Synapse
⌘+K
Synapse
PulseExploreClubsResearchersJournals
Instagram
HomeClubsExplore
January 1, 2010Thrombosis and Haemostasis

Selective activation of the prostaglandin E2 receptor subtype EP2 or EP4 leads to inhibition of platelet aggregation

View Full Paper
Ask AI
Bookmark
Share

Key result

Selective activation of EP2 or EP4 by agonists AE1-259 and AE1-329 potently inhibited U-46619-induced platelet aggregation, with AE1-329 showing an IC50 of 2.3 nM in human platelets.

Population

Platelets prepared from wild-type mice, EP2-/- mice, EP4-/- mice, and human platelets

Comparison

Selective activation of EP2 or EP4 using… vs Wild-type vs knockout platelets; presence vs…

Design

Preclinical

Authors

KYKoh‐ichi YuhkiFKFumiaki KojimaTYTakehiro Yamada

Discussion

Loading...

Member takes

Overview

EP4 agonists merit preclinical exploration as antiplatelet agents; leaves open translation to human efficacy and safety trials.

Structured PICO

P
Population
Platelets prepared from wild-type mice, EP2-/- mice, EP4-/- mice, and human platelets
I
Intervention
Selective activation of EP2 or EP4 using agonists AE1-259 and AE1-329, respectively, and PGE2
C
Comparator
Wild-type vs knockout platelets; presence vs absence of EP4 antagonist AE3-208
O
Outcome
Inhibition of platelet aggregation induced by U-46619 or ADPsurrogate

Selective activation of EP2 or EP4 receptors inhibits platelet aggregation, suggesting EP4 agonists may serve as novel anti-platelet agents.

Cite This Study

Yuhki et al. (2010) studied this question. Selective activation of EP2 or EP4 (AE1-259 and AE1-329) vs. Wild-type platelets / EP2-/- and EP4-/- platelets was evaluated on Inhibition of U-46619-induced platelet aggregation. Selective activation of EP2 or EP4 by agonists AE1-259 and AE1-329 potently inhibited U-46619-induced platelet aggregation, with AE1-329 showing an IC50 of 2.3 nM in human platelets.

synapsesocial.com/papers/6a9460bed1fa461db0c57787https://doi.org/10.1160/th10-01-0043
View Full Paper
Ask AI
Bookmark
Share

Also Consider

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

  1. 1The Prostaglandin E2Receptor EP4 Is Expressed by Human Platelets and Potently Inhibits Platelet Aggregation and Thrombus Formation2010 · 87 citations
  2. 2Activation of the murine EP3 receptor for PGE2 inhibits cAMP production and promotes platelet aggregation2001 · 173 citations
  3. 3PGE2reverses Gs-mediated inhibition of platelet aggregation by interaction with EP3 receptors, but adds to non-Gs-mediated inhibition of platelet aggregation by interaction with EP4 receptors2012 · 12 citations
  4. 4The role of prostanoid receptors in mediating the effects of PGE<sub>2</sub>on human platelet function2010 · 61 citations
  5. 5Increased Bleeding Tendency and Decreased Susceptibility to Thromboembolism in Mice Lacking the Prostaglandin E Receptor Subtype EP <sub>3</sub>2001 · 109 citations