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. 1989 Oct 17;172(4-5):407-11.
doi: 10.1016/0922-4106(89)90022-9.

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

M Böhm  1 , P Gierschik, M Ungerer, E Erdmann
Affiliations

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

M Böhm et al. Eur J Pharmacol. .

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.

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