Target intelligence / Profile preview

Prostanoid receptor (PR)

Target
PR
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Prostamide/prostanoid receptor target encompasses a family of G protein-coupled receptors that respond to lipid signaling molecules derived from arachidonic acid. The term specifically highlights the 'prostamide receptor,' a pharmacologically distinct entity often identified as a heterodimer of the prostaglandin F (FP) receptor and its splice variants, which is the primary target for the anti-glaucoma drug bimatoprost. These receptors are critical regulators of physiological processes such as intraocular pressure, vascular tone, and inflammatory responses. In the eye, their activation enhances the drainage of aqueous humor through both uveoscleral and trabecular pathways, making them central to the management of glaucoma and ocular hypertension. Additionally, their role in hair follicle cycling has led to the use of agonists for enhancing eyelash growth. Beyond ophthalmology, members of the prostanoid receptor family are targeted for treating pulmonary hypertension and various inflammatory conditions, reflecting their broad biological significance.

Other names
Prostamide receptorProstamide F receptorProstaglandin receptorFP receptorFP-altFP heterodimerProstaglandin F2-alpha receptor
02

Mechanism of action

Agonism of the receptor leads to increased uveoscleral and trabecular outflow of aqueous humor, relaxation of ciliary muscles, and remodeling of the extracellular matrix to lower intraocular pressure. In other tissues, activation can lead to vasodilation, inhibition of platelet aggregation, or induction of labor depending on the specific receptor subtype (e.g., IP, EP, or FP).

03

Biological functions

Signal transductionRegulation of intraocular pressureAqueous humor outflowSmooth muscle contractionInflammationPain perceptionPlatelet aggregationCell proliferation
04

Disease associations

GlaucomaOcular hypertensionHypotrichosisInflammationCardiovascular diseasePulmonary arterial hypertensionAsthma
05

Safety considerations

Conjunctival hyperemiaIris hyperpigmentationEyelash changes (trichomegaly)Ocular irritationProstaglandin-associated periorbitopathy (periorbital fat loss)Systemic effects such as headache or flushing (for systemic agonists)
06

Interacting drugs

Bimatoprost

11 more in the full profile.

07

Biomarkers

Intraocular pressure (IOP)Eyelash lengthEyelash thicknessMean pulmonary arterial pressure

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