|S1614||Riluzole||<1 mg/mL||46 mg/mL||46 mg/mL|
|S2454||Bupivacaine HCl||23 mg/mL||65 mg/mL||65 mg/mL|
|S1811||Amiloride HCl||6 mg/mL||53 mg/mL||5 mg/mL|
|S1256||Rufinamide||<1 mg/mL||18 mg/mL||<1 mg/mL|
|S1603||Furosemide||<1 mg/mL||66 mg/mL||<1 mg/mL|
|S3907||Bulleyaconi cine A||-1 mg/mL||7 mg/mL||-1 mg/mL|
|S3911||Veratramine||-1 mg/mL||63 mg/mL||-1 mg/mL|
|S3751||Quinidine sulfate||9 mg/mL||100 mg/mL||100 mg/mL|
|S1445||Zonisamide||<1 mg/mL||42 mg/mL||5 mg/mL|
|S2524||Phenytoin Sodium||3 mg/mL||32 mg/mL||11 mg/mL|
|S1693||Carbamazepine||<1 mg/mL||47 mg/mL||18 mg/mL|
|S2785||A-803467||<1 mg/mL||72 mg/mL||11 mg/mL|
|S2560||Amiloride HCl dihydrate||17 mg/mL||0 mg/mL||0 mg/mL|
|S2525||Phenytoin||<1 mg/mL||50 mg/mL||13 mg/mL|
|S2874||Camostat Mesilate||10 mg/mL||99 mg/mL||<1 mg/mL|
|S2114||Dronedarone HCl||<1 mg/mL||80 mg/mL||40 mg/mL|
|S3024||Lamotrigine||<1 mg/mL||10 mg/mL||3 mg/mL|
|S4016||Ouabain||<1 mg/mL||100 mg/mL||100 mg/mL|
|S1965||Primidone||<1 mg/mL||44 mg/mL||3 mg/mL|
|S3064||Ambroxol HCl||<1 mg/mL||4 mg/mL||<1 mg/mL|
|S2041||Dyclonine HCl||6 mg/mL||15 mg/mL||36 mg/mL|
|S4229||Oxybuprocaine HCl||69 mg/mL||69 mg/mL||69 mg/mL|
|S3155||Mepivacaine HCl||57 mg/mL||3 mg/mL||8 mg/mL|
|S2500||Propafenone HCl||<1 mg/mL||69 mg/mL||<1 mg/mL|
|S4023||Procaine HCl||55 mg/mL||55 mg/mL||<1 mg/mL|
|S1619||Prilocaine||<1 mg/mL||44 mg/mL||44 mg/mL|
|S4038||Dibucaine HCl||76 mg/mL||76 mg/mL||76 mg/mL|
|S1391||Oxcarbazepine||<1 mg/mL||7 mg/mL||<1 mg/mL|
|S4058||Ropivacaine HCl||46 mg/mL||62 mg/mL||<1 mg/mL|
|S4180||Nefopam HCl||21 mg/mL||1 mg/mL||<1 mg/mL|
|S4061||Levobupivacaine HCl||64 mg/mL||64 mg/mL||57 mg/mL|
|S4080||Triamterene||<1 mg/mL||20 mg/mL||<1 mg/mL|
|S4200||Tolperisone HCl||56 mg/mL||56 mg/mL||56 mg/mL|
|S4210||Benzocaine||<1 mg/mL||33 mg/mL||33 mg/mL|
|S4669||Benzocaine hydrochloride||<1 mg/mL||40 mg/mL||40 mg/mL|
|S4668||Procaine||<1 mg/mL||47 mg/mL||47 mg/mL|
|S4225||Mexiletine HCl||43 mg/mL||43 mg/mL||43 mg/mL|
|S4235||Phenazopyridine HCl||<1 mg/mL||50 mg/mL||<1 mg/mL|
|S1828||Proparacaine HCl||66 mg/mL||12 mg/mL||<1 mg/mL|
|S4284||Chloroprocaine HCl||61 mg/mL||61 mg/mL||<1 mg/mL|
|S2110||Vinpocetine||<1 mg/mL||3 mg/mL|
|S4290||Digoxin||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S2118||Ibutilide Fumarate||89 mg/mL||89 mg/mL||89 mg/mL|
|S4294||Procainamide HCl||54 mg/mL||54 mg/mL||54 mg/mL|
- Sodium Channel阻害剤(45)
- 新Sodium Channel製品
Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (*p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (*p≤0.036). c Swim Speed. Aged rats swam the most slowly (*p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (*p<0.001).
Bupivacaine HCl binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, used for treating cardiac arrhythmias.
Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used in the treatment of congestive heart failure and edema.
Bulleyaconitine A (BLA) is an active ingredient of Aconitum bulleyanum plants and classified as an "aconitine-like" alkaloid. It is a potent use-dependent blocker for both Nav1.7 and Nav1.8 Na+ currents.
Veratramine, a major alkaloid from Veratrum nigrum L., has distinct anti-tumor and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has a good stability in the gastrointestinal tract during its absorption.
Lappaconitine (LC) is a natural diterpenoid alkaloid (DTA), acting as a human heart sodium channel blocker and possessing a wide range of biological activities, including anti-arrhythmic, anti-inflammatory, antioxidative, anticancer, epileptiform etc.
Quinidine acts as a blocker of voltage-gated sodium channels, also an antimuscarinic and antimalarial.
Zonisamide is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
Phenytoin Sodium is an inactive voltage-gated sodium channel stabilizer.
Carbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.
Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
Phenytoin is an inactive voltage-gated sodium channel stabilizer.
Camostat is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.
Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 (*) and P<0.005 (**).
Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.
Effect of pharmacological agents capable of increasing intracellular calcium concentration on RSV. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with a specific Na+/K+-ATPase inhibitor ouabain at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. Statistical significance between treated and control group were analyzed by t-test (*, p < 0.05, **, p < 0.01).
Primidone is an anticonvulsant of the pyrimidinedione class.
AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
Dyclonine HCl is a hydrochloride salt form of dyclonine which is an oral anaesthetic, reversibly binds to activated sodium channels on the neuronal membrane, thereby decreasing the neuronal membrane's permeability to sodium ions, leading to an increased threshold for excitation.
Oxybuprocaine HCl is a local anesthetic, which is used especially in ophthalmology and otolaryngology. Oxybuprocaine binds to sodium channel and reversibly stabilizes the neuronal membrane which decreases its permeability to sodium ions
Mepivacaine is a tertiary amine used as a local anesthetic.
Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.
Procaine is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.
Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. *p<0.05, **p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
Prilocaine is a local anesthetic of the amino amide type. It acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation.
Dibucaine HCl is a local anesthetics.
Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.
Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.
Nefopam HCl is a centrally-acting but non-opioid analgesic drug by blocking voltage-gated sodium channel and inhibition of serotonin, dopamine and noradrenaline reuptake.
Levobupivacaine HCl, the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.
Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.
Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.
Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.
Benzocaine hydrochloride is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.
Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses.
Mexiletine HCl belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.
Phenazopyridine HCl is a local analgesic that has been used in urinary tract disorders. It is an inhibitor of sodium channel protein type 1 subunit alpha.
Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.
Chloroprocaine HCl is a local anesthetic during surgical procedures.
Vinpocetine is a selective inhibitor of voltage-sensitive sodium channel for the treatment of stroke, vascular dementia and Alzheimer's disease.
Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.
Ibutilide Fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current, which prolongs action potential and refractory period of myocardial cells.
Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.