Effects of A(3) adenosine receptor activation and gene knock-out in ischemic-reperfused mouse heart

Cardiovasc Res. 2002 Jan;53(1):147-55. doi: 10.1016/s0008-6363(01)00424-2.

Abstract

Objectives: To characterize effects of A(3) adenosine receptor (A(3)AR) activation and gene knock-out on responses to ischemia-reperfusion in mouse heart.

Methods: Perfused hearts from wild-type and A(3)AR gene knock-out (A(3)AR KO) mice were subjected to 20 min ischemia and 30 min reperfusion. Functional responses were assessed and changes in energy metabolism and cytosolic pH monitored via 31P-NMR spectroscopy.

Results: Selective A(3)AR agonism with 100 nM 2-chloro-N(6)-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (chloro-IB-MECA) enhanced post-ischemic contractile recovery without altering contracture development in wild-type hearts, an effect unrelated to non-selective activation of A(1) or A(2) adenosine receptors. Chloro-IB-MECA also improved recovery in hearts overexpressing A(1)ARs. Paradoxically, post-ischemic recovery was enhanced by A(3)AR KO. Developed pressure, +dP/dt, and -dP/dt all recovered to higher levels in A(3)AR KO (70-80% of pre-ischemia) vs. wild-type hearts (45-50% of pre-ischemia) (P<0.05). Enhanced recovery was unrelated to recoveries of ATP, phosphocreatine (PCr), inorganic phosphate (P(i)), energy state ([ATP]/[ADP] x [P(i)], DeltaG(ATP)) or cytosolic pH.

Conclusions: Selective A(3)AR activation is cardioprotective in wild-type hearts and hearts overexpressing A(1)ARs, yet A(3)AR gene deletion generates an ischemia-tolerant phenotype without altering energy metabolism or pH. This may be due to compensatory changes or undefined genotypic differences in A(3)AR KO vs. wild-type hearts.

Publication types

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

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / analysis
  • Adenosine / pharmacology
  • Amino Acids / pharmacology
  • Animals
  • Creatine / analysis
  • Heart Rate / drug effects
  • Hydrogen-Ion Concentration
  • Magnetic Resonance Spectroscopy
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Myocardial Contraction* / drug effects
  • Myocardial Reperfusion Injury / metabolism*
  • Myocardium / chemistry
  • Myocardium / metabolism*
  • Perfusion
  • Phenethylamines / pharmacology
  • Pipecolic Acids / pharmacology
  • Purinergic P1 Receptor Antagonists
  • Quinazolines / pharmacology
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1 / genetics
  • Receptors, Purinergic P1 / metabolism*
  • Triazoles / pharmacology
  • Xanthines / pharmacology

Substances

  • 9-chloro-2-(2-furyl)-5-phenylacetylamino(1,2,4)triazolo(1,5-c)quinazoline
  • Amino Acids
  • Phenethylamines
  • Pipecolic Acids
  • Purinergic P1 Receptor Antagonists
  • Quinazolines
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1
  • Triazoles
  • Xanthines
  • 2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine
  • cyclopentenosine
  • 1,3-dipropyl-8-cyclopentylxanthine
  • Adenosine
  • Creatine