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Prostaglandin E2 receptor (EP receptor) (EP receptor (or EP1, EP2, EP3, EP4, as subtypes))

Target
EP receptor (or EP1, EP2, EP3, EP4, as subtypes)
Molecular classification
G protein-coupled receptor, Receptor, Eicosanoid receptor, Rhodopsin-like receptor
01

Overview

**Prostaglandin E2 receptors (EP receptors)** are a family of four G protein-coupled receptors (EP1, EP2, EP3, EP4) encoded by separate genes (PTGER1–4) that mediate the effects of prostaglandin E1 (PGE1) and prostaglandin E2 (PGE2) in various tissues[5][10]. While there is no specific, unique "prostaglandin E1 receptor," PGE1 exerts its effects by binding to these EP receptors and the prostaglandin I (IP) receptor[2][5]. Each EP receptor subtype has distinct signaling mechanisms: EP2 and EP4 couple with Gs proteins to stimulate cAMP production, EP1 couples with Gq to mobilize intracellular Ca²⁺, and EP3 couples to Gi to inhibit cAMP formation[5][10]. PGE1 and its analogues like alprostadil and misoprostol mediate vasodilation, inhibit platelet aggregation, relax or contract smooth muscle, and have important clinical applications in cardiovascular, gastrointestinal, and reproductive medicine[1][9]. These receptors are considered therapeutic targets for drugs aimed at managing erectile dysfunction, maintaining ductus arteriosus patency in neonates, preventing gastric ulcers, and managing inflammation and pain[1][6][9]. **Clarification on correctness:** - There is no distinct, unique "Prostaglandin E1 receptor"—the canonical targets are the four EP receptor subtypes (EP1–EP4), which recognize both PGE1 and PGE2, along with some affinity for the IP receptor[2][5][10]. Therefore, the term "Prostaglandin E1 receptor" is non-standard and should be mapped to "Prostaglandin E2 receptor" (EP receptor, including EP1, EP2, EP3, EP4) for canonical structuring.

Other names
Prostaglandin E receptorEP receptorEP1 receptorEP2 receptorEP3 receptorEP4 receptorPTGER1 (EP1 gene)PTGER2 (EP2 gene)PTGER3 (EP3 gene)PTGER4 (EP4 gene)
02

Mechanism of action

- Activation of G protein-coupled signaling pathways (different subtypes couple to Gs, Gi, or Gq proteins) - Increase of intracellular cAMP (via EP2, EP4, IP) - Increase of intracellular Ca²⁺ (EP1) - Decrease of intracellular cAMP (EP3) - Inhibition of platelet aggregation (via IP and EP3) - Cytoprotection of gastric mucosa

03

Biological functions

Signal transductionVasodilationSmooth muscle relaxation/contractionPlatelet inhibitionInhibition of gastric acid secretionMediation of inflammationRegulation of immune responseMediation of pain and feverCytoprotection in various tissues
04

Disease associations

Cardiovascular diseaseInflammationErectile dysfunctionUlcer diseaseReproductive disorders (e.g., induction of labor, abortion)Cirrhosis/Liver diseasePeptic ulcer disease
05

Safety considerations

Hypotension/low blood pressureBronchospasmUterine contractions (risk in pregnancy)Bleeding risk (due to platelet inhibition)Diarrhea, abdominal pain (gastrointestinal side effects)
06

Interacting drugs

Alprostadil

3 more in the full profile.

07

Biomarkers

Expression of PTGER1–4 gene (EP1–4 receptor expression)cAMP and Ca²⁺ signaling activation states

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