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Beta-3 adrenoceptors as new therapeutic targets for cardiovascular pathologies.

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Gauthier, Chantal Rozec, Bertrand Manoury, Boris [UCL] Balligand, Jean-Luc [UCL]

Catecholamines play a key role in the regulation of cardiovascular function, classically through ß(1/2)-adrenoreceptors (AR) activation. After ß(3)-AR cloning in the late 1980s, convincing evidence for ß(3)-AR expression and function in cardiovascular tissues recently initiated a reexamination of their involvement in the pathophysiology of cardiovascular diseases. Their upregulation in diseased cardiovascular tissues and resistance to desensitization suggest they may be attractive therapeutic targets. They may substitute for inoperant ß(1/2)-AR to mediate vasodilation in diabetic or atherosclerotic vessels. In cardiac ventricle, their contractile effects are functionally antipathetic to those of ß(1/2)-AR; in normal heart, ß(3)-ARs may mediate a moderate negative inotropic effect, but in heart failure, it may protect against adverse effects of excessive catecholamine stimulation by action on excitation-contraction coupling, electrophysiology, or remodelling. Thus, prospective studies in animals and patients at different stages of heart failure should lead to identify the best therapeutic window to use ß(3)-AR agonists and/or antagonists.

Document type Article de périodique (Journal article) – Journal Article, Research Support, Non-U.S. Gov't, Review
Access type Accès libre
Publication date 2011
Language Anglais
Journal information "Current Heart Failure Reports" - Vol. 8, no. 3, p. 184-192 (2011)
Peer reviewed yes
Publisher Current Medicine Group LLC
issn 1546-9530
e-issn 1546-9549
Publication status Publié
Affiliations UCL - SSS/IREC/FATH - Pôle de Pharmacologie et thérapeutique
UCL - SSS/IREC - Institut de recherche expérimentale et clinique
UCL - (SLuc) Service de médecine interne et maladies infectieuses (MIMI)
MESH Subject Ventricular Remodeling ; Sepsis - drug therapy - metabolism - physiopathology ; Receptors, Adrenergic, beta-3 - physiology ; Myocardial Infarction - drug therapy - metabolism - physiopathology ; Myocardial Contraction - drug effects - physiology ; Models, Animal ; Liver Cirrhosis - drug therapy - metabolism - physiopathology ; Hypothyroidism - drug therapy - metabolism - physiopathology ; Hypertension - drug therapy - metabolism - physiopathology ; Humans ; Heart Failure - drug therapy - metabolism - physiopathology ; Gene Expression - drug effects - physiology ; Diabetes Mellitus - drug therapy - metabolism - physiopathology ; Cardiovascular System - drug effects - metabolism - physiopathology ; Animals ; Aging - physiology ; Adrenergic beta-Antagonists - pharmacology ; Adrenergic beta-3 Receptor Agonists - pharmacology
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Bibliographic reference Gauthier, Chantal ; Rozec, Bertrand ; Manoury, Boris ; Balligand, Jean-Luc. Beta-3 adrenoceptors as new therapeutic targets for cardiovascular pathologies.. In: Current Heart Failure Reports, Vol. 8, no. 3, p. 184-192 (2011)
Permanent URL http://hdl.handle.net/2078.1/82290