Antiarrhythmic activity in occlusion-reperfusion model of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino} propan-2-ol and its enantiomers. 2016

Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
Department of Pharmacological Screening, Jagiellonian University Medical College, Kraków, Poland.

Acute myocardial infarction (AMI) is a leading cause of mortality and morbidity worldwide, especially in developed countries. The most serious problem after myocardial infarction is reperfusion injury that manifests as functional impairment, arrhythmia, and accelerated progression of cell death in certain critically injured myocytes. Subsequently the infarcted myocardium develops features of necrosis and reactive inflammation. To reduce lethal reperfusion injury in patient with AMI antioxidants, anti-inflammatory agents, adenosine, opioids, metabolic modulators (glucose, insulin, and potassium, nicorandil and agents which reduce intracellular Ca(2+) overload and inhibit Na(+)-H(+) exchange) are used. In this study a novel compound (compound 9) 1-(1 h-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy) ethyl]amino}propan-2-ol and its enantiomers are examined in arrhythmia associated with coronary artery occlusion and reperfusion in a rat model. Antioxidant properties are also determined for test compounds using the malondialdehyde (MDA) lipid peroxidation and ferric reducing antioxidant power (FRAP) tests. In summary, the tested compounds, especially the S enantiomer has a strong antiarrhythmic activity in a model of occlusion and reperfusion of the left coronary artery which is probably related to their adrenolytic action. In contrast to carvedilol, none of the test compound reduced the lipid peroxidation but increased ferric reducing antioxidant power. In the antioxidant effect, there was no difference between the optical forms of compound 9.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D008297 Male Males
D010084 Oxidation-Reduction A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471). Redox,Oxidation Reduction
D011412 Propanolamines AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives. Aminopropanols
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D002118 Calcium A basic element found in nearly all tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes. Coagulation Factor IV,Factor IV,Blood Coagulation Factor IV,Calcium-40,Calcium 40,Factor IV, Coagulation
D004195 Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. Animal Disease Model,Animal Disease Models,Disease Model, Animal
D004562 Electrocardiography Recording of the moment-to-moment electromotive forces of the HEART as projected onto various sites on the body's surface, delineated as a scalar function of time. The recording is monitored by a tracing on slow moving chart paper or by observing it on a cardioscope, which is a CATHODE RAY TUBE DISPLAY. 12-Lead ECG,12-Lead EKG,12-Lead Electrocardiography,Cardiography,ECG,EKG,Electrocardiogram,Electrocardiograph,12 Lead ECG,12 Lead EKG,12 Lead Electrocardiography,12-Lead ECGs,12-Lead EKGs,12-Lead Electrocardiographies,Cardiographies,ECG, 12-Lead,EKG, 12-Lead,Electrocardiograms,Electrocardiographies, 12-Lead,Electrocardiographs,Electrocardiography, 12-Lead
D006321 Heart The hollow, muscular organ that maintains the circulation of the blood. Hearts
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

Related Publications

Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
February 2009, European journal of medicinal chemistry,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
July 2011, Acta crystallographica. Section C, Crystal structure communications,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
February 2020, Toxicology letters,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
November 2004, International journal of pharmaceutics,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
August 2012, Chirality,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
April 2012, Acta crystallographica. Section E, Structure reports online,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
January 2006, Acta poloniae pharmaceutica,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
January 2013, Acta crystallographica. Section E, Structure reports online,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
October 2010, Acta crystallographica. Section E, Structure reports online,
Marek Bednarski, and Monika Otto, and Magdalena Dudek, and Agata Siwek, and Małgorzata Zygmunt, and Joanna Knutelska, and Leszek Nowiński, and Grażyna Groszek, and Jacek Sapa
April 2006, Journal of medicinal chemistry,
Copied contents to your clipboard!