voltage-gated channel

Kv3 modulator 1 is a voltage-gated potassium channel Kv3 modulator that can be used to study neurologic-level diseases.

PF-06305591 is an effective and selective blocker of voltage-gated sodium channel NaV1.8 (IC50 = 15 nM).

SAK3 is a novel modulator of nAChR activity that enhances T-type voltage-gated Ca2+ channel (T-VGCC) activity, and has potentiating effects on both Cav3.1 and Cav3.3 T-type Ca2+ channel currents.SAK3 is neuroprotective against scopolamine-induced cholinergic dysfunction in human neuroblastoma SH-SY5Y cells.SAK3 is used for the study of memory deficits and Alzheimer's disease. SAK3 can be used to study memory deficits and Alzheimer's disease.

Hymenidin, an alkaloid isolated from the Okinawan sponge Hymeniacidon sp. is a 5-hydroxytryptaminergic receptor antagonist and voltage-gated potassium channel inhibitor with potential antiprotozoal effects.It selectively binds to FOXO1 DNA and reduces depolarization-induced elevation of cellular calcium.

HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit with analgesic activity.

Flosatidil is a small molecule voltage-gated calcium channel complex (VDCCs) blocker for the treatment of neurological disorders and cardiovascular diseases, and can be used in the study of angina pectoris.

Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.

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

Primidone (NCI-C56360) is a potent anticonvulsant agent. It is a neuronal voltage-gated sodium channel blocker and has value in the study of epilepsy, essential tremor, and psychiatric disorders.

Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride (Proparacaine HCl) stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, and resulting in a loss of sensation.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

Mexiletine hydrochloride (KOE-1173 hydrochloride) is a voltage-gated sodium channel blocker and a Class IB antiarrhythmic drug. Mexiletine hydrochloride exerts antiarrhythmic effects by inhibiting sodium current in myocardial cells, thereby reducing the rise rate of cardiac action potential (phase 0) and reducing the automaticity of Purkinje fibers.

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

Tetrandrine (Sinomenine A) is a naturally occurring biphenylisoquinoline alkaloid, a calcium channel inhibitor. Tetrandrine inhibits voltage-gated calcium channels (ICa) and Ca2+-activated potassium channels.

Amifampridine (3,4-Diaminopyridine) is primarily used to treat rare muscle diseases. It blocks potassium channel efflux in nerve terminals, increasing action potential duration, which allows Ca2+ channels to remain open longer and enhances acetylcholine release to stimulate muscles at the end plate.

Hemin (Hemin chloride) is a chlorinated iron-containing porphyrin, a heme oxygenase (HO)-1 inducer. Hemin has therapeutic activity in porphyrias by reducing heme deficiency in patients, thereby inhibiting δ-aminolevulinic acid synthetase activity through biochemical feedback.

Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na+ channel(IC50 of 0.8 mM tested with a potential of +30 mV).

Calcium Channel antagonist 4 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Calcium Channel antagonist 3 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Brevetoxin-3 (PbTx-3) is a potent allosteric activator of voltage-gated Na+ channels, exhibiting a high affinity for site 5 and inhibiting the inactivation of these channels.

Meclofenamic acid (Meclofenamate) is a non-selective gap-junction blocker and a selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, with notable anti-inflammatory activities.

Mexiletine D6 hydrochloride is a non-selective voltage-gated sodium channel blocker,is a Class IB antianhythmic.

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