Receptor Subtype Abundance as a Tool for Effective Intracellular Signalling

Author(s): Jaromir Myslivecek, Martina Novakova, Martin Klein.

Journal Name:Cardiovascular & Hematological Disorders-Drug Targets

Volume 8 , Issue 1 , 2008


The regulation of heart function is one of the essentials for the survival of organism. Therefore, the effective mechanisms of regulation can minimize the energy requirements and improve the ability to react to different needs on time and appropriately . Two receptor types, β-adrenoceptors and muscarinic receptors, with almost antagonistic function, are “basic regulators” of the heart parameters. It is relevant to mention that beside the main adrenoceptors and muscarinic receptors subtypes (β1- and M2-subtype), other minor subtypes that regulate heart function, i.e. β2-, β3-adrenoceptors, α1-adrenoceptors and minor subtypes of muscarinic receptors (M1, M3 and M5) are present in the heart. In this regard is intriguing that just two catecholamines (adrenaline, noradrenaline) have many “targets” – receptors that differ so much in the functional consequences of their activation: while β1- and β2-adrenoceptors cause cardiostimulation, β3-adrenoceptors are responsible for cardioinhibition and α1-adrenoceptors contribute to enhanced inotropy. Similarly, some data show that other muscarinic receptors than M2 muscarinic subtype, are expressed in the heart and these minor subtype(s) can contribute to the heart regulation in similar way as β3-adrenoceptors to the catecholamine action. Taken together, regulation of heart function through different receptor subtypes and using homologous and heterologous regulation can represent an effective tool for coping with permanently changing environmental conditions.

Keywords: Adrenoceptors, muscarinic receptors, heart, G protein coupled receptor regulation

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Article Details

Year: 2008
Page: [66 - 79]
Pages: 14
DOI: 10.2174/187152908783884939