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February 5, 2009ACS Chemical Biology

Antagonists of the EP3 Receptor for Prostaglandin E2 Are Novel Antiplatelet Agents That Do Not Prolong Bleeding

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Key result

DG-041, a selective EP3 antagonist, inhibited PGE2-facilitated platelet aggregation without prolonging bleeding time in rats, suggesting a superior safety profile to P2Y12 antagonists.

Why the study?

Does DG-041 inhibit platelet aggregation without prolonging bleeding time in preclinical models?

Population

In vitro/ex vivo platelets and rat models

Comparison

DG-041, alone or co-administered with clopidogrel vs Clopidogrel alone or control

Design

Preclinical

Authors

JSJasbir SinghManagement Sciences (United States)WZWayne E. ZellerU.S. Dairy Forage Research CenterNZNian ZhouGuangxi Medical University

Discussion

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Overview

May support EP3 antagonism for safer antiplatelet effects; leaves open human trials to confirm translation.

Structured PICO

Does DG-041 inhibit platelet aggregation without prolonging bleeding time in preclinical models?

P
Population
In vitro/ex vivo platelets and rat models
I
Intervention
DG-041 (selective EP3 antagonist), alone or co-administered with clopidogrel
C
Comparator
Clopidogrel alone or control
O
Outcome
Platelet aggregation and bleeding timesurrogate

DG-041 is a novel EP3 antagonist that inhibits platelet aggregation without increasing bleeding risk in preclinical models, suggesting a potentially safer antiplatelet profile.

Cite This Study

Singh et al. (2009) studied Atherothrombosis. DG-041 vs. clopidogrel was evaluated on PGE2 facilitation of platelet aggregation and bleeding time. DG-041, a selective EP3 antagonist, inhibited PGE2-facilitated platelet aggregation without prolonging bleeding time in rats, suggesting a superior safety profile to P2Y12 antagonists.

synapsesocial.com/papers/6a6ae6c747a1bfb288f2f6c7https://doi.org/10.1021/cb8002094
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1DG-041 inhibits the EP3 prostanoid receptor—A new target for inhibition of platelet function in atherothrombotic disease2008 · 68 citations
  2. 2Blocking the EP3 receptor for PGE2 with DG-041 decreases thrombosis without impairing haemostatic competence2013 · 53 citations
  3. 3Inhibiting thrombosis without causing bleeding: can EP3 blockers fulfil the dream?2014 · 5 citations
  4. 4The Prostaglandin E2Receptor EP4 Is Expressed by Human Platelets and Potently Inhibits Platelet Aggregation and Thrombus Formation2010 · 87 citations
  5. 5Blocking the receptor EP3 to PGE2 as a way to safely prevent atherothrombosis2016