depolarization

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

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

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.

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.

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.

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).

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

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.

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.

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.

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

Disopyramide (Triombrin) is a class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.

Genistein 8-c-glucoside (G8CG), a natural glucoside isolated from the flowers of Lupinus luteus L., induces mitochondrial membrane depolarization and apoptosis.

N-Depropylpropafenone, an active metabolite of Propafenone, is produced through the metabolism by the CYP450 enzyme system (primarily CYP2D6). It functions by blocking sodium ion channels, thereby delaying the depolarization process in myocardial cells and exhibiting antiarrhythmic properties.

Butoprozine exhibits various cardiac electrophysiological effects: it prolongs action potential duration, akin to the effect of amiodarone; it inhibits the plateau phase, similar to verapamil; and it reduces both amplitude and the maximum rate of depolarization.

Gamma-DGG TFA is an antagonist of excitatory amino acids that can inhibit depolarization induced by NMDA, Kainate, and Quisqualate. In addition, it counteracts excitatory postsynaptic potentials (e.p.s.p.) in rat hippocampal slices.

5R(6S)-EET is a metabolite of Arachidonic acid. It activates the synthesis of endogenous prostaglandin (PGE2), which inhibits Na+ absorption, increases intracellular Ca2+, and promotes transmembrane voltage depolarization. 5R(6S)-EET demonstrates stereoselectivity and is less active compared to 5S(6R)-EET.

p38-α MAPK-IN-8 (Compound 13) is a lipophilic cationic derivative. It exhibits cytotoxicity toward various tumor cells, inducing cell cycle arrest and apoptosis, as well as increasing reactive oxygen species (ROS) production and causing mitochondrial membrane potential depolarization. Its antitumor activity may be related to the p38α MAPK pathway, making it a potential candidate for cancer research.

Mitochondria modulator-2 (Compound Ir1) induces depolarization of the mitochondrial membrane potential, generates reactive oxygen species (ROS), inhibits the migration of A549 cells, causes cell cycle arrest at the G2 M phase, and triggers apoptosis in A549 cells.

EGFR-IN-141 (Compound 8I) functions as an EGFR inhibitor with an IC50 of 2.67 nM. It exhibits cytotoxicity in A549 cancer cells with an IC50 of 13.75 μM. EGFR-IN-141 induces apoptosis and mitochondrial membrane depolarization and shows potential antitumor activity.

1,1-Dimethyl-4-acetylpiperazinium iodide is an agonist of nicotinic acetylcholine receptors (nAChR) that activates ion channels, resulting in depolarization of the cell membrane.