k+ currents

Cloperastine fendizoate (Hustazol) inhibits the hERG K+ currents in a concentration-dependent manner (IC50: 27 nM).

8-Bromo-cGMP sodium is a PKG activator, a membrane-permeable analog of cGMP. 8-Bromo-cGMP sodium has pain-relieving and vasodilatory effects, significantly inhibits Ca2+ macroscopic currents, and inhibits high K+-stimulated insulin release.

Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.

Quinidine hydrochloride monohydrate is an optical isomer of quinine, extracted from the bark of the Cinchona tree and similar plant species. It prolongs cellular action potential and decreases automaticity. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity (IC50: 3.3 nM). Zaldaride maleate is an effective and selective inhibitor of calmodulin. Zaldaride maleate prevents estrogen-induced transcription activation by ER, re

AUT2 is a Kv3.1 channel modulator with the potential to treat sensory hyperreactivity in patients with FXS by shifting the activation of high-threshold currents to more negative potentials. This shift reduces high-threshold K+ currents and increases low-threshold K+ currents in neurons, restoring wave IV of the ABR. Due to its ability to regulate neuronal excitability, AUT2 is also promising for the treatment of hearing impairments.

(S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide (N-Docosahexacnoylethanolamide(22:6)) is a homologue of dehydroepiandrosterone (DHEA). This compound can block Shaker-related voltage-gated potassium channels and inhibits Kv1.2 K+ currents with an IC50 value of 1.5 μM.

SRA-36 is a selective inhibitor of CLC-K chloride ion channels, exhibiting high selectivity for CLC-5 and CLC-1 channels. It blocks CLC-Ka currents with an IC50 of 6.6 μM and a Kd of 3.8 μM. SRA-36 effectively inhibits chloride ion currents mediated by target channels and suppresses currents resulting from the hypertension-related CLC-KaA447T and CLC-KaY315F polymorphisms. It is applicable in hypertension research.

Doxapram (Dopram) is a respiratory stimulant that inhibits TASK-1, TASK-3, and TASK-1/TASK-3 heterodimer channels and is used to study ventilatory failure caused by apnea of ​​prematurity and exacerbation of chronic obstructive pulmonary disease.

Chromanol 293B is an inhibitor of the slow component (IK) of delayed rectifier potassium currents in cardiac cells (IC50 = 1–10 μM) and a weak inhibitor of KATP channels. It also blocks CFTR chloride currents (IC50 = 19 μM) and can be used in arrhythmia research.

inhibitor of outward K+ currents

Tedisamil is a blocker of K+ currents in cardiac tissues, exerts bradycardic effects. It is an antiarrhythmic drug with predominantly class III activity. It has shown clinical efficacy in angina pectoris.

Nerispirdine is a acetylcholine release enhancer, sodium channel blocker and K(V) 2.1 channel blocker. Nerispirdine inhibits voltage-dependent Na(+) channel currents recorded from human SH-SY5Y cells with an IC(50) of 11.9 micromol/L when measured from a

Water-soluble salt of lamotrigine . Displays anticonvulsant effects and inhibits glutamate release, possibly through inhibition of Na+, K+ and Ca2+ currents. Leach et al (1991) Neurochemical and behavioral aspects of lamotr. Epilepsia 32 S4 PMID:1685439 |Smith and Meldrum (1995) Cardioprotective effect of lamotr. after focal ischemia in rats. Stroke 26 117 PMID:7839380 |Zona and Avoli (1997) Lamotrigine reduces voltage-gated sodium currents in rat central neurons in culture. Epilepsia 38 522 PMID:9184596 |Grunze et al (1998) Modulation of calcium and potassium currents by lamotr. Neuropsychobiology 38 131 PMID:9778600

Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg/kg twice daily.3 Alaproclate (40 mg/kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988). Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg/kg twice daily.3 Alaproclate (40 mg/kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4 References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988).

N-Salicyloyltryptamine(STP) is a tryptamine analogue with anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect. N-Salicyloyltryptamine acts as the voltage-dependent Na +, Ca 2+, and K + ion channels inhibitor which inhibits K + currents with an IC 50 value of 34.6 μM ( /to) [1] - [5].

Quinine hemisulfate hydrate is an alkaloid extracted from the bark of cinchona, which has antimalarial effect. Quinine hemisulfate hydrate can be used as a potassium ion channel inhibitor to inhibit the voltage-induced mSlo3(KCa5.1) channel current, and its IC₅₀ is 169 μM under the condition of +100 mV.

ShK toxin, isolated from the Caribbean sea anemone (Stichodactyla helianthus), is an inhibitor of the voltage-dependent potassium channel (Kv1.3 channel). It competes with dendrotoxin I and α-dendrotoxin in binding to rat brain synaptosomal membranes and promotes acetylcholine release. Additionally, ShK toxin reduces K+ currents in cultured rat dorsal root ganglion neurons and inhibits T lymphocyte proliferation [1] [2].

Tamapin, a venom peptide isolated from the Indian red scorpion (Mesobuthus tamulus) [1], selectively targets and blocks small-conductance Ca(2+)-activated K(+) (SK) channels, particularily SK2 (Potassium Channel). It inhibits SK channel-mediated currents in the pyramidal neurons of the hippocampus.

Tamapin TFA, a venom peptide isolated from the Indian red scorpion (Mesobuthus tamulus) [1], selectively targets and blocks small conductance Ca(2+)-activated K(+) (SK) channels, particularly the SK2 subtype (Potassium Channel). It is known to inhibit SK channel-mediated currents in the hippocampal pyramidal neurons.

VU 0546110, a selective inhibitor of the sperm-specific potassium channel SLO3 (IC50= 64 μM), demonstrates 40-fold selectivity over SLO1. It effectively blocks both heterologous SLO3 currents and endogenous K+ currents, inhibiting sperm hyperpolarization and preventing hyperactivated mobility.

Guangxitoxin 1E acts as a gating modifier since it shifts the voltage-dependence of Kv2.1 K+ currents towards depolarized potentials.

Potent and selective μ opioid receptor antagonist (Ki values are 0.96 and >10,000 nM for μ and δ receptors respectively). Causes behavioral effects on central administration in vivo. Also increases K+ currents in rat locus ceruleus neurons in vitro via a