine FA is a sodium channel blocker used in the treatment of neurological disorders and cardiovascular diseases, study of stroke.

Applications Zonisamide-13C2-15N is the labeled analogue of Zonisamide (Z700000), a sulfonamide antiseizure agent; blocks repetitive firing of voltagesensitive sodium channels and reduces voltage-sensitive T-type calcium currents. Heterocyclic methanesulfonide with anticonvulsant properties. The compound is under investigation for potential therapeutic use as an antiepileptic drug. Anticonvulsant. References Masuda, Y., et al.: Arzneim.-Forsch., 30, 477 (1980); Hammond, E.J., et al.: Gen. Pharmacol., 18, 303 (1987); Schmidt, D., et al.: Epilepsy Res., 15, 67 (1993); Sorkin, E.M., et al.: Drugs, 45, 760 (1993)

Stability Light and Moisture Sensitive Applications Isotope Labelled analogue of rac-Kavain (K145490), the main kavalactone found in the roots of the kava plant. Kavain is known to exhibit anticonvulsive properties by attenuating vascular smooth muscle contraction through interactions with voltage-dependent sodium and calcium channels. rac-Kavain was shown in recent research to exhibit protective properties on anaerobic glycolysis, ATP content and intracellular calcium and sodium of anoxic brain vesicles. References Gleitz, J., et al: Neuropharmacol., 35, 1743 (1997); Hashimoto, T., et al.: Phytomedicine, 10, 309 (2003); Mulholland, P.J., et al.: Brain. Res., 945, 106 (2002);

Applications A derivative of Vincamine with vasodilating activity. Vasodilator (cerebral). References Han, et al.: J. Biol. Chem., 274, 22337 (1999), O’Donnell, et al.: Pharmacol. Biochem. Behav., 63, 185 (1999)

TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.

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

Applications Pentisomide is a sodium channel blocker; derivative of disopyramide. Antiarrhythmic (class I). References Kuhlkamp, V., et al.: Int. J. Cardiol., 36, 69 (1992), Yuan, S., et al.: Cardiovasc. Drug Rev., 11, 74 (1993)

Ancistrotecine B (Compound 2), a Nav1.7 channel inhibitor (IC50: 0.73 μM), has been shown to alleviate inflammatory pain in mice [1].

5-Tridecanol blocks ion flux in sodium channels.

Applications 2,6-Dichloro-N-(2,6-dimethylphenyl)hexanamide is an impurity of the local anesthetic Levobupivacaine (B689546).

6-Iodoamiloride is a potent inhibitor of acid-sensing ion channel 1 (ASIC1), exhibiting an IC50 value of 88 nM.

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

Ajmaline, a class Ia anti-arrhythmic, diagnoses Brugada syndrome and treats tachycardia; inhibits cardiac Kv1.5/Kv4.3 channels.

6-Benzoylheteratisine (Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth) is a Aconitum alkaloid.

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

Oxybuprocaine hydrochloride (Oxybuprocaine HCl), a local anesthetic, is used especially in otolaryngology and ophthalmology.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive