Comparative antithrombotic activities of the phosphodiesterase inhibitors pelrinone (AY-26,768), AY-31,390 and milrinone.

  title={Comparative antithrombotic activities of the phosphodiesterase inhibitors pelrinone (AY-26,768), AY-31,390 and milrinone.},
  author={D. Patelunas and William J. Carmint and J. Willis and Thomas Colatsky and Richard L. Fenichel},
  journal={Thrombosis research},
  volume={62 5},
The phosphodiesterase (PDE) inhibitors AY-31,390, milrinone and pelrinone (AY-28,768) were analyzed in human platelet aggregatory systems and in a rabbit arteriovenous shunt model to delineate their activity. AY-31,390 showed a remarkably potent capacity to inhibit human antithrombotic platelet aggregation. AY-31,390 inhibited arachidonic acid, U46619, collagen, epinephrine (second phase) and adenosine diphosphate (second phase) induced platelet aggregation (PA) with IC50 values of 0.18, 0.21… 
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Results demonstrate that, even though this dose of pelrinone elicited near maximal inhibition of platelet aggregation, the concurrent administration of an alpha 2-adrenergic antagonist was able to potentiate markedly the phosphodiesterase inhibitor antithrombotic activity.
Role of plasma adenosine in the antiplatelet action of HL 725, a potent inhibitor of cAMP phosphodiesterase: species differences.
It is demonstrated that plasma adenosine plays a crucial role in the antiaggregatory actions of HL 725 and several other inhibitors of cAMP PDE both in human and rat blood.
Significance of plasma adenosine in the antiplatelet activity of forskolin: potentiation by dipyridamole and dilazep.
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HL 725, an extremely potent inhibitor of platelet phosphodiesterase and induced platelet aggregation in vitro.
The new pyrimido-isoquinoline compound HL 725 is an extremely potent inhibitor of the aggregation of human platelets induced in vitro by ADP, collagen, thrombin and epinephrine, higher than that of prostacyclin, the most active natural inhibitor of aggregation.
Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.
: Evaluation of a series of lactam heterocyclic analogues of cilostamide (2) as inhibitors of cyclic AMP phosphodiesterase derived from both human platelets and rat heart in comparison with their
Immunological identification of the major platelet low-Km cAMP phosphodiesterase: probable target for anti-thrombotic agents.
Several known phosphodiesterase inhibitor compounds that have been found useful in inhibiting platelet aggregation also inhibited the platelet low-Km cAMP phosphodiesters with potencies very similar to their antithrombotic effects.
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