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To the Mechanism of the Antiarrhythmic Action of Compound ALM-802: the Role of Ryanodine Receptors
by
Mokrov, G. V.
, Teplov, I. Yu
, Kryzhanovskii, S. A.
, Vititnova, M. B.
, Stolyaruk, V. N.
, Zinchenko, V. P.
, Tsorin, I. B.
in
Animal experimentation
/ Animals
/ Anti-Arrhythmia Agents - pharmacology
/ Anti-arrhythmia drugs
/ Antiarrhythmics
/ Biomedical and Life Sciences
/ Biomedicine
/ Caffeine
/ Caffeine - pharmacology
/ Calcium (intracellular)
/ Calcium - metabolism
/ Cardiac arrhythmia
/ Cardiomyocytes
/ Cell Biology
/ Cell culture
/ Experiments
/ Fura-2
/ Hippocampus
/ Internal Medicine
/ Laboratory Medicine
/ Myocardium
/ Myocardium - metabolism
/ Pathology
/ Pharmacology
/ Pharmacology and Toxicologypharmacology Toxicology
/ Potassium chloride
/ Rats
/ Ryanodine - metabolism
/ Ryanodine - pharmacology
/ Ryanodine Receptor Calcium Release Channel - metabolism
/ Ryanodine receptors
/ Sarcoplasmic Reticulum
/ Software
/ Toxicology
2023
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To the Mechanism of the Antiarrhythmic Action of Compound ALM-802: the Role of Ryanodine Receptors
by
Mokrov, G. V.
, Teplov, I. Yu
, Kryzhanovskii, S. A.
, Vititnova, M. B.
, Stolyaruk, V. N.
, Zinchenko, V. P.
, Tsorin, I. B.
in
Animal experimentation
/ Animals
/ Anti-Arrhythmia Agents - pharmacology
/ Anti-arrhythmia drugs
/ Antiarrhythmics
/ Biomedical and Life Sciences
/ Biomedicine
/ Caffeine
/ Caffeine - pharmacology
/ Calcium (intracellular)
/ Calcium - metabolism
/ Cardiac arrhythmia
/ Cardiomyocytes
/ Cell Biology
/ Cell culture
/ Experiments
/ Fura-2
/ Hippocampus
/ Internal Medicine
/ Laboratory Medicine
/ Myocardium
/ Myocardium - metabolism
/ Pathology
/ Pharmacology
/ Pharmacology and Toxicologypharmacology Toxicology
/ Potassium chloride
/ Rats
/ Ryanodine - metabolism
/ Ryanodine - pharmacology
/ Ryanodine Receptor Calcium Release Channel - metabolism
/ Ryanodine receptors
/ Sarcoplasmic Reticulum
/ Software
/ Toxicology
2023
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To the Mechanism of the Antiarrhythmic Action of Compound ALM-802: the Role of Ryanodine Receptors
by
Mokrov, G. V.
, Teplov, I. Yu
, Kryzhanovskii, S. A.
, Vititnova, M. B.
, Stolyaruk, V. N.
, Zinchenko, V. P.
, Tsorin, I. B.
in
Animal experimentation
/ Animals
/ Anti-Arrhythmia Agents - pharmacology
/ Anti-arrhythmia drugs
/ Antiarrhythmics
/ Biomedical and Life Sciences
/ Biomedicine
/ Caffeine
/ Caffeine - pharmacology
/ Calcium (intracellular)
/ Calcium - metabolism
/ Cardiac arrhythmia
/ Cardiomyocytes
/ Cell Biology
/ Cell culture
/ Experiments
/ Fura-2
/ Hippocampus
/ Internal Medicine
/ Laboratory Medicine
/ Myocardium
/ Myocardium - metabolism
/ Pathology
/ Pharmacology
/ Pharmacology and Toxicologypharmacology Toxicology
/ Potassium chloride
/ Rats
/ Ryanodine - metabolism
/ Ryanodine - pharmacology
/ Ryanodine Receptor Calcium Release Channel - metabolism
/ Ryanodine receptors
/ Sarcoplasmic Reticulum
/ Software
/ Toxicology
2023
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To the Mechanism of the Antiarrhythmic Action of Compound ALM-802: the Role of Ryanodine Receptors
Journal Article
To the Mechanism of the Antiarrhythmic Action of Compound ALM-802: the Role of Ryanodine Receptors
2023
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Overview
The effect of the compound N
1
-(2,3,4-trimethoxy)-N
2
-{2-[(2,3,4-trimethoxybenzyl)amino]ethyl}-1,2-ethane-diamine (code ALM-802) on the amplitude of the Ca
2+
response in the cell was studied in
in vitro
experiments. The concentration of intracellular calcium was assessed using a Fura-2 two-wave probe. The experiments were performed on a culture of isolated rat hippocampal neurons. The effect of compound ALM-802 on the activity of ryanodine receptors (RyR2) was studied on an isolated strip of rat myocardium. The compound ALM-802 (69.8 μM) in hippocampal neurons causes a significant decrease in the amplitude of the Ca
2+
response induced by addition of KCl to the medium. Experiments performed on an isolated myocardial strip showed that compound ALM-802 (10
-5
M) almost completely blocked the positive inotropic reaction of the strip to the RyR2 agonist caffeine (5×10
-5
M). The data obtained indicate that the decrease in the concentration of Ca
2+
ions in the cell caused by ALM-802 is due to its ability to block RyR2 located on the membrane of the sarcoplasmic reticulum, which can be associated with the antiarrhythmic activity of the compound.
Publisher
Springer US,Springer,Springer Nature B.V
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