current

Ifenprodil is a selective NMDA receptor (glutamate) antagonist.

Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of clarithromycin is Macrolides.

Ajmaline (Cardiorythmine) is a class Ia anti-arrhythmic compound that is widely used for the diagnosis of Brugada syndrome and the acute treatment of atrial or ventricular tachycardia. Ajmaline inhibits cardiac Kv1.5 and Kv4.3 channels at therapeutic concentrations.

NS3623 is an activator of human ether-a-go-go-related gene (hERG) potassium channels with a dual mode of action, also acting as an inhibitor of hERG1 channels. It activates the IKr and Ito currents and exhibits an antiarrhythmic effect.

NS5806 is an effective potassium current activator. NS5806 slows KV4.3 and KV4.2 current decay in channel complexes containing KChIP2. NS5806 enhances KV4.3/KChIP2 peak current amplitudes (EC50: 5.3 μM).

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

Linopirdine (DuP 996) is a TRPV1 agonist. Linopirdine is an orally active and selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor (IC50: 2.4 μM). Linopirdine is a cognitive enhancer. It acts by stimulating release of acetylcholine and other neurotransmitters.Linopirdine is a putative cognition-enhancing drug that increases acetylcholine release in rat brain tissue.

Sematilide hydrochloride (CK-1752) is a class III antiarrhythmic. It is a selectively delayed rectifier K+ current (IKr) channel blocker. It inhibits rapidly activating Ik in guinea pig atrial myocytes, resulting in the prolongation of refractoriness and action potential duration.

A2764 dihydrochloride is a highly selective inhibitor of TWIK-related spinal cord K+ channel (TRESK).

Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.

AM-92016 is a specific blocker of rectifier potassium current. AM-92016 delays rectifier potassium channel and repolarizes the membrane thereby restricting the duration of the nerve impulse.

Sematilide is a blocker of selective IKr channel.

Eleclazine hydrochloride (GS 6615 hydrochloride) is a novel inhibitor of late Na+ current (IC50: 0.7 uM).

XE 991 dihydrochloride is a Kv7 (KCNQ) channel blocker. XE 991 dihydrochloride potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current (IC50s: 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively).

GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.

Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).

Ibutilide Fumarate (U70226E) is the fumarate salt form of ibutilide, a class III antiarrhythmic agent. Ibutilide exerts its effect by activating a slow, inward, predominately sodium current rather than by blocking outward potassium currents. This results in prolongation of atrial and ventricular action potential duration and refractory periods. Ibutilide slightly decreases the sinus rate and atrioventricular (AV) conduction and produces a dose-related prolongation of the QT interval.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Flecainide is a medication used to prevent and treat abnormally fast heart rates. This includes ventricular and supraventricular tachycardias.

ICA-105574 (ICA) is an activator of hERG that binds to the channel to remove inactivation, thus increasing peak current amplitude and shortening the action potential. It also modulates activation kinetics of the channel.

Phe-Met-Arg-Phe, amide acetate, activates a K+ current in peptidergic caudodorsal neurons dose-dependently (ED50=23 nM) and appears to localize with neuropeptide Y in some brain regions.

Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

Tirzepatide (LY3298176) is a long-acting glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor dual agonist. In HEK293 cells, it can effectively stimulate cAMP accumulation, with an EC50 of 0.0224 nM for the GIP receptor (GIPR) and an EC50 of 0.934 nM for the GLP-1 receptor (GLP-1R).

Tween 80 is a nonionic surfactant and emulsifier that reduces bacterial adherence and inhibits biofilm formation. Tween 80 is widely used as a co-solvent in pharmacology experiments because of its ability to enhance the solubility of compounds in the aqueous phase.