Prostaglandin Receptor Antagonist

Laropiprant sodium is a potent and selective DP receptor antagonist with K_i values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

MK-8318 is a potent and selective CRTh2 receptor antagonist with a K_i of 5.0 nM.

ARRY-502 is an orally active, potent and selective CRTh2 antagonist. ARRY-502 blocks PGD2-mediated Th2 inflammation (e.g., eosinophil activation, airway hyperresponsiveness). ARRY-502 is promising for research of Th2-related asthma.

ICI 185282 is a potent, selective, orally active thromboxane A2 (TXA₂) receptor antagonist. ICI 185282 causes dose-dependent inhibition of U-46619 (HY-108566)-induced platelet aggregation ex-vivo in guinea-pig. ICI 185,282 inhibits bronchospasm induced by U-46619, PGD₂ (HY-101988), PGF_2α (HY-12956), arachidonic acid (HY-109590), LTD₄ and PAF (HY-108635) in vivo. ICI 185282 can be used for bronchial asthma research.

ACT-774312 is a potent and selective CRTH2 antagonist with an IC₅₀ of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD₂-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.

GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain.

MK-1029 is a DP2 antagonist. MK-1029 can be used in research on respiratory diseases such as asthma.

NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats.

(R)-Vorbipiprant ((R)-CR6086) is an orally active antagonist for prostaglandin E2 receptor 4 (EP4) with K_i of 16.6 nM for human EP4. (R)-Vorbipiprant inhibits PGE2 (HY-101952)-induced cAMP production with an IC₅₀ of 22 nM. (R)-Vorbipiprant exhibits immunomodulatory and anti-angiogenic activities, and ameliorates the collagen-induced arthritis in mice.

TGI-15 is a highly selective prostaglandin F receptor antagonist. TGI-15 inhibits downstream signaling pathways by blocking the binding of PGF2 α to FP receptors. TGI-15 can be used for research on fibrotic and inflammatory conditions.

EP1 receptor antagonist-1 (Compound Example 5a freebase) is an EP1 prostaglandin receptor antagonist. EP1 receptor antagonist-1 is promising for research of urinary system-related diseases.

ASP7657 free base is an orally active EP4 receptor antagonist, with K_is of 2.21 and 6.02 nM for the human and rat EP4 receptors.

(S)-Trimetoquinol hydrochloride (Compound 1) is a apotent, nonselective, nonclassical β-adrenergic agonist and nonprostanoid thromboxane A2/prostaglandin H2 antagonist. (S)-Trimetoquinol hydrochloride can be used for research of neurological and cardiovascular disease.

CGS 22652 is a potent thromboxane A2 receptor antagonist. CGS 22652 has selective thromboxane A2 synthase inhibitory properties. CGS 22652 can be used in the research of coronary artery thrombosis.

I-SAP is a radioiodinated TXA2/PGH2 receptor antagonist. The bind between I-SAP and the receptors, is inhibited by the histidine modifying reagent diethyl-pyrocarbonate (DEPC).

AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.

MF266-1 is a selective E prostanoid receptor 1 (EP1) antagonist with an K_i value of 3.8 nM. MF266-1 also has moderate selectivity for thromboxane A2 receptor (TP). MF266-1 is promising for research of arthritis.

KF15766 (compd 34E) is an orally active TXA₂ and H₁ dual antagonist with K_is of 740 and 20 nM. KF15766 can be used for antiallergic research.

Domitroban is a thromboxane A2 receptor (TBXA2R) antagonist. Domitroban can inhibit platelet aggregation. Domitroban can be used for the research of cardiovascular disease, such as thrombosis.

EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a K_i value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes.