electrophysiological

Tiaspirone hydrochloride (BMY-13859 hydrochloride) exhibits antipsychotic activity. Tiaspirone hydrochloride influences the electrophysiological activity of dopaminergic neurons in the substantia nigra zona compacta (A9 DA cells) and ventral tegmental area (A10 DA cells) in the brain of the rat.

Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves the metabolic and electrophysiological status of the ischemic penumbra region, and reduces the size of the lesion on magnetic resonance images in the acute phase after middle cerebral artery occlusion in rats.Pinokalant is a potential SARS-CoV-2 protease inhibitor for the study of stroke.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

NS11394 is a effective and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of α(5) > α(3) > α(2) > α(1) at GABA(A) alpha subunit-containing receptors.

GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.

SB-200646 is a selective and potent antagonist of 5-HT2B 5-HT2C receptor

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.

Quinacainol dihydrochloride (PK 10139 dihydrochloride) is the bis(2 hydrochloride) salt form of Quinacainol. It acts as an inhibitor of the sodium current, with an EC50 of 95 µM. This compound displays antiarrhythmic activity by modulating the electrophysiological properties of the heart.

Latrunculin B, an alkaloid from the Red Sea sponge, is an actin polymerization inhibitor with antifungal and antiprotozoal activity.Latrunculin B modulates the electrophysiological characteristics of the pulmonary veins and attenuates the occurrence of torsade de pointes, and may be used in the study of glaucoma in adolescents.

SB-200646A is an orally active, selective antagonist of 5-HT2B 2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.

BBR 2160 is a dihydropyridine derivative belonging to the group of the so-called tiampidine. BBR 2160 has calcium-antagonistic properties in cardiac tissue. Intracellular microelectrodes have been used to characterize the electrophysiological properties o

GYKI-16638 is a novel antiarrhythmic agent that demonstrates combined class IB and class III antiarrhythmic properties in human ventricular muscles, similar to the electrophysiological findings after chronic amiodarone treatment. In addition, GYKI 16638 h

VU6010608 is an effective mGlu7 NAM with excellent CNS permeability and is powerful in electrophysiological studies in blocking long-term enhancement of high-frequency stimuli.

U 66985 is a Platelet-activating factor (PAF) receptor antagonist that inhibit the electrophysiological effects of PAF.

Pitrazepin is a new GABAA receptor antagonist reported to antagonize electrophysiological effects of GABA

RO-5328673 is a dual NK2 NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of gp SNpc, RO5328673 inhibited the senktide-induced potentiation of spontaneous activity of dopaminergic neurons with an insurmountable mechanism of action. RO5328673 exhibited in-vivo activity in gerbils, robustly reversing the senktide-induced locomotor activity.

Recainam (Wy-42362) hydrochloride, an orally active anti-arrhythmic agent, exhibits Class I electrophysiological properties and effectively suppresses complex ventricular arrhythmias. It has demonstrated favorable pharmacokinetic characteristics in Sprague Dawley rats .

Amylin (AMY3) receptor antagonist. Inhibits andrenomedulin-stimulated cAMP production in vitro. Protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. Blocks el

Melanostatin, frog TFA is a highly efficient α-melanocyte-stimulating hormone (α-MSH) release inhibitor, a 36-amino acid peptide isolated from the frog brain, which modulates the electrophysiological activity of frog melanocytes by regulating K+, Na+, and Ca2+ currents.