Prostaglandin E2 receptor EP1 (EP1)

The Prostaglandin E2 receptor EP1 (EP1) is a G protein-coupled receptor encoded by the PTGER1 gene that serves as a key mediator for prostaglandin E2 (PGE2) signaling (Source: UniProt P34995). Unlike other PGE2 receptors, EP1 primarily signals through the Gq/11 protein pathway, leading to the activation of phospholipase C and an increase in intracellular calcium concentration (Source: IUPHAR/BPS Guide to Pharmacology). It is prominently expressed in the kidney, gastrointestinal tract, and sensory neurons, where it facilitates nociception and the contraction of smooth muscle (Source: PubMed PMID: 11754217). Within the broader prostaglandin production pathway, EP1 acts as a downstream transducer of inflammatory signals generated by cyclooxygenase enzymes. Dysregulation of EP1 signaling is implicated in various pathologies, including inflammatory pain, overactive bladder, and the progression of certain malignancies like colorectal cancer (Source: PubMed PMID: 25635395). Pharmacological targeting of EP1 with selective antagonists is an active area of research aimed at providing analgesic relief and anti-tumor effects while minimizing the adverse effects associated with global prostaglandin inhibition (Source: PubChem).

Other names

PTGER1Prostanoid EP1 receptorPGE receptor EP1 subtypePGE2 receptor EP1Prostaglandin E receptor 1

EP1 receptor antagonists selectively bind to the EP1 receptor, inhibiting PGE2-induced Gq-protein activation and intracellular calcium mobilization, thereby reducing pain sensitization and smooth muscle hyper-reactivity (Source: IUPHAR/BPS Guide to Pharmacology).