The anti-aggregating effect of BAY 41-2272, a stimulator of soluble guanylyl cyclase, requires the presence of nitric oxide

Br J Pharmacol. 2010 Nov;161(5):1044-58. doi: 10.1111/j.1476-5381.2010.00943.x.

Abstract

Background and purpose: The purpose of the present study was to determine whether a stimulator of soluble guanylyl cyclase, BAY 41-2272, inhibits platelet aggregation and to clarify its interaction with nitric oxide (NO).

Experimental approach: Blood was collected from anaesthetized Wistar Kyoto rats. The aggregation of washed platelets was measured and the production of cAMP and cGMP was determined.

Key results: In adenosine 5'-diphosphate (ADP)-induced platelet aggregation, the anti-aggregating effects of BAY 41-2272, nitroglycerin, sodium nitroprusside and DEA-NONOate were associated with increased levels of cGMP while that of beraprost, a prostacyclin analogue, was correlated with an increase in cAMP. 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) prevented the effects of BAY 41-2272 and that of nitroglycerin and sodium nitroprusside, but only inhibited the increase in cGMP produced by of DEA-NONOate. Hydroxocobalamin, an NO scavenger, inhibited the effects of the three NO donors and BAY 41-2272 but did not affect those of beraprost. ADP-induced aggregation and the effects of BAY 41-2272 were not affected by L-nitroarginine. A positive interaction was observed between BAY 41-2272 and the three NO donors. BAY 41-2272 potentiated also the anti-aggregating effects of beraprost, and again this potentiation was inhibited by hydroxocobalamin.

Conclusions and implications: Inhibition of platelet aggregation by BAY 41-2272 requires the reduced form of soluble guanylyl cyclase and the presence of NO. The positive interaction observed between BAY 41-2272 and various NO donors is qualitatively similar whatever the mechanism involved in NO release. Furthermore, a potent synergism is observed between BAY 41-2272 and a prostacyclin analogue, but only in the presence of NO.

MeSH terms

  • Animals
  • Cyclic AMP / metabolism
  • Cyclic GMP / metabolism
  • Drug Interactions
  • Drug Synergism
  • Epoprostenol / analogs & derivatives
  • Epoprostenol / pharmacology
  • Guanylate Cyclase / metabolism*
  • Male
  • Nitric Oxide / metabolism*
  • Nitric Oxide Donors / pharmacology
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology*
  • Pyrazoles / pharmacology*
  • Pyridines / pharmacology*
  • Rats
  • Rats, Inbred WKY
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Soluble Guanylyl Cyclase

Substances

  • 3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo(3,4-b)pyridine
  • Nitric Oxide Donors
  • Platelet Aggregation Inhibitors
  • Pyrazoles
  • Pyridines
  • Receptors, Cytoplasmic and Nuclear
  • Nitric Oxide
  • beraprost
  • Epoprostenol
  • Cyclic AMP
  • Guanylate Cyclase
  • Soluble Guanylyl Cyclase
  • Cyclic GMP