Prostaglandin D2 receptor 1 (DP1) (DP1)

The Prostaglandin D2 receptor 1 (DP1) is a G protein-coupled receptor (GPCR) encoded by the PTGDR gene that serves as a primary mediator for prostaglandin D2 (PGD2) signaling [PMID: 15608146]. It is predominantly expressed in the central nervous system, platelets, vascular smooth muscle, and various immune cells, where it typically couples with Gs proteins to increase intracellular cAMP levels [UniProt: P41597]. DP1 plays a significant role in physiological processes such as vasodilation, inhibition of platelet aggregation, and the regulation of the sleep-wake cycle [PMID: 10661069]. In pathology, DP1 is implicated in allergic inflammation, asthma, and the cutaneous flushing response induced by nicotinic acid (niacin) [PMID: 18317531]. Therapeutic strategies have targeted DP1 with antagonists like laropiprant to reduce niacin-induced flushing, although clinical challenges regarding efficacy and safety have limited its widespread use [PMID: 23445415]. Additionally, DP1 agonists have been explored for their potential in treating glaucoma and cardiovascular conditions due to their ability to modulate intraocular pressure and vascular tone [PMID: 15608146]. The receptor's involvement in both central and peripheral systems makes it a complex but valuable target for drug development in respiratory and inflammatory medicine.

Other names

PTGDRDP receptorProstanoid DP receptorPGD receptorASRT

DP1 receptor antagonists (e.g., laropiprant) work by competitively inhibiting the binding of PGD2 to the DP1 receptor, thereby preventing Gs-mediated activation of adenylate cyclase and subsequent vasodilation or inflammatory responses [PMID: 18317531]. Conversely, DP1 agonists (e.g., BW245C) mimic PGD2 to increase intracellular cAMP, which can lead to platelet inhibition or bronchodilation [PMID: 15608146].