depolarization

Immethridine dihydrobromide is a novel, highly potent and selective histamine H3 receptor (H3R) agonist that inhibits dendritic cell function and alleviates experimental autoimmune encephalomyelitis.Immethridine dihydrobromide MesV induces depolarization of neurons and the MMN and prevents cardiorenal and renal injury. injury.

GW 833972A is a selective CB2 receptor agonist that inhibits induced neural depolarization and citric acid-induced cough in an animal model.

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.

AZD 7009 is a novel antiarrhythmic compound that inhibits the sodium current of hNav1.5 in CHO K1 cells with an IC50 of 11 uM. AZD 7009 inhibited late sodium current in isolated rabbit atrial and ventricular myocytes, and prolonged E-4031-induced action potential duration, promoting early post-depolarization of Purkinye fibers (EADs).

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

λ-Cyhalothrin (Icon) is a type II synthetic pyrethroid insecticide featuring a high-efficiency, broad-spectrum formula with an α-cyano group. It is employed across various applications for controlling a wide array of pests. As a neurotoxin, λ-Cyhalothrin acts on sodium channels in neuron membranes within the central nervous system.

γ-Aminobutyric acid (4-Aminobutyric acid) is the predominant inhibitory neurotransmitter in the central nervous system.

Bupivacaine hydrochloride (Vivacaine) is a long-acting, amide-type local anesthetic. Bupivacaine hydrochloride reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation.

Ivabradine hydrochloride (S 16257-2) is a new If inhibitor (IC50: 2.9 μM). Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization.

Pyrantel hydrochloride is the hydrochloride form of Pyrantel.Pyrantel is a pyrimidine derivative.Pyrantel is an orally available drug for the treatment of a wide range of parasitic infections.Pyrantel acts as a depolarizing neuromuscular blocking agent.It acts as a nicotinic acetylcholine receptor (nAChR) agonist for nematodes.The neuromuscular depolarization of Pyrantel causes paralysis in worms.

DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.

MTP 131 is a mitochondria-targeted peptide antioxidant.1,2It localizes to the mitochondria and reducestert-butyl hydroperoxide-induced lipid peroxidation and apoptosis in SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 nM.1MTP 131 (2 mg kg) reduces infarct volume, hemispheric swelling, and glutathione (GSH) depletion in a mouse model of acute cerebral ischemia induced by middle cerebral artery occlusion (MCAO).2It increases survival, improves motor function, and decreases degeneration of the lumbar spinal cord in a superoxide dismutase 1 mutant (SOD1G93A) transgenic mouse model of amyotrophic lateral sclerosis (ALS) when administered at a dose of 5 mg kg. MTP 131 reduces albuminuria, urinary hydrogen peroxide levels, and mesangial matrix accumulation, as well as preserves superoxide production, in adb dbmouse model of diabetic nephropathy.3 1.Zhao, K., Luo, G., Giannelli, S., et al.Mitochondria-targeted peptide prevents mitochondrial depolarization and apoptosis induced by tert-butyl hydroperoxide in neuronal cell linesBiochem. Pharmacol.70(12)1796-1806(2005) 2.Szeto, H.H.Mitochondria-targeted peptide antioxidants: Novel neuroprotective agentsAAPS J.8(3)E521-E531(2006) 3.Miyamoto, S., Zhang, G., Hall, D., et al.Restoring mitochondrial superoxide levels with elamipretide (MTP-131) protects db db mice against progression of diabetic kidney diseaseJ. Biol. Chem.295(21)7249-7260(2020)

CCI-006, a selective inhibitor and chemosensitizer for MLL-rearranged leukemia cells, disrupts mitochondrial respiration. This action leads to irreversible mitochondrial depolarization and triggers a pro-apoptotic unfolded protein response in specific MLL-r leukemia cells.

Alosetron hydrochloride (GR 68755) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. Alosetron blocks the actions of serotonin at 5-HT3 sites in the peripheral nervous system, particularly on enteric and nociceptive sensory neurons, thereby affecting the regulation of visceral pain, decreasing gastrointestinal contraction and motility, and decreasing gastrointestinal secretions.

Mepivacaine hydrochloride (Mepivacaine HCl) is the hydrochloride salt form of mepivacaine, an amide derivative with local anesthetic properties.

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

Batrachotoxin (BTX), a potent neurotoxin and cardiotoxin, is found in the skin of the Colombian dart frog (Phyllobates aurotaenia). As an activator of sodium channels (sodium channel), it interferes with normal sodium channel closure by binding to voltage-gated sodium channels (sodium channel) on the cell membrane. This interaction causes a continuous influx of sodium ions into the cells, leading to persistent depolarization.

Moricizine Hydrochloride (EN 313) is an orally active Class I antiarrhythmic agent that reduces the maximum rate of phase 0 depolarization, increases the repolarization rate of phases 2 and 3, decreases the duration of action potentials, and shortens the effective refractory period.

Tubulin polymerization-IN-9, a potent inhibitor of tubulin (IC50: 1.82 μM), arrests the cell cycle of K562 cells in the G2 M phase, induces apoptosis and mitochondrial depolarization, and exhibits strong anti-vascular and anti-tumor effects.

α-Bag Cell Peptide (1-8) is an NH2-terminal fragment of α-bag cell peptide that inhibits LUQ (left upper quadrant) neurons and the depolarization of bag cells [1].

α-Angelica lactone has cardiotonic activity, may exert their effects by providing an increased contraction-dependent calcium pool to be released upon systolic depolarization.

Sulfonadyn-47 is a dynamin inhibitor that effectively inhibits dynamin GTPase activity with an IC50 of 3.5 µM in cell-free assays. Additionally, it disrupts clathrin-mediated endocytosis in U2OS cells (IC50 = 27.3 µM) and impedes the depolarization-stimulated uptake of the synaptic vesicle endocytosis (SVE) marker FM4-64 in isolated rat brain synaptosomes (IC50 = 12.3 µM). Significantly, in vivo administration of sulfonadyn-47 at doses of 30 and 60 mg/kg demonstrates anticonvulsant properties in the 6 Hz corneal kindling mouse model of seizures.

CK59 is a reversible inhibitor of calcium-calmodulin-dependent kinase II (CaMKII). CK59 inhibits multiple voltage-gated calcium channels, including the L-type channel during depolarization in a dose-dependent manner. The IC50 for CK59 was approximately 50

cPcAMP1 26, an antimicrobial peptide, exhibits potent bactericidal activity against A. hydrophila and S. aureus by inducing depolarization of the bacterial plasma membrane and elevating intracellular ROS (Reactive Oxygen Species) levels [1].