Cardioprotective properties of the platelet P2Y12 receptor inhibitor prasugrel on cardiac ischemia/reperfusion injury

Pharmacol Rep. 2020 Jun;72(3):672-679. doi: 10.1007/s43440-019-00046-5. Epub 2020 Jan 13.

Abstract

Objective: The effects of prasugrel, a third-generation thienopyridine, on myocardial infarction, and ischemia-induced ventricular arrhythmias was evaluated in open-chest anesthetized rats. The role of protein kinase C and phosphoinositide 3-kinase pathways in these effects was also examined.

Methods: The effect of P2Y12 receptor inhibition by prasugrel (3-10 mg/kg, po) on infarct size after 30-min coronary artery occlusion and 120-min reperfusion or on arrhythmias after 7-min coronary occlusion and 7-min reperfusion was evaluated.

Results: In the control group, 31.25 ± 3.01% of the risk zone infarcted. At both prasugrel doses, infarct size was significantly smaller than that in the control group: 5.03 ± 0.81% for 3 mg/kg (p < 0.0001), and 8.78 ± 2.04% for 10 mg/kg (p < 0.0001). The protein kinase C antagonist chelerythrine abolished the anti-infarct effect of prasugrel at 24.77 ± 1.73% as did the phosphoinositide 3-kinase antagonist wortmannin abolished the anti-infarct effect of prasugrel at 27.45 ± 2.74%. Ten mg/kg prasugrel reduced the duration of VT (p = 0.0152 vs control), and wortmannin, but not chelerythrine, reversed the effect of prasugrel on arrhythmias (p = 0.0295).

Conclusion: The selective P2Y12 inhibitor prasugrel provides effective protection against myocardial infarction and ischemia-induced ventricular arrhythmias in rats. As in ischemic postconditioning, protein kinase C and phosphoinositide 3-kinase signaling pathways play a role in this protection.

Keywords: Arrhythmia; Myocardial ischemia/reperfusion injury; P2Y12 receptor; PI3K; PKC.

MeSH terms

  • Animals
  • Arrhythmias, Cardiac / drug therapy
  • Hemodynamics / drug effects
  • Male
  • Myocardial Infarction / drug therapy
  • Myocardial Infarction / pathology
  • Myocardial Reperfusion Injury / drug therapy*
  • Myocardial Reperfusion Injury / metabolism
  • Myocardial Reperfusion Injury / pathology
  • Platelet Aggregation Inhibitors / pharmacology*
  • Prasugrel Hydrochloride / pharmacology*
  • Purinergic P2Y Receptor Agonists / pharmacology*
  • Rats
  • Rats, Wistar
  • Receptors, Purinergic P2Y12

Substances

  • P2ry12 protein, rat
  • Platelet Aggregation Inhibitors
  • Purinergic P2Y Receptor Agonists
  • Receptors, Purinergic P2Y12
  • Prasugrel Hydrochloride