Target intelligence / Profile preview

Prostamide receptor (PM receptor) (PM receptor)

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

Overview

The Prostamide receptor is a specialized G protein-coupled receptor (GPCR) primarily located in the trabecular meshwork and uveoscleral outflow pathways of the eye (Woodward et al., 2008). While its molecular identity was historically elusive, it is now understood to be a unique pharmacological entity, potentially involving a heterodimeric complex of the Prostaglandin F (FP) receptor and its splice variant, FP-alt (Liang et al., 2008). This receptor is the primary target for bimatoprost, a synthetic prostamide analog used to treat open-angle glaucoma and ocular hypertension. Unlike traditional prostaglandin analogs that mainly target the uveoscleral route, activation of the prostamide receptor enhances aqueous humor drainage through both the conventional trabecular meshwork and unconventional uveoscleral pathways (Wan et al., 2007). This dual-outflow mechanism results in a potent reduction of intraocular pressure, which is critical for preventing optic nerve damage. Beyond the eye, the receptor is also found in hair follicles, where its activation promotes the transition of hair into the anagen (growth) phase, leading to its use in treating eyelash hypotrichosis. Common clinical observations associated with its activation include conjunctival hyperemia, iris hyperpigmentation, and periorbital fat atrophy (Brubaker et al., 2001).

Other names
Bimatoprost receptorProstamide F2α receptorFP-alt receptor complexProstaglandin F2α ethanolamide receptor
02

Mechanism of action

Agonism of the prostamide receptor increases aqueous humor drainage via both the trabecular meshwork (conventional) and uveoscleral (unconventional) pathways.

03

Biological functions

Regulation of intraocular pressureAqueous humor outflow regulationSignal transduction
04

Disease associations

GlaucomaOcular hypertensionEyelash hypotrichosis
05

Safety considerations

Conjunctival hyperemiaIris hyperpigmentationEyelash growth (trichomegaly)Periorbital fat atrophyOcular irritation
06

Interacting drugs

Bimatoprost
07

Biomarkers

Intraocular pressure (IOP)

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