. 2017 Jun 13;77(12):1281–1294. doi: 10.1007/s40265-017-0777-2

Table 1.

Comparison between CRTH2 and DP receptors (based on Nagata and Hirai [14])

	CRTH2	DP
Main agonist	PGD₂, PGJ₂	PGD₂, PGJ₂
Selective agonist	Δ¹²-PGD₂, Δ¹²-PGJ₂, DK-PGD₂, 15d-PGJ₂, 15d-PGJ₂, indomethacin L888,607	BW245C
G protein coupled	G_i	G_s
Intracellular changes upon activation	Decrease in cAMP Increase in Ca²⁺	Increase in cAMP
Biological effect	Increase in cell migration, chemotaxis, shape change activation of eosinophils, basophils, and Th₂ cells, promotion of Th₂ inflammation and Th₂-type cytokine production (IL-4, 5, 13), upregulation of adhesion molecules	Inhibition of platelet aggregation, vasodilation, relaxation of smooth muscles, inhibition of cell migration, inhibition of apoptosis
Selective antagonists	AM211, AM156, ARRY-502, TASP0376377, MK-7246, AZD1981^a, OC000459^a, setipiprant^a, BI 671800^a	Laropiprant^a
Dual antagonist for CRTH2 and DP	AMG853^a
Dual antagonist for CRTH2 and TP	Ramatroban^b

cAMP cyclic adenosine monophosphate, CRTH2 chemoattractant receptor-homologous molecule on T helper type 2 cells, DP D-prostanoid, TP thromboxane prostanoid

^aCurrently under clinical evaluation

^bApproved for allergic rhinitis in Japan