Prostaglandin Receptor

PGD2-IN-1 (PGD2-inhibitor) is an effective DP receptor antagonist (IC50:0.3 nM), a compound that can inhibit prostaglandin D2 (PGD2) signaling. PGD2-IN-1 specifically targets and regulates the activity of PGD2 receptors or enzymes involved IN PGD2 synthesis or metabolism.

Cis-N-Feruloyltyramine is a naturally occurring compound found in various plants that shows cytotoxicity against the P-388 cancer cell line. Cis-N-Feruloyltyramine is an inhibitor of in vitro prostaglandin (PG) synthesis.

TP-16 is a novel potent and selective EP4 antagonist that blocks the function of IMCs and enhances cytotoxic T cell-mediated tumor elimination in vivo.

Furprofen is a non-steroidal anti-inflammatory agent that inhibits prostate (PGE) synthesis and is used in the study of rheumatoid arthritis and osteoarthritis.

PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.

Octimibate (Octimibato) is a non-prostaglandin platelet aggregation inhibitor and cyclic prostaglandin agonist.Octimibate is used in the treatment of cardiovascular disease and can be used to study atherosclerosis and thrombosis.

Ethamsylate (Dicynene) usually is used as a hemostatic drug, which increases capillary endothelial resistance and platelet adhesion, and inhibits biosynthesis and action of prostaglandins.

Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Benorilate (Salipran) is the esterification product of paracetamol and acetylsalicylic acid with anti-inflammatory, analgesic and antipyretic properties.

p-Hydroxycinnamic acid (NSC-59260) can inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.

Ramatroban (BAY u3405) (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

Rebamipide (OPC12759) is a quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense.

2-Acetylbenzoic acid is more potent than 2-propionyloxybenzoic acid in inhibiting platelet function and platelet prostaglandin (PG) synthesis although the potencies of these agents were comparable in inhibiting prostacyclin (PGI2) synthesis.

Pranoprofen (Pyranoprofen) (INN) is a non-steroidal anti-inflammatory drug used in ophthalmology.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Evodiamine (d-Evodiamine) is an alkaloid isolated from the fruit of daylily and has a variety of biological activities including anti-inflammatory, anti-obesity and anti-tumor.

ETHYL 2-AMINO-4-METHYL-5-PHENYLTHIOPHENE-3-CARBOXYLATE targets the prostaglandin E2 receptor EP2 subtype (human)

ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist used to study diseases of the biblical system and metabolism-related diseases.

Terbogrel is an oral thromboxane A2 receptor antagonist (IC50 is about 10 nM) and thromboxane A2 synthase inhibitor (IC50 is about 10 nM). Terbogrel is an antiplatelet compound that inhibits platelet aggregation and is a potential compound for the prevention of blood clots.

Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.

Isbogrel (CV4151) is a small molecule thromboxane A2 synthase (TXA2 synthase) inhibitor that can be used to study cardiac arrhythmias, transient ischemic attacks and thrombosis.

RO3244794 is a selective prostacyclin (IP) receptor antagonist that can be used to study liver injury.

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

Gestonorone Capronate  is a progesterone used to treat benign prostatic hyperplasia and endometrial cancer.

Anisotropine Methylbromide is an anticholinergic agent and has been used for relief of gastrointestinal spasm and for the suppression of gastric acid secretion.

Dazmegrel HCl is a platelet thromboxane inhibitor used in the study of myocardial infarction and arrhythmias.

AZ-1355 is a novel dibenzoxepine derivative with lipid-lowering properties.

Aligeron, a non-selective prostaglandin (PG) antagonist, inhibits PGF2α- and PGE2-induced blood pressure decreases in cats and can prevent PGF2α-induced diarrhea in mice and PGE2-induced paw edema in rats. Additionally, Aligeron is recognized for its antioxidant-protective effect against vascular complications.

pirmagrel is a potent thromboxane synthase inhibitor.

L-161982 is a selective antagonist of EP4 receptor. L-161982 could inhibit PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 could alleviate collagen-induced arthritis in mice.

MK-2894 is a prostaglandin receptor 4 antagonist.MK-2894 has anti-inflammatory activity and may be used in the study of inflammation.

Omidenepag isopropyl (DE-117) is a selective prostaglandin EP2 receptor agonist and a novel topical ocular blood pressure lowering compound.Omidenepag isopropyl has a weak affinity for EP1, EP2, and FP receptors.Omidenepag isopropyl is used in studies of glaucoma and hypertension. Omidenepag isopropyl can be used to study glaucoma and hypertension.

Vedaprofen (PM 150) inhibits COX-1 and reduces prostaglandin H2 synthesis with anti-inflammatory activities. Vedaprofen is an inhibitor of Escherichia coli sliding clamp with the IC50 of 222 μM and Ki of 131 μM.

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

Tiopinac (RS 40974) has anti-inflammatory and analgesic activity, and exhibits anti-flammatory activity in adrenalectomized rats.

Aganepag, a potent Prostanoid EP2 receptor agonist, exhibits remarkable selectivity with an EC50 of 0.19 nM, demonstrating no activity at the EP4 receptor. Its applications are primarily in the fields of wound healing, scar reduction, scar prevention, and the treatment and prevention of wrinkles.

L-902688 is an orally active EP4 receptor agonist (Ki: 0.38 nM; EC50: 0.6 nM). L-902688 displays >4,000-fold selective for EP4 over other EP and prostanoid receptors.

Tebufelone is a potent in vitro inhibitor of CO , a novel non-steroidal anti-inflammatory drug (NSAID) belonging to the di-tert-butylphenol (DTBP) class that has shown potent anti-inflammatory, analgesic and anti-reticulitis properties in various animal models. Tebufelone potently inhibits the formation of prostaglandins (PGE2) and blocks the formation of lipoxygenase pathway products [leukotriene (LTB4)] in rat macrophages (IC50 = 20 microM) and human whole blood (IC50 = 22 microM) in vitro. = 20 microM) and human whole blood (IC50 = 22 microM) from the formation of lipoxygenase pathway products [leukotriene (LTB4)] in vitro.

mPGES-1 Inhibitor-1 is a novel selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with anti-inflammatory and analgesic activity for the study of acute liver injury.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

Prostaglandin E2 (PGE2) is a naturally occurring hormone involved in various physiological processes, such as smooth muscle contraction and relaxation, vasodilation and constriction, blood pressure regulation, and inflammatory regulation.

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

Tafluprost, a prostaglandin analog, is the selective agonist of fluoroprostaglandin (FP) receptor PGF2α.

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10 30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

Dinoprost methoxyamine is a hormone.

Dinoprost (Prostaglandin F2a) is a naturally occurring prostaglandin. It is used in medicine to induce labor and as an abortifacient.