Coupling of adenosine receptors to a pertussis toxin-sensitive G protein in the human heart

European Journal of Pharmacology
M BöhmE Erdmann

Abstract

The adenosine receptors in myocardial membranes of human explanted hearts were labeled with the radiolabeled ligand [3H]DPCPX (1,3-dipropyl-8-cyclopentylxanthine). Agonist competition curves revealed high- and low-affinity states. The addition of guanylyl imidodiphosphate (Gpp (NH)p) converted all receptors to a low-affinity state. The portion of high-affinity states and the influence of guanine nucleotides were most pronounced at 22 degrees C. Only low-affinity states could be detected in pertussis toxin-treated membranes. It is concluded that adenosine receptors in the human ventricle couple via a G protein sensitive to pertussis-toxin. Alterations of the coupling of adenosine receptors might have a pathophysiological role in dilated cardiomyopathy in which pertussis toxin substrates are increased.

Citations

Mar 1, 1994·Journal of the American College of Cardiology·J KoglinE Erdmann
Jun 1, 1992·The American Journal of Medicine·A C RankinB A McGovern

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