• In hypothalamic neurons, modulators such as neuropeptide Y (NPY) and adenosine depress glutamatergic transmission by either a pertussis toxin (PTx)-sensitive G-protein-coupled pathway or by inhibition of voltage-activated calcium channels (VACCs). (jneurosci.org)
  • Although the exact mechanism by which adenosine receptor activation relaxes vascular smooth muscle is not known, there is evidence to support both inhibition of the slow inward calcium current reducing calcium uptake, and activation of adenylate cyclase through A2 receptors in smooth muscle cells. (globalrph.com)
  • These inhibitory effects may be associated with its dual‑receptor inhibition on P2Y12 and TP receptors. (spandidos-publications.com)
  • However, the wake-promoting effects of modafinil, unlike those of amphetamine[Rx] , were not antagonized by the dopamine receptor antagonist haloperidol[Rx] in rats. (illnesshacker.com)
  • The anxiolytic drug buspirone, a serotonin receptor 1A agonist, also functions as a potent D3R antagonist. (bvsalud.org)
  • We have previously shown that hypertonic stress (HS) can suppress chemoattractant-induced neutrophil responses via cyclic adenosine monophosphate and enhance these responses through p38 mitogen-activated protein kinase (MAPK) activation. (escholarship.org)
  • Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
  • Keywords: Soluble adenylyl cyclase cAMP Microdomain Cancer Diagnostics 1 Introduction Cyclic adenosine monophosphate (cAMP) is one of the most ancient CDCL1 signaling molecules present from bacteria to man. (bioinf.org)
  • These data suggest that glutamate, acting at several metabotropic receptors expressed by astrocytes, could modulate glial activity evoked by neurotransmitters and thereby influence the ongoing modulation of neurons by astrocytes. (jneurosci.org)
  • Here, we report that HS dose-dependently releases adenosine 5'-triphosphate (ATP) from neutrophils and that extracellular ATP is rapidly converted to adenosine or activates p38 MAPK and enhances N-formyl-methionyl-lencyl-phenylalanine-induced superoxide formation. (escholarship.org)
  • Enhancing endogenous adenosine A2A receptor signaling induces slow-wave sleep without affecting body temperature and cardiovascular function. (harvard.edu)
  • CD39 limits P2X7 receptor inflammatory signaling and attenuates sepsis-induced liver injury. (harvard.edu)
  • MCs can secrete nociceptor sensitizing and activating agents, such as serotonin, prostaglandins, histamine, and proteolytic enzymes that can also activate the pain-mediating transient receptor potential vanilloid channels. (frontiersin.org)
  • 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)
  • Through this mechanism, the increased level of adenosine after sleep deprivation could affect the light sensitivity of the circadian clock. (adxs.org)
  • The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine[Rx] by binding to the dopamine[Rx] reuptake pump, and lead to an increase in extracellular dopamine. (illnesshacker.com)
  • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (harvard.edu)
  • Peptides corresponding to the new amino terminal end of the proteolyzed seven-transmembrane domain thrombin receptor [TR42-55, SFLLRNPNDKYEPF, also known as TRAP (thrombin receptor-activating peptide)], previously have been demonstrated to activate the receptor. (umassmed.edu)
  • The molecular underpinnings common to and connecting these disorders are not known, but may include shared genetic risk factors ( 1 , 8 ), regulation of brain cations ( 9 , 10 ), or common receptor signaling events that activate pain ( 11 ), inflammation ( 12 ), or oxidative ( 13 ) pathways. (frontiersin.org)
  • Extracellular stimuli that activate cell surface receptors modulate glucocorticoid actions via as yet unclear mechanisms. (rupress.org)
  • Although metabotropic glutamate receptor (mGluR) modulation has been studied extensively in neurons, it has not been investigated in astrocytes. (jneurosci.org)
  • Suprachiasmatic nucleus (SCN) and cortical astrocytes showed striking differences in sensitivity to glutamate and to mGluR agonists, even after several weeks in culture. (jneurosci.org)
  • BACKGROUND: Studies have been performed on human fresh, liquid-preserved, and cryopreserved platelets (PLTs) to assess PLT-adhesive surface receptors, PLT membrane procoagulant activity, PLT aggregation, and thromboxane production. (umassmed.edu)
  • STUDY DESIGN AND METHODS: In both human and baboon fresh and lyophilized PLTs, aggregation response and PLT production of thromboxane A2 were measured after stimulation, and PLT surface markers P-selectin, glycoprotein (GP) Ib, GPIIb-IIIa, and factor (F) V were measured before and after stimulation. (umassmed.edu)
  • Data from a radiolabeled ligand‑binding assay indicated that LGP exhibited apparent competing effects on thromboxane receptor (TP) and P2Y12 receptors. (spandidos-publications.com)
  • These data indicate that GLP-1R agonists down-regulate innate inflammatory responses to endotoxins or endogenous inflammatory mediators. (justia.com)
  • However, no studies have reported the effect of GLP-1R agonists on lung IL-33 expression or release, the effect of GLP-1R agonists on the innate allergic inflammatory response that is mediated by ILC2, or the effect of GLP-1R agonists on respiratory syncytial virus (RSV) infection. (justia.com)
  • This study demonstrated that the Receptor for Activated C-Kinase 1 (RACK1) is important in SC function. (sdbonline.org)
  • Here, we report that the guanine nucleotide-binding protein (G protein)-coupled receptor-activated WD-repeat Gβ interacts with the glucocorticoid receptor (GR), comigrates with it into the nucleus and suppresses GR-induced transactivation of the glucocorticoid-responsive genes. (rupress.org)
  • Part of this adenosine is discharged from the cell and binds to adenosine receptors of neighboring cells, which is supposed to compensate for the disturbed balance between energy consumption and energy supply. (adxs.org)
  • Induction of Mregs is strongly linked with the interaction of Fc receptors located on the surface of Mregs with Fc fragments of antibodies. (wikipedia.org)
  • Unlike the mGluR-kainate interaction, which required a pretreatment with an mGluR agonist and was insensitive to pertussis toxin (PTx), the mGluR modulation of 5HT actions was rapid and was blocked by PTx. (jneurosci.org)
  • Adenosine is a potent vasodilator in most vascular beds, except in renal afferent arterioles and hepatic veins where it produces vasoconstriction. (globalrph.com)
  • Most tmACs are principally controlled by G protein coupled receptors via direct activation by heterotrimeric G proteins either by direct connection between tmACs and the G s subunit or subunits [1]. (bioinf.org)
  • Thrombin cleaves its G-protein-linked seven-transmembrane domain receptor, thereby releasing a 41-aa peptide and generating a new amino terminus that acts as a tethered ligand for the receptor. (umassmed.edu)
  • In contrast, adenosine suppresses superoxide formation. (escholarship.org)
  • the A2 receptor antagonists 8-(p-sulfophenyl)theophylline, 3,7-dimethyl-1-(2-propynyl)xanthine, 1,3,7-trimethyl-8-(3-chlorostyryl)xanthine, and 3-propylxanthine, but not A1 and A3 receptor antagonists, decreased the suppressive effect of HS, indicating that HS suppresses neutrophils via A2 receptor activation. (escholarship.org)
  • Taking advantage of the diverse γδ TCR repertoire or other ligand-receptor interactions, γδ T cells can recognize a broad spectrum of tumor-associated antigens (TAAs) in a major histocompatibility complex (MHC)-independent manner, thereby activating downstream pleiotropic effects. (explorationpub.com)
  • We conclude that hypertonic stress regulates neutrophil function via a single molecule (ATP) and its metabolite (adenosine), using positive- and negative-feedback mechanisms through the activation of P2 and A2 receptors, respectively. (escholarship.org)
  • however, modafinil is inactive in other in vitro assay systems known to be responsive to á-adrenergic agonists, such as the rat vas deferens preparation. (illnesshacker.com)
  • Attenuation of adverse effects of noise induced hearing loss on adult neurogenesis and memory in rats by intervention with Adenosine A2A receptor agonist. (harvard.edu)
  • The second signal can be stimulation with cytokines or toll-like receptor ligands. (wikipedia.org)
  • DEC-205 (CD205), a member of the macrophage mannose receptor protein family, is the prototypic endocytic receptor of dendritic cells, whose ligands include phosphorothioated cytosine-guanosine (CpG) oligonucleotides, a motif often seen in bacterial or viral DNA. (uci.edu)
  • Adenosine is thought to exert its pharmacological effects through activation of purine receptors (cell-surface A1 and A2 adenosine receptors). (globalrph.com)
  • M2d are pro-angiogenic cells that secrete IL-10, TGF-β, and vascular endothelial growth factor and are induced by IL-6 and A2 adenosine receptor agonist (A2R). (wikipedia.org)
  • Adenosine may also lessen vascular tone by modulating sympathetic neurotransmission. (globalrph.com)
  • Normally, the transient nicotinic impact was absent since just muscarinic receptors had been activated. (californiaehealth.org)
  • The type III mGluR agonist l -2-amino-4-phosphonobutyrate consistently inhibited 5HT-evoked calcium rises, whereas in a smaller number of cells quisqualate and L-CCG-I showed both inhibitory and additive effects. (jneurosci.org)
  • Linkage and comparative mapping studies indicate that the transferred chromosome segment contains a number of candidate genes for hypertension, including genes encoding a brain dopamine receptor and a renal epithelial potassium channel. (jci.org)
  • Several studies report that GLP-1R agonists had anti-inflammatory effects in multiple disorders including T2D. (justia.com)
  • In addition, the GLP-1R agonist, exendin-4, reduced serum inflammatory cytokines during LPS-induced endotoxemia, liver inflammation, and aortic atherosclerosis in a rodent model. (justia.com)
  • The present disclosure relates to glucagon-like peptide-1 receptor (GLP-1R) agonists and methods of treating or preventing allergic inflammation and/or methods of treating or preventing respiratory syncytial virus (RSV) infection. (justia.com)
  • It has been shown that anti-TNF monoclonal antibodies interacting with Fcγ receptor of Mregs induce differentiation of Mregs through activation of STAT3 signaling pathway. (wikipedia.org)
  • MCs express receptors for both estrogen and progesterone that induce degranulation upon binding. (frontiersin.org)
  • A pharmacological and genetic blockade of the dopamine D3 receptor (D3R) has shown to be neuroprotective in models of Parkinson's disease (PD). (bvsalud.org)
  • Recent evidence has shown that in cases of generalized ischemia after hemorrhagic shock, the effectiveness of melatonin in improving liver function depends on the melatonin receptor (40). (ectrx.org)
  • γδ T cells express unique T cell receptor (TCR) γ and TCR δ chains, with structural and functional heterogeneity. (explorationpub.com)
  • Antagonists of P2 receptors counteracted the enhancing effects of ATP, suggesting that HS costimulates neutrophils by means of P2 receptor activation. (escholarship.org)
  • Modafinil has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors. (illnesshacker.com)
  • The process of ischemia and reperfusion is known to cause inducible nitric oxide synthase induction and activation, and there is evidence that interleukin (IL)-1β (46), IL-1 receptor (47), and IL-1 receptor along with nuclear factor-kappa beta (48) may have an important role in that induction. (ectrx.org)
  • The long-lasting program can result in the activation of a larger absolute quantities and a different ensemble of muscarinic receptors and may cause their desensitization/internalization inducing a different general change. (californiaehealth.org)
  • cAMP microdomains were first appreciated in the 1970s from the groups of Keely Hayes Brunton and others when they identified that different tmAC activating hormones (e.g. β-adrenergic receptor and prostaglandin E1 agonists) all led to cAMP elevation but each induced unique cellular events in cardiomyocytes e.g. only β-adrenergic activation induced improved contractility and glycogen rate of metabolism [12]. (bioinf.org)
  • Mregs do not contribute to the production of extracellular matrix because they express low levels of arginase. (wikipedia.org)
  • Extracellular Adenosine Stimulates Vacuolar ATPase-Dependent Proton Secretion in Medullary Intercalated Cells. (harvard.edu)
  • The inventors found that GLP-1R agonists inhibited IL-33 expression and release from the lungs of mice in response to an airway challenge the allergen extract of the aeroallergen Alternaria alternata , an aeroallergen which has protease activity and which is associated with severe asthma exacerbations. (justia.com)
  • Receptor-mediated tobacco toxicity: alterations of the NF-kappaB expression and activity downstream of alpha7 nicotinic receptor in oral keratinocytes. (famri.org)
  • In this study, we demonstrate that the 41-aa cleaved peptide, TR1-41 (MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPR) is a strong platelet agonist. (umassmed.edu)
  • GLP-1 receptor (GLP-1R) agonists, such as liraglutide and exenatide are approved by the Food and Drug Administration (FDA) for treatment of type 2 diabetes (T2D). (justia.com)
  • For instance, GLP-1R agonist administration decreased TNFα and IL-6 production by peripheral blood mononuclear cells (PBMC) of obese patients with T2D and diabetic mouse adipose tissue. (justia.com)