Prostaglandin E2 receptor 1 (EP1)

Prostaglandin E2 receptor 1 (EP1) is a G protein-coupled receptor encoded by the PTGER1 gene, primarily responsive to prostaglandin E2 (PGE2)[1]. It is one of four EP receptors (EP1–EP4) mediating diverse physiological and pathological processes including pain perception, blood pressure regulation, inflammatory responses, immune modulation, and neuronal excitability[1][2][5][8]. EP1 couples to Gq proteins, leading to increased intracellular calcium and activation of downstream signaling pathways. EP1 has been implicated in multiple disease contexts, such as hypertension, neurodegeneration, cancer, and inflammatory disorders. While highly conserved in mammals, key differences exist between animal models and humans regarding receptor distribution and function. Structural insight into EP1 has enabled exploration of selective modulators, although no EP1-specific drugs are yet clinically available[2][5]. Safety and efficacy of EP1 targeting remain areas of active research due to its diverse tissue roles and potential for both therapeutic benefit and adverse effects.

Other names

PTGER1EP1 receptorPGE2 EP1 receptorProstaglandin E2 EP1 receptor

Agonists stimulate EP1 receptor, leading to increased intracellular calcium signaling via Gq protein pathways Antagonists block EP1-mediated PGE2 signaling, reducing pain, inflammation, and neurotoxicity[2][5][7][8] Modulation of immune cell function (e.g., favoring Th1 cell differentiation)[1]