Exposure of isolated bovine coronary arteries to high glucose (30 mmol/l d -glucose) but not to osmotic control mannitol (30 mmol/l) switched angiotensin II-stimulated prostacyclin (PGI 2 )-dependent relaxation into a persistent vasoconstriction that was sensitive to either indomethacin, a cyclooxygenase inhibitor, or SQ29548, a selective thromboxane receptor antagonist. (diabetesjournals.org)
Ramatroban is "an orally-active, dual Gpr44 and thromboxane A2 receptor antagonist" which was developed in Germany. (nicehair.org)
A specific example is ramatroban, an orally-active, dual Gpr44 and thromboxane A2 receptor antagonist, which is approved in Japan for the treatment of allergic rhinitis in humans Future studies could examine the effect of ramatroban in stimulating hair follicle neogenesis. (nicehair.org)
Ramatroban is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. (csnpharm.com)
Galangin functions as an antagonist of the aryl hydrocarbon receptor and also inhibits CYP1A1 (IC50 1 M). It belongs to flavonoids and can be extracted from the rhizome of Zingiber officinale Roscoe with anti-inflammatory properties. (csnpharm.com)
Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. (csnpharm.com)
Prostaglandin-endopero1
Therefore, COX - also known as prostaglandin-endoperoxide synthase (PTGS), fatty acid COX, prostaglandin H (PGH) synthase, and EC 1.14.99.1 - is implicated in the production of fever, inflammation, and pain. (medscape.com)
Signal transduction3
Disorders of receptors and signal transduction: platelet cyclo-oxygenase deficiency, thromboxane synthase deficiency, thromboxane A2 receptor defect, ADP receptor defect. (calcuttayellowpages.com)
In addition, the results showed that LGP suppressed Ras homolog family member A and phosphoinositide 3‑kinase/Akt/glycogen synthase kinase 3β signal transduction. (spandidos-publications.com)
The NK1 receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema. (csnpharm.com)
Inhibitor3
Stiripentol is an antiepileptic drug that can inhibit the synaptosomal uptake of GABA, increase the activation of GABAA receptors, its also a microsomal cytochrome P450 (CYP) isoforms CYP3A4, CYP1A2, and CYP2C19 inhibitor. (csnpharm.com)
Ozagrel Sodium, also known as KCT-0809 and Cataclot, is a thromboxane A2 synthase inhibitor used to treat cerebrovascular diseases. (csnpharm.com)
Dazoxiben hydrochloride is a potent, orally active thromboxane (TX) synthase inhibitor that reduces the formation of blood clots. (csnpharm.com)
Endothelial6
In the present study, we aimed to study the roles of endothelial nitric oxide synthase (eNOS) in diabetes. (diabetesjournals.org)
There is an overwhelming mass of evidence demonstrating the development of endothelial dysfunction in animal models of diabetes and in human blood vessels from diabetic patients, as evidenced by increased release of reactive oxygen species, decreased nitric oxide (NO) bioactivity, decreased release of prostacyclin (PGI 2 ), and enhanced endothelial production of vasoconstrictor thromboxane (Tx)A 2 /prostaglandin (PG)H 2 in early stages of diabetes ( 1 - 3 ). (diabetesjournals.org)
However, many disease-predisposing factors and/or contributing factors have been identified, including inflammation, endothelial cell dysfunction, aberrant vascular wall cell proliferation and mutations in the bone morphogenetic protein-receptor type 2 ( Bmpr2 ) gene [ 1 - 3 ]. (ersjournals.com)
This is primarily accomplished by timely and balanced production and release of endothelial relaxing factors, namely, nitric oxide, prostacyclin, or endothelium-derived hyperpolarizing factor [2C4], as well as endothelium-derived contracting autacoids, such as endothelin-1, thromboxane A2, angiotensin II, or superoxide anion. (mundial-brasil2014.net)
Endothelial dysfunction can be primarily seen as a impaired rules of vascular shade due to decreased endothelial nitric oxide synthase activity, insufficient cofactors for nitric oxide synthesis, attenuated nitric oxide launch, or improved nitric oxide degradation. (mundial-brasil2014.net)
Pharmacological strategy in enhancing/reversal of endothelial dysfunction was been shown to be helpful in medical YKL-06-061 trails which have looked into Pramlintide Acetate activities of angiotensin switching enzyme inhibitors, angiotensin receptor blockers, statins and additional lipid lowering real estate agents, calcium route blockers, some circumstances. (mundial-brasil2014.net)
Inhibition1
These inhibitory effects may be associated with its dual‑receptor inhibition on P2Y12 and TP receptors. (spandidos-publications.com)
Polyunsaturated fatt1
Their distinct biosynthetic activity includes an endoperoxidase synthase reaction that oxygenates and cyclizes polyunsaturated fatty acid precursors (eg, arachidonic acid) to form prostaglandin G 2 (PGG2), and a peroxidase reaction that converts PGG2 to prostaglandin H 2 (PGH2), as shown below. (medscape.com)
Selective2
Hikida T , Yawata S , Yamaguchi T, Danjo T, Sasaoka T, Wang Y, Nakanishi S . Pathway-specific modulation of nucleus accumbens in reward and aversive behavior via selective transmitter receptors. (neurotree.org)
Yawata S , Yamaguchi T, Danjo T, Hikida T , Nakanishi S . Pathway-specific control of reward learning and its flexibility via selective dopamine receptors in the nucleus accumbens. (neurotree.org)
Platelet activation1
Available antiplatelet agents, such as cyclooxygenase-1 (COX-1) inhibitors (aspirin), ADP P2Y 12 receptor antagonists, and GP IIb/IIIa receptor inhibitors, are effective and save in the treatment and prevention of thrombotic events, these drugs interfere with the platelet activation process, including adhesion, release, and aggregation. (hindawi.com)
Agonist1
Schisandrin A is a naturally occuring agonist of the adiponectin receptor 2 with an IC50 value of 3.5 M. (csnpharm.com)
Synthesis1
It was also found that LGP exhibited marked inhibitory effects on the activation of αIIbβ3 integrin, the secretion of serotonin from granules, and the synthesis of thromboxane A2. (spandidos-publications.com)
P2Y121
Data from a radiolabeled ligand‑binding assay indicated that LGP exhibited apparent competing effects on thromboxane receptor (TP) and P2Y12 receptors. (spandidos-publications.com)
PGE21
In turn, PGH2 is converted to biologically active products (ie, prostaglandin E 2 [PGE2]) by individual synthase and reductase reactions. (medscape.com)
Platelets1
They contain denser granules, secrete more serotonin and β -thromboglobulin, produce more thromboxane A2 and have more adhesion molecules (like P-selectin and platelet glycoprotein-GP-IIbIIIa), than smaller platelets. (hindawi.com)
Superoxide1
In parallel, high glucose, but not mannitol, significantly increased superoxide and 3-nitrotyrosine in PGI 2 synthase (PGIS). (diabetesjournals.org)
Protein3
Structure-activity relationships of agonists for the orphan G protein-coupled receptor GPR27. (uliege.be)
In S. Martins & D. Prazeres, G Protein-Coupled Receptor Screening Assays - Methods in Molecular Biology (pp. 149-157). (uliege.be)
We show that prostaglandin D2 synthase (PTGDS) is elevated at the mRNA and protein levels in bald scalp compared to haired scalp of men with AGA. (nicehair.org)
Inhibits1
We have demonstrated that Prostaglandin D2 is elevated in male balding scalp and that it functionally inhibits hair lengthening through its receptor GPR44, which directly suggests treatments for male pattern hair loss. (nicehair.org)
Binds2
Phenol red in cell culture medium binds to receptors on cell surfaces and causes the cell to respond as though pharmacologic levels of estrogen and/or inflammatory mediators (such as prostaglandin or thromboxane A2) are present in the medium. (cell-systems.com)
Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. (csnpharm.com)
Enzyme1
2009). Rather, there can be an anatomical demarcation in enzymes that regulate this process in which MAGL plays this role not only in the brain, but also in the liver and lung, whereas cytosolic phospholipase A2 (cPLA2) is the dominant AA-releasing enzyme in gut, spleen and macrophages (Bonventre et al. (tuskonus.org)
Inflammatory1
MAGL blockade decreases bulk AA amounts in the mind, to 2-AG elevation stoichiometrically, which also leads to a reduced amount of lipopolysaccharide (LPS)-induced pro-inflammatory degrees of downstream COX-driven prostaglandin and thromboxane creation in the mind (Nomura et al. (tuskonus.org)
Family1
Superconserved receptors expressed in the brain: Expression, function, motifs and evolution of an orphan receptor family. (uliege.be)
Mouse1
Peptide (C)RAPHWYASHMKTR, corresponding to amino acid residues 137-149 of mouse prostanoid EP3 receptor (Accession P34980 ). (alomone.com)