Cross-talk between adenosine and the oxatriazole derivative GEA 3175 in platelets

Eur J Pharmacol. 2005 Jul 11;517(3):149-57. doi: 10.1016/j.ejphar.2005.05.019.

Abstract

We examined the interplay between adenosine and the nitric oxide (NO)-containing oxatriazole derivative GEA 3175 in human platelets. The importance of cyclic guanosine 3'5'-monophosphate (cGMP)-inhibited phosphodiesterases (PDEs) was elucidated by treating the platelets with adenosine combined with either GEA 3175 or the PDE3-inhibitor milrinone. The drug combinations provoked similar cyclic adenosine 3'5'-monophosphate (cAMP) responses. On the contrary, cGMP levels were increased only in GEA 3175-treated platelets. Both drug combinations reduced P-selectin exposure, platelet adhesion and fibrinogen-binding. However, adenosine together with GEA 3175 was more effective in inhibiting platelet aggregation and ATP release. Thrombin-induced rises in cytosolic Ca2+ were suppressed by the two drug combinations. Adenosine administered with GEA 3175 was, however, more effective in reducing Ca2+ influx. In conclusion, the interaction between adenosine and GEA 3175 involves cGMP-mediated inhibition of PDE3. The results also imply that inhibition of Ca2+ influx represent another cGMP-specific mechanism that enhances the effect of adenosine.

Publication types

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

MeSH terms

  • Adenosine / pharmacology*
  • Blood Platelets / drug effects*
  • Blood Platelets / metabolism
  • Calcium / metabolism
  • Cyclic AMP / metabolism
  • Cyclic GMP / metabolism
  • Cytosol / drug effects
  • Cytosol / metabolism
  • Drug Interactions
  • Enzyme Inhibitors / pharmacology
  • Guanylate Cyclase / antagonists & inhibitors
  • Humans
  • Milrinone / pharmacology
  • Oxadiazoles / pharmacology
  • Phosphodiesterase Inhibitors / pharmacology
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology
  • Quinoxalines / pharmacology
  • Thrombin / pharmacology
  • Time Factors
  • Triazoles / pharmacology*

Substances

  • 1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
  • Enzyme Inhibitors
  • GEA 3175
  • Oxadiazoles
  • Phosphodiesterase Inhibitors
  • Platelet Aggregation Inhibitors
  • Quinoxalines
  • Triazoles
  • Cyclic AMP
  • Thrombin
  • Guanylate Cyclase
  • Cyclic GMP
  • Milrinone
  • Adenosine
  • Calcium