Target intelligence / Profile preview

Prostaglandin EP and FP receptors (EP and FP receptors)

Target
EP and FP receptors
Molecular classification
G protein-coupled receptor, Prostanoid receptor, Receptor
01

Overview

Prostaglandin EP and FP receptors are a group of G protein-coupled receptors (GPCRs) that mediate the biological actions of prostaglandin E2 (PGE2) and prostaglandin F2α (PGF2α). The EP receptor family consists of four distinct subtypes (EP1, EP2, EP3, and EP4), while the FP receptor is primarily represented by a single type with various splice variants. These receptors are widely distributed throughout the body and regulate essential physiological functions such as smooth muscle tone, renal water and sodium handling, and reproductive processes like labor and ovulation. In disease states, they are heavily involved in the mediation of pain, inflammation, and the progression of certain cancers. Pharmacologically, FP receptor agonists are a mainstay in the treatment of glaucoma due to their ability to lower intraocular pressure by increasing aqueous humor outflow. EP receptor-targeted drugs are used for diverse indications, including labor induction, gastrointestinal protection, and the management of erectile dysfunction.

Other names
Prostanoid receptorsPGE2 receptorsPGF2alpha receptorsPTGERPTGFRE-prostanoid receptorsF-prostanoid receptors
02

Mechanism of action

Agonism (activation of Gs, Gq, or Gi signaling pathways depending on subtype) and Antagonism (blocking endogenous prostaglandin binding)

03

Biological functions

Signal transductionSmooth muscle contractionSmooth muscle relaxationInflammationPain perceptionRenal fluid and electrolyte balanceBlood pressure regulationUterine contractionCervical ripeningOvulationLuteolysisBone remodelingIntraocular pressure regulationGastric acid secretion inhibitionAngiogenesis
04

Disease associations

GlaucomaOcular hypertensionInflammationChronic painCancer (e.g., colorectal, lung)HypertensionAtherosclerosisPeptic ulcer diseaseDysmenorrheaEndometriosisPostpartum hemorrhageErectile dysfunction
05

Safety considerations

Gastrointestinal distress (diarrhea, nausea, abdominal cramping)Uterine contractions (risk of miscarriage or premature labor)Ocular side effects (iris pigmentation, eyelash growth, conjunctival hyperemia)Cardiovascular risks (potential for blood pressure fluctuations)Inflammatory flare-ups in certain contexts
06

Interacting drugs

Latanoprost

14 more in the full profile.

07

Biomarkers

Intraocular pressure (IOP)Prostaglandin E2 (PGE2) levelsProstaglandin F2alpha (PGF2alpha) levelsUterine activity/contractions

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