Human thromboxane A2 recepInhibitionAgonistsPotentSelectiveProstaglandin D2 recepSynthasePlateletsU46619LigandAntagonismP2Y12Adenylyl cyclaseRecognized signal transductionPulmonaryProstacyclinSynthesisProstanoidMimeticCyclooxygenaseTXA2AggregationPGE2CharacterizationProstaglandinsProtein-coupled receptorMediatorsIntracellularLigandsConstitutiveIndomethacinAspirinLipidProteinsSubtypeBindsGPCRsVascularArachidonicKidneyC57BLExpressionCoronary
Human thromboxane A2 recep1
- Arg60 to Leu mutation of the human thromboxane A2 receptor in a dominantly inherited bleeding disorder. (jci.org)
Inhibition7
- These inhibitory effects may be associated with its dual‑receptor inhibition on P2Y12 and TP receptors. (spandidos-publications.com)
- Thienopyridines are a group of drugs whose metabolites bind irreversibly to adenosine diphosphate (ADP) receptors on platelets (P2Y12 receptors), resulting in the inhibition of ADP-induced platelet activation and aggregation. (jabfm.org)
- On the other hand, although UCM871 and UCM924 reduced collagen-induced platelet aggregation and adhesion, inhibition of collagen-induced platelet aggregation by Ago was not mediated by melatonin receptors because it was not affected by luzindole. (bvsalud.org)
- Forskolin-induced VASP-phosphorylation was reduced in porcine coronary arteries exposed to UDP-glucose and MRS2690, consistent with P2Y14 receptor coupling to Gi/o proteins and inhibition of adenylyl cyclase activity. (nottingham.ac.uk)
- An opioid agonist/antagonist, nalbuphine stimulates kappa opioid receptor in the CNS, which causes inhibition of ascending pain pathways. (medscape.com)
- Codeine binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering perception and response to pain. (medscape.com)
- Effect of thromboxane A2 inhibition and antagonism on prostaglandin and leukotriene synthesis in glomerular immune injury. (mcw.edu)
Agonists6
- Furthermore, EP receptors have been subdivided into four groups, EP 1 , EP 2 , EP 3 and EP 4 , originally on the basis of their relative sensitivities to a range of selective agonists and antagonists, but subsequently, all have been cloned. (sigmaaldrich.com)
- The original basis for the classification was functional, and there are many agonists selective for the various prostanoid receptors. (sigmaaldrich.com)
- However, few agonists are truly selective for one type of receptor over all of the others, exceptions being BW245C at DP (DP 1 ) receptors, fluprostenol at FP receptors, and cicaprost at IP receptors. (sigmaaldrich.com)
- UDP-glucose, UDP-glucuronic acid UDP-N-acetylglucosamine (P2Y14 receptor agonists), elicited concentration-dependent contractions in the porcine coronary artery. (nottingham.ac.uk)
- Structure-activity relationships of agonists for the orphan G protein-coupled receptor GPR27. (uliege.be)
- R&D Systems offers antibodies for the receptors listed below, as well as agonists for the cannabinoid receptors. (rndsystems.com)
Potent7
- Ramatroban is an orally bioavailable, potent, dual antagonist of the thromboxane A 2 (TPr) and PGD 2 (DPr2) receptors. (researchsquare.com)
- EP 3 antagonists are just emerging, but there are still no well characterized potent selective antagonists at EP 2 , FP or IP receptors. (sigmaaldrich.com)
- b) Iloprost is a partial agonist at EP 1 receptors, but is a potent full agonist at IP receptors. (sigmaaldrich.com)
- f) AH23848 is also a potent TP receptor blocking drug. (sigmaaldrich.com)
- Potent thromboxane A2 (TP) inhibitor (IC50 = 16.4 nM). (chemspider.com)
- U46619 is a potent, and stable thromboxane A2 (TP) receptor agonist. (guidetopharmacology.org)
- A synthetic opioid analgesic that is primarily a mu receptor agonist, fentanyl is 50-100 times more potent than morphine. (medscape.com)
Selective4
- Ramatroban and vidupiprant are non-selective (i.e. known to influence other receptors) antagonists of DP2. (wikipedia.org)
- in vivo: Terutroban is a selective antagonist of the thromboxane/prostaglandin endoperoxide receptor, in preventing retinal ischaemia in a model of diabetes in rats. (chemspider.com)
- 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)
- In this study we sought to investigate whether P2Y14 receptors are functionally expressed in the porcine coronary artery using a selective P2Y14 receptor agonist, MRS2690, and a novel selective P2Y14 receptor antagonist, PPTN (4,7-disubstituted naphthoic acid derivative). (nottingham.ac.uk)
Prostaglandin D2 recep1
- Prostaglandin D2 receptor 2 (DP2 or CRTH2) is a human protein encoded by the PTGDR2 gene and GPR44. (wikipedia.org)
Synthase1
- Disorders of receptors and signal transduction: platelet cyclo-oxygenase deficiency, thromboxane synthase deficiency, thromboxane A2 receptor defect, ADP receptor defect. (calcuttayellowpages.com)
Platelets6
- 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)
- The irreversible binding to the receptors makes these drugs capable of inhibiting platelet function for the life span of platelets (5-7 days). (jabfm.org)
- These drugs, unlike thienopyridines, bind reversibly, but directly without biotransformation, to P2Y12 receptors on platelets and hence inhibit platelet function. (jabfm.org)
- Thienopyridines are converted to active metabolites ( Figure 1 ) that bind irreversibly to P2Y12 receptors on platelets and thereby inhibit ADP-induced platelet activation and aggregation. (jabfm.org)
- In the present study we investigated whether agomelatine (Ago), an antidepressant with agonist activity at melatonin receptor 1 (MT1) and MT2 could reduce platelets aggregation and adhesion. (bvsalud.org)
- ADP, thromboxane A2, and other mediators induce activation and aggregation of additional platelets on the injured endothelium. (msdmanuals.com)
U466192
- Concentration dependent contractile responses to MRS2690 and UDP-sugars were enhanced in the presence of forskolin (activator of cAMP), where the level of basal tone was maintained by addition of U46619, a thromboxane A2 mimetic. (nottingham.ac.uk)
- Platelet-rich plasma (PRP) or isolated cells prepared from the blood of healthy, adult humans were treated with bedaquiline (0.625-10 μg/ml), followed by activation with adenosine 5'-diphosphate (ADP), thrombin or the thromboxane A2 receptor agonist (U46619). (up.ac.za)
Ligand5
- The mutant receptor expressed in Chinese hamster ovary cells showed decreased agonist-induced second messenger formation despite its normal ligand binding affinities. (jci.org)
- Data from a radiolabeled ligand‑binding assay indicated that LGP exhibited apparent competing effects on thromboxane receptor (TP) and P2Y12 receptors. (spandidos-publications.com)
- G protein-coupled receptors (GPCRs) such as DP2 are integral membrane proteins that, when bound by their cognate ligands (or, in some cases, even when not ligand-bound and thereby acting continuously in a constitutive manner {see Receptor (biochemistry)#Constitutive activity}), mobilize one or more types of Heterotrimeric G proteins. (wikipedia.org)
- In all cases, the splicing occurs in the intracellular C-terminal region, and while there is no evidence that it affects ligand affinities, it does appear to influence the receptors' coupling to particular signal transduction processes. (sigmaaldrich.com)
- Changes in glomerular thromboxane A2 receptor expression and ligand binding following immune injury. (mcw.edu)
Antagonism1
- Gamma-butyrolactone antagonism of the picrotoxin receptor: comparison of a pure antagonist and a mixed antagonist/inverse agonist. (aspetjournals.org)
P2Y121
- Platelet receptors for ADP include the P2Y12 receptor, which sends signals to suppress adenylate cyclase, decreases cyclic adenosine monophosphate (cAMP) levels, and promotes activation of the glycoprotein IIb/IIIa receptor (assembled on the activated platelet surface membrane from glycoproteins IIb and IIIa). (msdmanuals.com)
Adenylyl cyclase3
- DP 1 , EP 2 , EP 4 and IP receptors couple positively to adenylyl cyclase through binding to a G q/11 protein. (sigmaaldrich.com)
- EP 3 receptors can either couple negatively to adenylyl cyclase through binding to a G i protein, or like EP 1 , FP and TP receptors, via G q/11 binding to inositol phospholipid hydrolysis and calcium mobilization. (sigmaaldrich.com)
- Regulation of responsiveness at D2 dopamine receptors by receptor desensitization and adenylyl cyclase sensitization. (aspetjournals.org)
Recognized signal transduction1
- The splice variant of the EP 1 receptor is distinct, in that the splice region incorporates the sixth and seventh intracellular domains, and the resulting receptor does not appear to couple directly to any recognized signal transduction process. (sigmaaldrich.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)
Prostacyclin1
- 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)
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)
- It inhibits prostaglandin synthesis, which prevents the formation of platelet-aggregating thromboxane A2. (medscape.com)
Prostanoid7
- DP2 has little or no such amino acid sequence relationship to the eight other Prostanoid receptors (see Eicosanoid receptor#Prostenoid receptors). (wikipedia.org)
- DP2 is classified as a "contractile" prostanoid receptor in that it can cause the contraction of smooth muscle. (wikipedia.org)
- These receptors are termed P receptors, with a preceding letter indicating the natural prostanoid to which each receptor is most sensitive - i.e. (sigmaaldrich.com)
- Interestingly, this receptor is unrelated to the other prostanoid receptors, being more similar to the FPR and BLT chemotactic receptors. (sigmaaldrich.com)
- In addition, it has been suggested that certain prostaglandins ethanolamides (prostamides) also act at receptors distinct from the 'classical' prostanoid receptors, but definitive evidence is still awaited. (sigmaaldrich.com)
- IP receptors appear to be most unusual among the prostanoid receptors, and indeed among G protein-coupled receptors in general, in that the receptor protein requires isoprenylation in order to optimize agonist-induced activation. (sigmaaldrich.com)
- Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line. (bindingdb.org)
Mimetic1
- Characterization of a thromboxane A2/prostaglandin H2 receptor in guinea pig lung membranes using a radioiodinated thromboxane mimetic. (aspetjournals.org)
Cyclooxygenase1
- 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)
TXA24
- Thromboxane A2 (TXA2) receptor is a member of the family of G protein-coupled receptors and performs an essential role in hemostasis by interacting with TXA2 to induce platelet aggregation. (jci.org)
- Leu) in the first cytoplasmic loop of the TXA2 receptor in a dominantly inherited bleeding disorder characterized by defective platelet response to TXA2. (jci.org)
- Moreover, dominant inheritance of the disorder suggests the possibility that the mutation produces a dominant negative TXA2 receptor. (jci.org)
- BACKGROUND: 11-Dehydro-thromboxane B2 (11-dehydro-TXB2) is the final stable metabolite of thromboxane A2 (TXA2) and is involved in thrombus formation. (bvsalud.org)
Aggregation1
- We performed aggregation and adhesion assays, thromboxane B2 (TxB2), cAMP and cGMP measurements, intra-platelet calcium registration and flow cytometry assays. (bvsalud.org)
PGE21
- PGF2alpha=PGE2>PGI2=thromboxane A2. (wikipedia.org)
Characterization1
- Characterization of polyclonal antibodies to the Ah receptor prepared by immunization with a synthetic peptide hapten. (aspetjournals.org)
Prostaglandins2
- It is a member of the class of prostaglandin receptors which bind with and respond to various prostaglandins. (wikipedia.org)
- Prostanoids comprise prostaglandins (PGs) and thromboxanes (Txs). (sigmaaldrich.com)
Protein-coupled receptor3
- It consists of two introns and three exons and codes for a G protein coupled receptor (GPCR) composed of 472 amino acids. (wikipedia.org)
- Concurrently with the mobilization of these pathways, activated DP2 also mobilizes G protein-coupled receptor kinases (GRKs, GRK2, GRK3, and/or GRK6) and Arrestin-2 (also termed Arrestin beta 1 or β-arrestin). (wikipedia.org)
- In S. Martins & D. Prazeres, G Protein-Coupled Receptor Screening Assays - Methods in Molecular Biology (pp. 149-157). (uliege.be)
Mediators1
- This group of G protein-coupled receptors share lipid mediators as ligands. (rndsystems.com)
Intracellular1
- Ago also reduced AA-induced increase in thromboxane B2 (TxB2) production, intracellular calcium levels and P-selectin expression at plasma membrane. (bvsalud.org)
Ligands1
- Activation of DP2 by PGD2 or other cognate receptor ligands has been associated with certain physiological and pathological responses, particularly those associated with allergy and inflammation, in animal models and certain human diseases. (wikipedia.org)
Constitutive1
- Among them, mutations in G protein-coupled receptors have clearly demonstrated two types of abnormalities, namely loss of function and constitutive activation of the receptors. (jci.org)
Indomethacin1
- Indomethacin acts as an agonist at this receptor, and the TP antagonist, ramatroban, has antagonist activity. (sigmaaldrich.com)
Aspirin1
- Aspirin, which exerts its antiplatelet effects by inhibiting thromboxane A2 production, has been the mainstay of antiplatelet therapy in patients with ACS. (jabfm.org)
Lipid1
- Sandhu, H, Xu, C-B & Edvinsson, L 2009, ' DMSO-Lipid Soluble Cigarette Smoking Particles Upregulate Contractile Endothelin Type B And Thromboxane A2 Receptors Of Rat Middle Cerebral Arteries ', Hypertension , vol. 54, no. 5, pp. 1175-1176. (lu.se)
Proteins1
- The GRKs, along with the DAG-activated PKCs, phosphorylate DP2 to promote its internalization while arrestin-2 inhibits DP2 from further activating heterotrimeric G proteins while also linking DP2 to elements, clathrin and clathrin adaptor AP2, of the receptor internalization machinery. (wikipedia.org)
Subtype1
- Evidence for a second subtype of DP receptor has been published, found in T-lymphocytes, and originally termed CRTH 2 . (sigmaaldrich.com)
Binds1
- VWF binds to receptors on the platelet surface membrane (glycoprotein Ib/IX). (msdmanuals.com)
GPCRs1
- DP2, is related to members of the chemotactic factor class of GPCRs, sharing an amino acid sequence identity of 29% with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. (wikipedia.org)
Vascular2
- Thromboxane A 2 also increases vascular permeability, contracts bronchial smooth muscle, triggers and amplifies platelet activation, and promotes a prothrombotic state. (researchsquare.com)
- SIP receptors are regulators of developmental vascular integrity, anaphylaxis and leukocyte egress from lymphoid organs. (rndsystems.com)
Arachidonic1
- Isoprostanes, prostanoids synthesized through non-enzymatic conversion of arachidonic acid have been suggested to act at their own receptors, distinct from those for other prostanoids, but the evidence is ambiguous, and the case not proven. (sigmaaldrich.com)
Kidney1
- Localization of authentic thromboxane A2/prostaglandin H2 receptor in the rat kidney. (mcw.edu)
C57BL1
- Purification and N-terminal amino acid sequence of the Ah receptor from the C57BL/6J mouse. (aspetjournals.org)
Expression1
- Superconserved receptors expressed in the brain: Expression, function, motifs and evolution of an orphan receptor family. (uliege.be)
Coronary1
- Our data support a role of UDP-sugars as extracellular signalling molecules and show for the first time that they mediate contraction of porcine coronary arteries via P2Y14 receptors. (nottingham.ac.uk)