Bulleyaconitine A is an analgesic and antiinflammatory drug isolated from Aconitum plants; has several potential targets, including voltage-gated Na+ channels.
μ-Conotoxin Sx IIIA is a biological active peptide. (NaV1.4 Channels Blocker)
Riluzole-13C,15N2 is the 13C and 15N labeled Riluzole[1]. Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM[2][3].
Licarbazepine-d4-1 is deuterium labeled Licarbazepine. Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1].
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain[1][2].
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively[1][2].
Lidocaine-d10 (Lignocaine-d10) hydrochloride is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
ABBV-318 is a potent Nav1.7/ Nav1.8 blocker, with IC50s of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. ABBV-318 can be used for the research of pain[1].
VGSCs-IN-1 (compound 14), a 2-piperazine analog of Riluzole (HY-B0211), is a human voltage-gated sodium channels (VGSCs) inhibitor. VGSCs-IN-1 shows great Nav1.4 blocking activity. VGSCs-IN-1 has a pKa of 7.6 and a cLog P of 2.4. VGSCs-IN-1 can be used for cell excitability disorders research[1].
β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells[1].
Articaine (Hoe-045 free base) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway[1][2][3].
GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively[1].
Benzocaine shares a common receptor with all other local anesthetics (LAs) in the voltage-gated Na+ channel, with an IC50 of 0.8 mM tested with a potential of +30 mV.
Indoxacarb ((±)-Indoxacarb) is a broad-spectrum oxadiazine insecticide. Indoxacarb is metabolized in vivo to its active N-decarbomethoxyllated metabolite DCJW. Indoxacarb suppresses voltage-gated sodium channel currents in rat dorsal root ganglion neurons.
Flecainide hydrochloride is a potent and orally active antiarrhythmic agent. Flecainide hydrochloride blocks the cardiac fast inward Na+ current (INa) and the rapid component of the delayed rectifier K+ current. Flecainide hydrochloride prolongs the action potential duration (APD) in ventricular and atrial muscle fibres. Flecainide hydrochloride has the potential for the research of fetal tachycardias[1][2][3].
Halazone is an atypical antimicrobial sulfonamide derivative and a carbonic anhydrase II inhibitor with a Kd value of 1.45 µM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water[1][2].
Pilsicainide hydrochloride (SUN-1165) is an orally active sodium channel blocker and potent class Ic antiarrhythmic agent[1][2].
Phenytoin-15N2,13C is the 13C and 15N labeled Phenytoin[1]. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[2][3].
μ-Conotoxin GIIIB is a 22-residue polypeptide that can be isolated from the venom of piscivorous cone snail Conus geographus. μ-Conotoxin GIIIB is a NaV1.4 channel inhibitor. μ-Conotoxin GIIIB blocks muscle cell's contraction[1][2][3].
Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local anesthetic that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease[1].
Zonisamide sodium is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug.Target: Calcium channel inhibitor; Sodium channel inhibitorZonisamide sodium is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures for adults; infantile spasm, mixed seizure types of Lennox-Gastaut syndrome, myoclonic, and generalized tonic clonic seizure. Zonisamide sodium is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug. It has shown activity in various animal models of epilepsy, and although a detailed mode of action awaits clarification it appears to block the propagation/spread of seizure discharges and to suppress the epileptogenic focus [1].Zonisamide sodium 500 mg/day was significantly superior to placebo in reducing the frequency of complex partial seizures (-51% versus -16%), all partial seizures and all seizures, with dose-dependent benefit provided over a 100-500 mg/day dose range. Supporting trials have confirmed significant increases in reduction in median seizure frequency (up to 41%) and responder rates (35-42%) compared with placebo following zonisamide sodium 400-600 mg/day, enabling 20-27% of patients to attain >or=75% reduction in seizure frequency [2].Clinical indications: Epilepsy; Lewy body dementia; Parkinsons diseaseToxicity: Anorexia; Somnolence; Dizziness; Irritability; Confusional state; Depression; Diplopia; Memory impairment
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[1][2].
Zonisamide is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug.Target: Calcium channel inhibitor; Sodium channel inhibitorZonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures for adults; infantile spasm, mixed seizure types of Lennox-Gastaut syndrome, myoclonic, and generalized tonic clonic seizure. Zonisamide is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug. It has shown activity in various animal models of epilepsy, and although a detailed mode of action awaits clarification it appears to block the propagation/spread of seizure discharges and to suppress the epileptogenic focus [1].Zonisamide 500 mg/day was significantly superior to placebo in reducing the frequency of complex partial seizures (-51% versus -16%), all partial seizures and all seizures, with dose-dependent benefit provided over a 100-500 mg/day dose range. Supporting trials have confirmed significant increases in reduction in median seizure frequency (up to 41%) and responder rates (35-42%) compared with placebo following zonisamide 400-600 mg/day, enabling 20-27% of patients to attain >or=75% reduction in seizure frequency [2].Clinical indications: Epilepsy; Lewy body dementia; Parkinsons diseaseToxicity: Anorexia; Somnolence; Dizziness; Irritability; Confusional state; Depression; Diplopia; Memory impairment
Zandatrigine is a sodium channel protein type 8 subunit alpha (Scn8α) blocker[1].
Dyclonine is an oral anaesthetic found in Sucrets, an over the counter throat lozenge.Target: Sodium ChannelDyclonine is an oral anaesthetic that is the active ingredient of Sucrets, an over the counter throat lozenge. It is also found in some varieties of the Cepacol sore throat spray. It is a local anesthetic, used topically as the hydrochloride salt. Dyclonine hydrochloride has been found to possess, in addition to its topical anesthetic properties, significant bactericidal and fungicidal activity. Self-sterilizing action manifested by preparations containing the drug was considerably enhanced upon the addition of chlorobutanol. Results of in vitro tests employing microorganisms commonly involved in local infections indicated that the two agents in combination act synergistically [1, 2].
Clathrodin is a marine alkaloid that can be isolated from sponges of the genus, Agelas. Clathrodin is a modulator of voltage-gated sodium (NaV) channels. Clathrodin is a sodium channel neurotoxin influencing sodium channel ionic conductance[1][2].
PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
Nav1.7 inhibitor is a potent Nav1.7 inhibitor.IC50 value:Target: Nav1.7Preparation of sulfonamide derivatives as Nav1.7 inhibitorsBy Brown, Alan Daniel; Rawson, David James; Storer, Robert Ian; Swain, Nigel Alan From PCT Int. Appl. (2012), WO 2012007868 A2 20120119.
Nav1.8-IN-4 (compound 9a) is a Nav1.8 channel inhibitor (IC50=0.014 μM). Nav1.8-IN-4 can be used for research on pain-related diseases[1].
Hardwickiic acid ((-)-Hardwikiic acid) is an antinociceptive compound that blocks Tetrodotoxin-sensitive voltage-dependent sodium channels. Hardwickiic acid shows insecticidal activity[1][2].