A new cyclic AMP-independent, Gs-mediated stimulatory mechanism via the adenosine A2a receptor in the intact cardiac cell

J Biol Chem. 1996 Aug 2;271(31):18678-85. doi: 10.1074/jbc.271.31.18678.

Abstract

The objectives of this study were to investigate the mechanism underlying the adenosine A2a receptor (A2aR)-mediated positive inotropic response and to define its contractile function using chick embryo ventricular cells as a model. Activation of the A2aR caused a marked stimulation of calcium entry and cell contractility, which were blocked by verapamil or nifedipine. The effects elicited by maximal concentrations of the A2aR agonist 2-[4-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadenos ine and the beta-adrenergic agonist isoproterenol were additive, indicating that the two receptors do not share a common stimulatory mechanism. The cAMP antagonist (Rp)-adenosine cyclic 3':5'-monophosphorothioate was ineffective in inhibiting the A2aR-mediated stimulation of contractility or the L-type calcium channel, while it completely abolished the isoproterenol effects. Activation of the A2aR had no effect on Na+/Ca2+ exchange or inositol 1,4,5-trisphosphate accumulation. Blocking of the A2aR resulted in unopposed A1 receptor-mediated inhibitory effects and led to an inhibition of basal contractility and an enhanced anti-adrenergic effect by A1 agonist. The adenosine A2a receptor mediates a new cyclic AMP-independent mechanism and a new contractile function in the cardiac cell.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenosine / analogs & derivatives
  • Adenosine / pharmacology
  • Adrenergic beta-Agonists / pharmacology
  • Animals
  • Calcium / metabolism
  • Calcium Channel Blockers / pharmacology
  • Cells, Cultured
  • Chick Embryo
  • Cyclic AMP / metabolism
  • GTP-Binding Proteins / metabolism*
  • Ion Transport / drug effects
  • Isoproterenol / pharmacology
  • Myocardial Contraction / drug effects
  • Myocardial Contraction / physiology
  • Myocardium / cytology
  • Myocardium / metabolism*
  • Nifedipine / pharmacology
  • Phenethylamines / pharmacology
  • Purinergic P1 Receptor Agonists
  • Receptors, Purinergic P1 / metabolism*
  • Verapamil / pharmacology

Substances

  • Adrenergic beta-Agonists
  • Calcium Channel Blockers
  • Phenethylamines
  • Purinergic P1 Receptor Agonists
  • Receptors, Purinergic P1
  • 2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine
  • Verapamil
  • Cyclic AMP
  • GTP-Binding Proteins
  • Nifedipine
  • Adenosine
  • Isoproterenol
  • Calcium