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Modulation of receptor sensitivity: possible therapeutic target?
Author(s) -
Cohen Michel V,
Downey James M
Publication year - 2009
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2009.00115.x
Subject(s) - cardioprotection , receptor , medicine , pharmacology , adenosine receptor , adenosine , ischemic preconditioning , adenosine a1 receptor , desensitization (medicine) , g protein coupled receptor , myocardial infarction , agonist , cardiology , ischemia
Ischaemic preconditioning and post‐conditioning are cardioprotective interventions that salvage ischaemic myocardium and reduce infarct size. Yet this cardioprotective effect is not the sole response of the heart to ischaemic preconditioning and post‐conditioning. It was known that protein kinase C activation in the signalling cascade of ischaemic preconditioning increased the affinity of the adenosine A 2b receptor so that much lower concentrations of adenosine caused A 2b receptor‐dependent signalling. In this issue of the British Journal of Pharmacology , these cardioprotective interventions are shown to block desensitization of surface receptors on the sarcolemma of the cardiomyocyte and this receptor effect is divorced from any cardioprotection. Modulating receptor function through signalling pathways is a novel idea but, currently, whether these observations have any clinical relevance is not known. Additional investigations are warranted to determine whether this effect on receptors can be generalized to other surface receptors, and whether the effect can be harnessed to improve treatment of the patient with acute myocardial infarction.