spare receptors
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2021 ◽  
Vol 22 (14) ◽  
pp. 7584
Author(s):  
Régis Guieu ◽  
Michele Brignole ◽  
Jean Claude Deharo ◽  
Pierre Deharo ◽  
Giovanna Mottola ◽  
...  

While the concept of a receptor reserve (spare receptors) is old, their presence on human cells as an adaptive mechanism in cardiovascular disease is a new suggestion. The presence of spare receptors is suspected when the activation of a weak fraction of receptors leads to maximal biological effects, in other words, when the half-maximal effective concentration (EC50) for a biological effect (cAMP production, for example) is lower than the affinity (KD) of the ligand for a receptor. Adenosine is an ATP derivative that strongly impacts the cardiovascular system via its four membrane receptors, named A1R, A2AR, A2BR, and A3R, with the A1R being more particularly involved in heart rhythm, while the A2AR controls vasodilation. After a general description of the tools necessary to explore the presence of spare receptors, this review focuses on the consequences of the presence of spare adenosine receptors in cardiovascular physiopathology. Finally, the role of the adenosinergic system in the long-term potentiation and its possible consequences on the physiopathology are also mentioned.


2019 ◽  
Vol 20 (23) ◽  
pp. 5964 ◽  
Author(s):  
Emmanuel Fenouillet ◽  
Giovanna Mottola ◽  
Nathalie Kipson ◽  
Franck Paganelli ◽  
Régis Guieu ◽  
...  

Adenosine and its receptors exert a potent control on the cardiovascular system. This review aims to present emerging experimental evidence supporting the existence and implication in cardiovascular disorders of specific adenosinergic pharmacological profiles, conforming to the concept of “receptor reserve”, also known as “spare receptors”. This kind of receptors allow agonists to achieve their maximal effect without occupying all of the relevant cell receptors. In the cardiovascular system, spare adenosine receptors appear to compensate for a low extracellular adenosine level and/or a low adenosine receptor number, such as in coronary artery disease or some kinds of neurocardiogenic syncopes. In both cases, the presence of spare receptors appears to be an attempt to overcome a weak interaction between adenosine and its receptors. The identification of adenosine spare receptors in cardiovascular disorders may be helpful for diagnostic purposes.


FEBS Open Bio ◽  
2012 ◽  
Vol 3 (1) ◽  
pp. 1-5 ◽  
Author(s):  
Laurent Jacquin ◽  
Frédéric Franceschi ◽  
Youlet By ◽  
Josée-Martine Durand-Gorde ◽  
Jocelyne Condo ◽  
...  

2007 ◽  
Vol 21 (5) ◽  
Author(s):  
Stephen Rush Fuhs ◽  
Richard A Bundey ◽  
Zhenghong Ling ◽  
Paul A Insel

2005 ◽  
Vol 203 (1) ◽  
pp. 31-39 ◽  
Author(s):  
Y. Marunaka ◽  
N. Niisato ◽  
H. Miyazaki
Keyword(s):  

1997 ◽  
Vol 356 (3) ◽  
pp. 283-292 ◽  
Author(s):  
E. Agneter ◽  
E. A. Singer ◽  
W. Sauermann ◽  
T. J. Feuerstein

Synapse ◽  
1995 ◽  
Vol 21 (2) ◽  
pp. 177-187 ◽  
Author(s):  
Val J. Watts ◽  
Cindy P. Lawler ◽  
Andrea J. Gonzales ◽  
Qun-Yong Zhou ◽  
Olmer Civelli ◽  
...  

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