Prostaglandin F receptor–alternative splice variant heterodimer (FP–altFP)

The Prostamide receptor is a pharmacological target characterized as a heterodimeric complex formed by the wild-type Prostaglandin F (FP) receptor and its alternative splice variant, altFP (Woodward et al., 2013, Drug Discovery Today). This heterodimer was identified to explain the unique activity of prostamides, such as bimatoprost, which do not interact with the standard FP receptor in the same manner as traditional prostaglandins (Liang et al., 2008, Journal of Biological Chemistry). The receptor is primarily expressed in ocular tissues, where it plays a vital role in regulating intraocular pressure by increasing the uveoscleral outflow of aqueous humor (Woodward et al., 2003, British Journal of Pharmacology). Clinically, it is the primary target for drugs like bimatoprost used in the management of glaucoma and ocular hypertension. Additionally, the receptor's presence in hair follicles mediates the stimulation of eyelash growth, leading to its application in treating hypotrichosis (Filippi et al., 2013, Journal of Ocular Pharmacology and Therapeutics). Pharmacological targeting of this heterodimer is associated with specific side effects, including conjunctival hyperemia and periorbital fat loss, which are distinct from those of pure FP receptor agonists.

Other names

Prostamide receptorBimatoprost receptorFP-altFP complexProstamide F2α receptor

Agonism of the FP–altFP heterodimer increases uveoscleral outflow of aqueous humor and stimulates hair follicle transition to the anagen phase.