Delving into the Latest Updates on AP-155 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

PDE1C

Action

inhibitors

Mechanism

PDE1C inhibitors(phosphodiesterase 1C inhibitors), Platelet aggregation inhibitors

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Myocardial IschemiaThrombosis

Originator Organization

University of Genova

Active Organization-

Inactive Organization

University of Genova

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

The effect on human platelets of 2-(1-piperazinyl)-4H-pyrido[1,2-a]pyrimi din-4-one (AP155) was tested in vitro by measuring cyclic adenosine monophosphate (cAMP) level, cytosolic Ca++, [(125I)]fibrinogen binding as well as aggregation induced by several agonists. AP155 dose-dependently inhibited aggregation both in platelet rich plasma (PRP) and in washed platelets (WP), exerting its maximal power in the presence of collagen, ADP and platelet activating factor (PAF). It specifically inhibited the activity of cAMP high affinity phosphodiesterase (PDE), resulting in a sufficient increase in cAMP levels to activate cAMP-dependent protein kinase. AP155 was able to inhibit aggregation, the increase in cytosolic Ca++ induced by thrombin, and fibrinogen binding to ADP or thrombin-stimulated platelets. Thus, this new pyridopyrimidine derivative exerts its antiplatelet activity by increasing cAMP intracellular concentration.

100 Deals associated with AP-155

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