Sodium Channel

SYM2206 is a low affinity non-competitive AMPA receptor antagonist with an IC50 value of 1.6 μM.SYM2206 exhibits anticancer activity by blocking Nav1.6-mediated

Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use as an adjunctive therapy for partial-onset seizures.

Applications 3-Deoxyyunaconitine is a metabolite of Aconitine (A189875), a neurotoxin that binds, activates tetrodotoxin-sensitive Na+ channels and prolongs the opening of the sodium-ion channel by suppressing conformational changes. References Derbre, S., et al.: Anal. Bioanal. Chem., 398, 1747 (2010), Li, M., et al.: J. Pharm. Biomed. Anal., 53, 1063 (2010),

Mepivacaine hydrochloride (Mepivacaine HCl) is the hydrochloride salt form of mepivacaine, an amide derivative with local anesthetic properties.

Stability Hygroscopic Applications Antiepileptic; increases levels of GABA in the brain. References Chang, Z.L., et al.: Anal. Profiles Drug Subs., 8, 529 (1979), Nau, H., et al.: Pharmacol. Toxicol., 69, 310 (1991), Loscher, W., et al.: Prog. Neurobiol., 58, 31 (1999)

Dibucaine hydrochloride (Cinchocaine hydrochloride), a long-acting local amide anestheticsis, is usually used for surface anesthesia.

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

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer.

Zoniporide (CP-597396) is an NHE-1 inhibitor that inhibits platelet swelling and can be used in the study of cardiovascular diseases.

Stability Light Sensitive Applications 2-Chloro-2',6'-dimethyl-d6-acetanilide is the labeled analogue of 2-Chloro-2',6'-dimethylacetanilide (C365375), an intermediate of Lidocaine (L397800), a local anesthetic; antiarrhythmic (class IB). Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic. References Moen, A., et al.: Biocatal. Biotransform., 23, 45 (2005); Yogeeswari, P., et al.: Bioorg. Med. Chem. Lett., 17, 3712 (2007); Duce, R., et al.: J. Pharmacol. Exp. Ther., 179, 580 (1971); Kronberg, G.H., et al.: J. Med. Chem., 16, 739 (1973); Groningsson, K., et al.: Anal. Profiles Drug Subs., 14, 207 (1985); Davies, P.S., et al.: Drugs, 64, 937 (2004)

Applications Antiepileptic triazole derivative which decreases firing by neurons at sodium channels. Anticonvulsant. Neuroprotective & Neuroresearch Product. References Cheung, W.K., et al.: Pharm. Res., 12, 1878 (1995), Cardot, J.-M., et al.: Biopharm. Drug Dispos., 19, 259 (1998), Palhagen, S., et al.: Epilepsy Res., 43, 115 (2001),

Phenytoin sodium (Diphantoine) is an inactive stabilizer for voltage-gated sodium channel .

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide.

Olorigliflozin is a sodium glucose co-transporter (SGLT) inhibitor with antihyperglycemic properties.

NHE3-IN-1 是钠/质子交换剂 3 (NHE-3) 的抑制剂。

Trapencaine is a newly synthesized carbamate type local anesthetic that induces conformational changes in sodium channels on hypertrophic cell membranes.

Applications Labelled Rufinamide (R701552). Antiepileptic triazole derivative which decreases firing by neurons at sodium channels. Anticonvulsant. References Cheung, W.K., et al.: Pharm. Res., 12, 1878 (1995), Cardot, J.-M., et al.: Biopharm. Drug Dispos., 19, 259 (1998), Palhagen, S., et al.: Epilepsy Res., 43, 115 (2001),

Applications Labelled analogue of a local anesthetic with stimulant properties. Studies have shown its potency to be about half that of Cocaine (C633500). References Wppdward, J.J. et al.: Eur. J. Pharmacol., 277, 7 (1995); Rigon, A.R. et al.: Psychopharmacol., 127, 323 (1996); Wilcox, K.M. et al.: Synapse, 58, 220 (2005);

Flecainide is a medication used to prevent and treat abnormally fast heart rates. This includes ventricular and supraventricular tachycardias.

Applications 4,4'-Dichlorodiphenyltrichloroethane - D8 is a synthetic organochlorine insecticide. 4,4'-Dichlorodiphenyltrichloroethane - D8 functions by opening sodium ion channels in the insects’ neurons, causing them to fire spontaneously which in turn leads to death. 4,4'-Dichlorodiphenyltrichloroethane - D8 is banned for agricultural use in North America, it is still commonly used in some countries and particularly as a means of malaria control. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Balkew, M. et al.: Paras. Vect., 3, No pp. given (2010); Kikankie, C.K. et al.: Malaria J., 9, No pp. given. (2010); Battu, R.S. et al.: Sci. Total Environ., 78, 173 (1989).

Eleclazine hydrochloride (GS 6615 hydrochloride) is a novel inhibitor of late Na+ current (IC50: 0.7 uM).

AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.

Applications 4-Methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-2-thiophenecarboxylic Acid is an impurity of Articaine (A777900), an amide based short-acting local anesthetic use for regional anaesthesia in day-case settings such arthroscopy, hand , food surgery and in dentistry. References Grossman, M., et al.: J. Clin. Pharmacol., 44, 1282 (2004); Oertel, R., et al.: Pharmazie., 53, 646 (1998); Vree, T.B., et al.: Brit. J. Clin. Pharmacol., 44, 29 (1997);

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Applications Benzocaine is used as an anesthetic (local). References Kholod, Y., et al.: Environ. Sci. Technol., 43, 9208 (2009), Fliri, A., et al.: J. Med. Chem., 52, 8038 (2009), Perez-Garrido, Alfonso; Helguera, A., et al.: J. Pharm. Sci., 98, 4557 (2009), Onoue, S., et al.: J. Pharm. Sci., 98, 3647 (2009),

Vilobelimab (CaCP-29) is a human-mouse chimeric IgG antibody targeting human complement component 5a, a C5a inhibitor that inhibits neutrophil activation.

Applications A labelled metabolite of the sodium channel blocker Propafenone (P757500). References Hege, H.G. et al.: Arzneim.-Forsch., 34, 972 (1984); Hollmann, M., et al.: Arzneim.-Forsch., 33, 763 (1983); Bryson, H. M., et al.:Drugs, 45, 85 (1993);

Applications A local anesthetic used topically in opthalmology. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Fliri, A., et al.: J. Med. Chem., 52, 8038 (2009), Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010),

Cariporide (HOE-642), an NHE1 inhibitor, reduces human platelet degranulation, platelet-leukocyte aggregates, and GPIIb/IIIa activation.

Ranolazine (RS 43285-003) inhibits calcium uptake, treats chronic angina by targeting sodium/calcium channels to modulate intracellular sodium.

N-Me-aminopyrimidinone9 is a sodium channel antagonist

Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures.

Applications Flecainide is an antiarrhythmic (class IC). References Hodess, A.B., et al.: J. Cardiovasc. Pharmacol., 1, 427 (1979), Somani, P., et al.: Clin. Pharmacol. Ther., 27, 464 (1980), Alessi-Severini, S., et al.: Anal. Profiles Drug Subs. Excip., 21, 169 (1992)

Applications Butanilicaine Hydrochloride, is a local anesthetic. References Gall, H., et al.: J. Allergy and Clinical immunology, 97, 933 (1996)

Veratridine is a benzoate-cevane found in Veratrum and Schoenocaulon. It activates sodium channels to stay open longer than normal.

PF-05661014, a demethylated analogue of PF-06526290, selectively inhibits Nav1.3 and Nav1.7 currents by stabilizing the inactivated state through interaction with the D4 VSD. This compound is utilized in research focused on sodium channel modulation.

CL-424032 is an inhibitor of sodium channels (sodium channel).

Stability Hygroscopic Applications 5,5-Diphenyl Hydantoin Sodium salt reduces incidence of grand mal seizures; appears to stabilize excitable membranes perhaps through effects on Na+, K+, and Ca2+ channels. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Faucette, S., et al.: J. Pharmacol. Exp. Ther., 320, 72 (2007), Guo, D., et al.: J. Biol. Chem., 282, 36766 (2007), Merrell, M., et al.: Drug Metab. Dispos., 36, 1716 (2008),

Fosphenytoin disodium (ACC-9653) is a prodrug of phenytoin that is rapidly converted to phenytoin, a voltage-gated sodium channel blocker

Rilmakalim is a potassium channel opener. Rilmakalim shows antivasoconstrictor effect.

Suzetrigine (VX-548) is an oral NaV1.8 inhibitor with analgesic properties for acute pain research.

Benzonatate (PEGn) is a unique non-narcotic cough suppressant featuring sodium channel blocking properties and anesthetic effects on respiratory tract stretch receptors.

Ranolazine 2HCl, an antianginal, treats arrhythmia by inhibiting sodium current without changing blood pressure or heart rate.

Carbamazepine: a tricyclic with anticonvulsant and analgesic effects, treats trigeminal neuralgia.

A-803467 is a selective NaV1.8 channel blocker.

Myomodulin is a neuropeptide present in molluscs, insects, and gastropods.Myomodulin is present in two identified aplysia neurons that contain myomodulin A the

(R)-Duloxetine, an isomer of Duloxetine, induces tonic and use-dependent blockade of neuronal Na+ channels. This compound is utilized in pain research.