InhibitorAntagonistSignal transductionInhibitionProstacyclinPlateletsTXA2CyclooxygenaseVasoconstrictorProstaglandin-endoperoPulmonaryInhibitsKinasePGE2AgonistProstaglandinsAryl hydrocarEndothelialEstrogen ReceptorsPolyunsaturated fattSelectiveGeneSynthesisPGISP2Y12PhospholipaseBindsProstanoidPGD2MRNAGPR44VivoLungNeuropathic PainPatientsAssayMembranePeptideMotifsActivation
Inhibitor5
- 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)
- an inhibitor of protein kinase A (PKA). (geogise.com)
- 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)
Antagonist5
- 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)
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)
Inhibition1
- These inhibitory effects may be associated with its dual‑receptor inhibition on P2Y12 and TP receptors. (spandidos-publications.com)
Prostacyclin2
- 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)
- Prostanoids are made by the sequential activities of cyclooxygenase (COX) and particular prostanoid synthases to produce prostaglandin PGD2, PGE2, PGF2, prostacyclin (PGI2), and thromboxane A2 (TXA2) (Fig. 1). (mdm2-inhibitors.com)
Platelets3
- Thromboxane A2 (TXA2) is a type of thromboxane that is produced by activated platelets during hemostasis and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation. (wikipedia.org)
- Circulating fibrinogen binds these receptors on adjacent platelets, further strengthening the clot. (wikipedia.org)
- 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)
TXA25
- Receptors that mediate TXA2 actions are thromboxane A2 receptors. (wikipedia.org)
- The human TXA2 receptor (TP) is a typical G protein-coupled receptor (GPCR) with seven transmembrane segments. (wikipedia.org)
- TXA2 is generated from prostaglandin H2 by thromboxane-A synthase in a metabolic reaction which generates approximately equal amounts of 12-Hydroxyheptadecatrienoic acid (12-HHT). (wikipedia.org)
- TXA2 is very unstable in aqueous solution, since it is hydrated within about 30 seconds to the biologically inactive thromboxane B2. (wikipedia.org)
- PGI2 counteracts the vasoconstrictor and platelet aggregation ramifications of thromboxane A2 (TXA2), and both prostanoids make an important stability in cardiovascular homeostasis. (mdm2-inhibitors.com)
Cyclooxygenase4
- Aspirin irreversibly inhibits platelet cyclooxygenase 1 preventing the formation of prostaglandin H2, and therefore thromboxane A2. (wikipedia.org)
- 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)
- Thus, the term ' prostanoids ' relates to the products of the cyclooxygenase pathway ( prostaglandins , prostacyclins , and thromboxanes ) but to compounds produced by free radical-catalyzed mechanism ( Isoprotanes, phytoprostanes, neuroprostanes ). (gerli.com)
- To summarize the cyclooxygenase metabolism, prostaglandin G/H synthase catalyzes the sequential formation of PGG2 and PGH2 (they are both named endoperoxides) by addition of molecular oxygen at the C9, C11 and C15 positions. (gerli.com)
Vasoconstrictor1
- Thromboxane A2 is also a known vasoconstrictor and is especially important during tissue injury and inflammation. (wikipedia.org)
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)
Pulmonary2
- 1989. Adenosine produces pulmonary vasoconstriction in sheep: Evidence for thromboxane A2- prostaglandin endoperoxide receptor activation. (hopkinsmedicine.org)
- Pulmonary vascular effects of prostaglandin D2 but not its systemic vascular or airway effects are mediated through thromboxane receptor activation. (hopkinsmedicine.org)
Inhibits2
- 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)
- oncogenic II areas will be the localized years primary for central self-induced atrium by other medicaments in activity oxidant and, more Moreover, enhance if and by what neurohormone Toxicology A2 inhibits book only renal hypofunction in this disorder. (hone.world)
Kinase1
- Thromboxane A2-induced contraction of rat caudal arterial smooth muscle involves activation of Ca2+ entry and Ca2+sensitization: Rho-associated kinase-mediated phosphorylation of MYPT1 at Thr-855 but not Thr-697" (PDF). (wikipedia.org)
PGE21
- In turn, PGH2 is converted to biologically active products (ie, prostaglandin E 2 [PGE2]) by individual synthase and reductase reactions. (medscape.com)
Agonist1
- Schisandrin A is a naturally occuring agonist of the adiponectin receptor 2 with an IC50 value of 3.5 M. (csnpharm.com)
Prostaglandins1
- This term includes prostaglandins, prostacyclins, thromboxanes, and related substances, but 'prostaglandins' is often used loosely to include all prostanoids. (gerli.com)
Aryl hydrocar1
- Forkhead box P3 (FoxP3) and aryl hydrocarbon receptor (AhR) mRNA levels were assessed by real-time polymerase chain reaction. (bvsalud.org)
Endothelial2
- In the present study, we aimed to study the roles of endothelial nitric oxide synthase (eNOS) in diabetes. (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)
Estrogen Receptors1
- Purpose Estrogenic endocrine disruptors acting via estrogen receptors and have already been implicated in the etiology of hypospadias. (hoot4owls.org)
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)
Gene1
- Gene ontology functional enrichment analysis was performed using search tool for the retrieval of interacting genes/proteins. (ijpsonline.com)
Synthesis2
- 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)
- This simplified development protocol has the potential to entice fresh entrants to cell-free protein synthesis and to broaden the pool of applications. (geogise.com)
PGIS1
- In parallel, high glucose, but not mannitol, significantly increased superoxide and 3-nitrotyrosine in PGI 2 synthase (PGIS). (diabetesjournals.org)
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)
Phospholipase2
- I. Launch Eicosanoids are lipid mediators produced from the hydrolysis of membrane phospholipids by phospholipase A2 (PLA21) into arachidonic acidity (AA), the main element molecule in eicosanoid biosynthesis. (mdm2-inhibitors.com)
- 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)
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)
Prostanoid1
- Peptide (C)RAPHWYASHMKTR, corresponding to amino acid residues 137-149 of mouse prostanoid EP3 receptor (Accession P34980 ). (alomone.com)
PGD21
- GPR44 is a PGD2 receptor. (nicehair.org)
MRNA3
- The transcription of COX-1 yields a 2.7-kilobase (kb) messenger ribonucleic acid (mRNA) that encodes a 576-residue, 65-kd protein. (medscape.com)
- Conversely, the transcription of COX-2 yields a 4.5-kb mRNA that encodes a 70-kd protein with roughly 70-75% homology to the COX-1 protein. (medscape.com)
- 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)
GPR441
- Gpr44 is one of the receptors of Prostaglandin D2 . (nicehair.org)
Vivo1
- Klinisch bedeutsame Substanzen wie Clopidogrel oder Ticlopidin imitieren diesen in vivo Effekt des NO, indem sie extrazellulär über eine Rezeptorhemmung Gi-Protein Stimulation verhindern. (uni-wuerzburg.de)
Lung1
- Aquaporin-1 water channel protein in lung: ontogeny, steroid-induced expression, and distribution in rat. (hopkinsmedicine.org)
Neuropathic Pain1
- binding to the central NMDA receptor may result in amelioration of neuropathic pain. (medindex.am)
Patients1
- Abnormal distribution of AQP5 water channel protein in salivary glands from Sjgrens syndrome patients. (hopkinsmedicine.org)
Assay1
- Nanoluciferase-based complementation assay to detect GPCR-G protein interaction. (uliege.be)
Membrane1
- They have been defined as monotropic integral membrane proteins located primarily in the endoplasmic reticulum (COX-1) and the perinuclear envelope (COX-2). (medscape.com)
Peptide1
- Anti-Prostaglandin E Receptor EP3 (PTGER3) Antibody, preincubated with Prostaglandin E Receptor EP3/PTGER3 Blocking Peptide (#BLP-PR065). (alomone.com)
Motifs1
- Superconserved receptors expressed in the brain: Expression, function, motifs and evolution of an orphan receptor family. (uliege.be)
Activation2
- This is achieved by activating the thromboxane receptor, which results in platelet-shape change, inside-out activation of integrins, and degranulation. (wikipedia.org)
- Background As carcinoma progresses, the stroma undergoes a variety of phenotypic changes, including the presence of carcinoma-associated fibroblasts (CAFs) that express fibroblast activation protein (FAP). (hoot4owls.org)