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Regulation of Cardiac β<sub>3</sub>-Adrenergic Receptors in Hyperglycemia

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Field Value
 
Title Regulation of Cardiac β3-Adrenergic Receptors in Hyperglycemia
 
Creator Turan, Belma
Tuncay, Erkan
 
Subject β-Blockers
β-Adrenoceptor subtypes
Heart function
Oxidative stress
Diabetes mellitus
 
Description 483-492
Beta-adrenoceptors (β-AR), members of the G
protein-coupled receptors play important roles in the regulation of heart
function. A positive inotropic action of catecholamines is mediated through
their interaction with β-AR, located on the sarcolemma, while they can also
mediate some deleterious effects, such as cardiac arrhythmias or myocardial
apoptosis. The well-known β-AR-associated signaling in heart is composed of a
coupled mechanism among both β1- and β2-AR and
stimulatory G protein (Gs). This coupled mechanism further leads to
the activation of adenylyl cyclase and thereby increases in intracellular cAMP
level. However, recent studies have emphasized the contribution of constitutive
β3-AR coupling to Gi proteins, thereby initiating
additional signal transduction pathways, particularly under physiopathological
conditions. Diabetic cardiomyopathy, as a distinct entity is recognized due to
its diminished responsiveness to β1-AR agonist stimulation in the
heart from diabetic rats with no important changes in the responses mediated
with β2-AR. Furthermore, an upregulation of β3-AR has
been shown in diabetic rat heart with a strong negative inotropic effect on
left ventricular function. Experimental data provide evidences that the
mechanisms for the negative inotropic effect with β3-AR activation
appear to involve a pertussis toxin (PTX)-sensitive
G protein and the activation of a nitric oxide synthase pathway. On the other
hand, β-blockers demonstrate marked beneficial effects in heart dysfunction
with scavenging free radicals and/or acting as an antioxidant with both sex-
and dose-dependent manner. However, further investigations are needed to
clarify the roles of both altered expression and/or responsiveness of β-AR and
the benefits with β-blocker treatment in diabetes. This review discusses the
role of β-AR activation, particularly β3-AR in cardiac pathological remodeling under hyperglycemia.
 
Date 2015-02-11T04:23:45Z
2015-02-11T04:23:45Z
2014-12
 
Type Article
 
Identifier 0975-0959 (Online); 0301-1208 (Print)
http://hdl.handle.net/123456789/30497
 
Language en_US
 
Rights CC Attribution-Noncommercial-No Derivative Works 2.5 India
 
Publisher NISCAIR-CSIR, India
 
Source IJBB Vol.51(6) [December 2014]