[On the function of beta3-adrenoceptors in the human heart: signal transduction, inotropic effect and therapeutic prospects].
Beta-adrenergic stimulation is an important regulatory mechanism of cardiac function. Next to beta1- and beta2-adrenoceptors, the expression of a third beta-adrenoceptor population, the beta3-adrenoceptor, has recently been evidenced in the human heart. Stimulation of cardiac beta3-adrenoceptors leads to a decrease in contractility via a release of nitric oxide (NO). In this context, different molecular mechanisms of endothelial nitric oxide synthase (eNOS) activation have been uncovered to occur as a consequence of beta3-adrenergic stimulation. In both nonfailing and failing myocardium, beta3-adrenergic stimulation may have a protective effect against excessive chatecolaminergic stimulation as it occurs during somatic and mental stress and during heart failure. For this reason, the beta3-adrenoceptor is discussed as a possible target for the pharmacological therapy of heart failure.
Pott
Christian
C
Universitätsklinikum Münster, Medizinische Klinik und Poliklinik C für Kardiologie und Angiologie, Münster, Germany. christian.pott@ukmuenster.de
Steinritz
Dirk
D
Napp
Andreas
A
Bloch
Wilhelm
W
Schwinger
Robert H G
RH
Brixius
Klara
K
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000627:therapeutic use; D002395:Catecholamines / Q000502:physiology; D004730:Endothelium, Vascular / Q000187:drug effects / Q000503:physiopathology; D004789:Enzyme Activation / Q000187:drug effects / Q000502:physiology; D004983:Ethanolamines / Q000627:therapeutic use; D006321:Heart / Q000187:drug effects / Q000503:physiopathology*; D006333:Heart Failure / Q000188:drug therapy / Q000503:physiopathology; D006801:Humans; D009200:Myocardial Contraction / Q000187:drug effects / Q000502:physiology*; D009569:Nitric Oxide / Q000378:metabolism; D019001:Nitric Oxide Synthase / Q000378:metabolism; D022702:Receptors, Adrenergic, beta-3 / Q000502:physiology*; D015398:Signal Transduction / Q000187:drug effects / Q000502:physiology*; D013315:Stress, Psychological / Q000150:complications
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; D002395:Catecholamines; D004983:Ethanolamines; D022702:Receptors, Adrenergic, beta-3; D009569:Nitric Oxide; C057368:BRL 37344; D019001:Nitric Oxide Synthase