Pinacidil pretreatment improves vascular reactivity after shock through PKCα and PKCε in rats

J Cardiovasc Pharmacol. 2012 Jun;59(6):514-22. doi: 10.1097/FJC.0b013e31824d4d75.

Abstract

We investigated the beneficial effect of pinacidil pretreatment on vascular reactivity, calcium sensitivity, and animal survival after hemorrhagic shock, its relationship to protein kinase Cα (PKCα), protein kinase Cε (PKCε), and adenosine. Using hemorrhagic shock rats, the protective effects of different extents of pinacidil pretreatment on vascular reactivity and in which the roles of PKCα, PKCε, and adenosine were observed. Pinacidil pretreatment significantly improved shock-induced decrease of vascular reactivity of superior mesenteric artery, which was antagonized by the PKCα antagonist Gö-6976 (5 × 10 mole/L) and PKCε pseudosubstrate inhibitory peptide (1 × 10 mole/L). Pinacidil pretreatment induced the translocation of PKCα and PKCε from the cytoplasm to the membrane. This translocation of PKCα and PKCε was eliminated by adenosine A1 receptor antagonist DPCPX (1 × 10 mole/L). As compared with simple fluid resuscitation, combination with pinacidil pretreatment significantly improved the vascular reactivity and survival rate of hemorrhagic-shocked rats. These results suggested that pinacidil pretreatment could induce good protective effects on vascular reactivity and calcium sensitivity after hemorrhagic shock mainly through the activation of PKCα and PKCε via adenosine A1 receptor, and this protective effect made an important contribution to the overall outcome of shock therapy.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / metabolism
  • Animals
  • Calcium / metabolism
  • Disease Models, Animal
  • Female
  • Fluid Therapy / methods
  • Male
  • Mesenteric Artery, Superior / drug effects
  • Mesenteric Artery, Superior / metabolism
  • Pinacidil / pharmacology*
  • Protein Kinase C-alpha / metabolism*
  • Protein Kinase C-epsilon / metabolism*
  • Protein Transport / drug effects
  • Rats
  • Rats, Wistar
  • Receptor, Adenosine A1 / drug effects
  • Receptor, Adenosine A1 / metabolism
  • Resuscitation / methods
  • Shock, Hemorrhagic / drug therapy*
  • Shock, Hemorrhagic / physiopathology
  • Shock, Hemorrhagic / therapy
  • Survival Rate
  • Vasodilator Agents / pharmacology
  • Xanthines / pharmacology

Substances

  • Receptor, Adenosine A1
  • Vasodilator Agents
  • Xanthines
  • Pinacidil
  • 1,3-dipropyl-8-cyclopentylxanthine
  • Protein Kinase C-alpha
  • Protein Kinase C-epsilon
  • Adenosine
  • Calcium