Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?

U Deniz DincerDepartment of Pharmacology, Ufuk University School of Medicine. Mevlana Bulvari, Balgat, Ankara, TurkeyAbstract: Metabolic syndrome is characterized by a combination of obesity, hypertension, insulin resistance, dyslipidemia, and impaired glucose tolerance. This multifaceted syndrome i...

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Autor principal:	Dincer UD
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Specialties of internal medicine RC581-951
Acceso en línea:	https://doaj.org/article/12d8b20c84574c369ff7c6f48d103471
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spelling	oai:doaj.org-article:12d8b20c84574c369ff7c6f48d1034712021-12-02T00:55:49ZCardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?1178-7007https://doaj.org/article/12d8b20c84574c369ff7c6f48d1034712012-04-01T00:00:00Zhttp://www.dovepress.com/cardiac-ryanodine-receptor-in-metabolic-syndrome-is-jtv519-k201-future-a9641https://doaj.org/toc/1178-7007U Deniz DincerDepartment of Pharmacology, Ufuk University School of Medicine. Mevlana Bulvari, Balgat, Ankara, TurkeyAbstract: Metabolic syndrome is characterized by a combination of obesity, hypertension, insulin resistance, dyslipidemia, and impaired glucose tolerance. This multifaceted syndrome is often accompanied by a hyperdynamic circulatory state characterized by increased blood pressure, total blood volume, cardiac output, and metabolic tissue demand. Experimental, epidemiological, and clinical studies have demonstrated that patients with metabolic syndrome have significantly elevated cardiovascular morbidity and mortality rates. One of the main and frequent complications seen in metabolic syndrome is cardiovascular disease. The primary endpoints of cardiometabolic risk are coronary and peripheral arterial disease, myocardial infarction, congestive heart failure, arrhythmia, and stroke. Alterations in expression and/or functioning of several key proteins involved in regulating and maintaining ionic homeostasis can cause cardiac disturbances. One such group of proteins is known as ryanodine receptors (intracellular calcium release channels), which are the major channels through which Ca2+ ions leave the sarcoplasmic reticulum, leading to cardiac muscle contraction. The economic cost of metabolic syndrome and its associated complications has a significant effect on health care budgets. Improvements in body weight, blood lipid profile, and hyperglycemia can reduce cardiometabolic risk. However, constant hyperadrenergic stimulation still contributes to the burden of disease. Normalization of the hyperdynamic circulatory state with conventional therapies is the most reasonable therapeutic strategy to date. JTV519 (K201) is a newly developed 1,4-benzothiazepine drug with antiarrhythmic and cardioprotective properties. It appears to be very effective in not only preventing but also in reversing the characteristic myocardial changes and preventing lethal arrhythmias. It is also a unique candidate to improve diastolic heart failure in metabolic syndrome.Keywords: ryanodine receptors, metabolic syndrome, JTV519, K201Dincer UDDove Medical PressarticleSpecialties of internal medicineRC581-951ENDiabetes, Metabolic Syndrome and Obesity: Targets and Therapy, Vol 2012, Iss default, Pp 89-99 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Specialties of internal medicine RC581-951
spellingShingle	Specialties of internal medicine RC581-951 Dincer UD Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?
description	U Deniz DincerDepartment of Pharmacology, Ufuk University School of Medicine. Mevlana Bulvari, Balgat, Ankara, TurkeyAbstract: Metabolic syndrome is characterized by a combination of obesity, hypertension, insulin resistance, dyslipidemia, and impaired glucose tolerance. This multifaceted syndrome is often accompanied by a hyperdynamic circulatory state characterized by increased blood pressure, total blood volume, cardiac output, and metabolic tissue demand. Experimental, epidemiological, and clinical studies have demonstrated that patients with metabolic syndrome have significantly elevated cardiovascular morbidity and mortality rates. One of the main and frequent complications seen in metabolic syndrome is cardiovascular disease. The primary endpoints of cardiometabolic risk are coronary and peripheral arterial disease, myocardial infarction, congestive heart failure, arrhythmia, and stroke. Alterations in expression and/or functioning of several key proteins involved in regulating and maintaining ionic homeostasis can cause cardiac disturbances. One such group of proteins is known as ryanodine receptors (intracellular calcium release channels), which are the major channels through which Ca2+ ions leave the sarcoplasmic reticulum, leading to cardiac muscle contraction. The economic cost of metabolic syndrome and its associated complications has a significant effect on health care budgets. Improvements in body weight, blood lipid profile, and hyperglycemia can reduce cardiometabolic risk. However, constant hyperadrenergic stimulation still contributes to the burden of disease. Normalization of the hyperdynamic circulatory state with conventional therapies is the most reasonable therapeutic strategy to date. JTV519 (K201) is a newly developed 1,4-benzothiazepine drug with antiarrhythmic and cardioprotective properties. It appears to be very effective in not only preventing but also in reversing the characteristic myocardial changes and preventing lethal arrhythmias. It is also a unique candidate to improve diastolic heart failure in metabolic syndrome.Keywords: ryanodine receptors, metabolic syndrome, JTV519, K201
format	article
author	Dincer UD
author_facet	Dincer UD
author_sort	Dincer UD
title	Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?
title_short	Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?
title_full	Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?
title_fullStr	Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?
title_full_unstemmed	Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?
title_sort	cardiac ryanodine receptor in metabolic syndrome: is jtv519 (k201) future therapy?
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/12d8b20c84574c369ff7c6f48d103471
work_keys_str_mv	AT dincerud cardiacryanodinereceptorinmetabolicsyndromeisjtv519k201futuretherapy
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Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy?

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