Mambalgin 1 is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 binds to closed/inactive channel. Mambalgin 1 is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
Flecainide is a potent and orally active antiarrhythmic agent. Flecainide blocks the cardiac fast inward Na+ current (INa) and the rapid component of the delayed rectifier K+ current. Flecainide prolongs the action potential duration (APD) in ventricular and atrial muscle fibres. Flecainide has the potential for the research of fetal tachycardias[1][2][3].
Irampanel (BIIR 561) is an AMPA receptor and voltage-dependent sodium channel blocker. Irampanel inhibits kainate-induced currents in rat cortical neurons[1].
GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7[1].
Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.
Methocarbamol-d3 is the deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research[1][2][3].
YM758 is a “funny” If current channel (If channel) inhibitor.
Bliretrigine is a sodium channel blocker. Bliretrigine has the effect of relieving pain[1][2][3].
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization[1][2].
Phenytoin sodium is an inactive voltage-gated sodium channel stabilizer.Target: Sodium ChannelPhenytoin sodium is an antiepileptic drug. It is useful to treat partial seizures and generalized tonic-clonic seizures but not primary generalized seizures such as absence seizures or myoclonic seizures. Phenytoin is believed to protect against seizures by causing voltage-dependent block of voltage-gated sodium channels [1]. Phenytoin has low affinity for resting sodium channels at hyperpolarized membrane potentials [2]. When neurons are depolarized and the channels transition into the open and inactivated states, greater binding and block occur. The inhibitory potency is strongly use dependent, so that block accumulates with prolonged or repetitive activation, such as occurs during a seizure discharge. The blocking of sodium channels by phenytoin is of slow onset. The time course of fast sodium currents is therefore not altered in the presence of the drug and action potentials evoked by synaptic depolarizations of ordinary duration are not blocked. Thus phenytoin is able to selectively inhibit pathological hyperexcitability in epilepsy without unduly impairing ongoing activity. Phenytoin also blocks persistent sodium current and this may be of particular importance in seizure control. Phenytoin is a class 1b antiarrhythmic [3].
NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration[1].
μ-Conotoxin KIIIA is an analgesic μ-conotoxin that can be isolated from Conus kinoshitai. μ-Conotoxin KIIIA blocks mammalian neuronal voltage-gated sodium channels (VGSCs) (Nav1.2).μ-Conotoxin KIIIA can be used for research of pain[1][2].
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][6].
SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5[1].
AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM; potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays; displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5; blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking; exhibits pharmacodynamic effects in translatable models of both itch and pain.
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM)[1][2].
PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.
Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.
Lamotrigine-13C2,15N is the 13C and 15N labeled Lamotrigine[1]. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al[2][3].
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
Ralfinamide (FCE-26742A) is an orally available Na(+) channel blocker derived from α-aminoamide, with function of suppressing pain[1].
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo[1].
ATX-II is a specific Na+ channel Modulator toxin that can be isolated from the venom of sea anemone (Anemonia sulcata). ATX-II causes delayed inactivation of the Na+HY-B1010), Caffeine, and Ryanodine (HY-103306). ATX-II also induces pulmonary vein arrhythmogenesis and atrial fibrillation[1][2].
Mexiletine D6 hydrochloride (KOE-1173 D6 hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1].
Lamotrigine-13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1[1].
Disopyramide-d14 (Dicorantil-d14) tosylate salt is the deuterium labeled Disopyramide. Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action[1][2][3][4].
NBI-921352 (XEN901) is a potent inhibitor of sodium channels, specially targeting Nat/1.6 channels. NBI-921352 (XEN901) treats the nervous system pathologies of epilepsy effectively without adverse side effects (extracted from patent WO2017201468A1)[1].