P2X7AntagonistsP2Y1CytokineMICROGLIAMetabotropicSubtypePreferentially activated by adenosineP2Y12P2Y2AgonistP2X3SubtypesPurinoceptorFamily of G-protein cExtracellularPathwaysProtein-coupledModulateIonotropicRegulationPurinoceptorsLigandPerfusionModulatesPlateletDistinctNeuronsNeurotransmitterStimuliP2Y11ActivateTargetsMuscarinicVIVOInhibitionExpressionNicotinicMediateMRNAWidely distributedFunctionalLipoproteinRole
P2X74
- Recent research has identified a role for microglial P2X receptors in neuropathic pain and inflammatory pain, especially the P2X4 and P2X7 receptors. (wikipedia.org)
- Here we studied whether p2rx7, encoding the P2X7 receptor (P2X7R), is a candidate gene for the differential susceptibility to vascular dysfunction under high angiotensin II tone. (ed.ac.uk)
- ATP-induced activation of ionotropic P2X4 and P2X7 receptors differentially induces receptor-operated Ca(2+) entry (ROCE). (uea.ac.uk)
- Webborn, P Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists. (bindingdb.org)
Antagonists3
- Data obtained from using P2 receptor-selective antagonists has produced evidence supporting ATP's ability to initiate and maintain chronic pain states after exposure to noxious stimuli. (wikipedia.org)
- While some P2 receptor-selective compounds have proven useful in preclinical trials, more research is required to understand the potential viability of P2 receptor antagonists for pain. (wikipedia.org)
- Incubation of blood with ATP in the presence of selective P2 receptor antagonists showed that the stimulatory effect of ATP on IL-10 release was completely annihilated by both 2-MeSAMP (a P2Y(12/13) receptor antagonist) and PSB-0413 (a P2Y(12) receptor antagonist). (maastrichtuniversity.nl)
P2Y11
- There are eight mammalian P2Y receptors known to date ( P2Y1 , P2Y2 , P2Y4 , P2Y6 , P2Y11 , P2Y12 , P2Y13 and P2Y14 ) and they are found in most human tissues. (atlasgeneticsoncology.org)
Cytokine2
- Inoue, K 2006, ' The function of microglia through purinergic receptors: Neuropathic pain and cytokine release ', Pharmacology and Therapeutics , vol. 109, no. 1-2, pp. 210-226. (elsevierpure.com)
- In particular we are studying the role of eicosanoids in normal pregnancy and preeclampsia, the contribution of a purinergic receptor to the release of the cytokine interleukin-1beta in pregnancy as well as investigation of the inflammasome in coordinating inflammatory pathways coupled to cytokine release. (nottingham.ac.uk)
MICROGLIA8
- P2X4 receptors found on MICROGLIA cells may also play a role in the mediation of allodynia -related NEUROPATHIC PAIN . (online-medical-dictionary.org)
- Recently, a great deal of attention is focusing on the relation between activated microglia through adenosine 5′-triphosphate (ATP) receptors and neuropathic pain. (elsevierpure.com)
- The expression of P2X4 receptor, a subtype of ATP receptors, is enhanced in spinal microglia after peripheral nerve injury model, and blocking pharmacologically and suppressing molecularly P2X4 receptors produce a reduction of the neuropathic pain. (elsevierpure.com)
- Thus, diffusible factors released from activated microglia by the stimulation of purinergic receptors may have an important role in the development of neuropathic pain. (elsevierpure.com)
- Understanding the key roles of ATP receptors, including P2X4 receptors, in the microglia may lead to new strategies for the management of neuropathic pain. (elsevierpure.com)
- Extracellular purines can elicit Ca(2+)-mediated microglia activation involving P2X/P2Y receptors with metabotropic (P2Y) and ionotropic (P2X) cell signaling in target cells. (uea.ac.uk)
- Diurnal enhancement of pain hypersensitivity is mediated by glucocorticoid-induced enhancement of the extracellular release of ATP in the spinal cord, which stimulates purinergic receptors on microglia in the dorsal horn. (nature.com)
- Temporal elevations in glucocorticoid levels enhance the extracellular release of ATP in the spinal cord, which stimulates purinergic receptors on microglia in the dorsal horn. (nature.com)
Metabotropic4
- To distinguish P2 receptors further, the subclasses have been divided into families of metabotropic (P2Y, P2U, and P2T) and ionotropic receptors (P2X and P2Z). (wikipedia.org)
- Both of these metabotropic receptors are distinguished by their reactivity to specific activators. (wikipedia.org)
- These plasma membraneClocalized receptors belong to a bigger family members that can end up being categorized into ionotropic G2A receptor and metabotropic G2Y receptors (Burnstock and Ralevic, 1998). (abt-888.net)
- Metabotropic receptors are combined to intracellular signaling paths through heterotrimeric G protein (Abbracchio et al. (abt-888.net)
Subtype1
- A widely distributed purinergic P2X receptor subtype that plays a role in pain sensation . (online-medical-dictionary.org)
Preferentially activated by adenosine2
- P1 receptors are preferentially activated by adenosine and P2Y receptors are preferentially more activated by ATP. (wikipedia.org)
- The protein encoded by P2RY8 gene is composed of 359-amino acids and belongs to the P2Y family of G-protein coupled receptors that are preferentially activated by adenosine and uridine nucleotides. (atlasgeneticsoncology.org)
P2Y121
- All of these are antiplatelet agents that block P2Y12 receptors. (wikipedia.org)
P2Y22
- P2Y2 purinergic receptor modulates virus yield, calcium homeostasis, and cell motility in human cytomegalovirus-infected cells. (princeton.edu)
- Our study reveals that levels of several components of the purinergic signaling system, including the P2Y2 and P2X5 receptors, are elevated in HCMV-infected fibroblasts. (princeton.edu)
Agonist2
- It was found that with treatment of the purinergic ligand 2-methylthioladenosine 5' diphosphate (2-MeSADP), which is an agonist and has a high preference for the purinergic receptor type 1 isoform (P2Y1R), significantly contributes to the reduction of an ischemic lesions caused by cytotoxic edema. (wikipedia.org)
- A P₂-purinergic receptor agonist that acts as a potent insulin secretagogue. (merckmillipore.com)
P2X35
- This produces a depolarization that may allow CALMH1 channels to open and release ATP, which serves as a neurotransmitter to activate closely associated nerve afferents expressing P2X2, P2X3 receptors and adjacent type III cells expressing P2Y4 receptors. (genome.jp)
- With this research, we've validated P2X3 receptors as a novel drug target for the treatment of cardiovascular disease by demonstrating that blockade of these receptors with a selective antagonist controls carotid body activity," said Dr Angus Nightingale, a cardiology consultant who runs the specialist hypertensive clinic at the Bristol Heart Institute and is a co-author of the study. (sciencedaily.com)
- The question now is whether blocking these P2X3 receptors in humans will lower elevated blood pressure, and how we can best identify those patients with carotid body hyperactivity who are most likely to respond to treatment. (sciencedaily.com)
- The researchers collaborated to test whether MK-7624/AF-219, a highly selective and potent orally available P2X3 receptor antagonist, can stop this nervous activity from occurring, thereby lowering blood pressure. (sciencedaily.com)
- They discovered that the energy molecule ATP (adenosine triphosphate), a recognized common signaling nucleotide, was able to persistently activate the P2X3 receptor, and that this protein was upregulated by almost 5 fold in the carotid body in hypertension. (sciencedaily.com)
Subtypes3
- This recent knowledge of purinergic receptors' effects on chronic pain provide promise in discovering a drug that specifically targets individual P2 receptor subtypes. (wikipedia.org)
- This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. (nih.gov)
- This paper introduces the abnormal changes of sympathetic nerve in diabetes mellitus and summarizes the recently published studies on the role of several purinergic receptor subtypes in diabetic cardiac sympathetic nerve injury . (bvsalud.org)
Purinoceptor1
- This receptor is coupled to the stimulation of the phosphoinositide and adenylyl cyclase pathways and behaves as a selective purinoceptor. (nih.gov)
Family of G-protein c1
- The product of this gene belongs to the family of G-protein coupled receptors. (nih.gov)
Extracellular4
- The physiological modulator Zn2+ allosterically enhances ATP-induced inward cation currents in the P2X4 receptor by binding to cysteine 132 and cystine 149 residues on the extracellular domain of the P2X4 protein. (wikipedia.org)
- The P2Y(11) receptor of human M2 macrophages activates canonical and IL-1 receptor signaling to translate the extracellular danger signal ATP into anti-inflammatory and pro-angiogenic responses. (nih.gov)
- Extracellular adenosine triphosphate (ATP) can activate purinergic receptors of the plasma membrane and modulate multiple mobile functions. (abt-888.net)
- P1 receptors are adenosine receptors, whereas P2 receptors are activated by other extracellular purine and pyrimidine nucleotides such as ATP, ADP, UTP, UDP or UDP-glucose. (semmelweis.hu)
Pathways2
- Diabetic cardiac sympathetic nerve injury affects the expression of purinergic receptors , and activated purinergic receptors affect the phosphorylation of different signaling pathways and the regulation of inflammatory processes. (bvsalud.org)
- We demonstrate specific drug effects on purinergic Ca(2+) pathways and provide new pharmacological insights into Ca(2+) oscillations in BV2 cells. (uea.ac.uk)
Protein-coupled1
- P2X receptors are ligand-gated ion channels, whereas the P1 and P2Y receptors are G protein-coupled receptors. (wikipedia.org)
Modulate4
- Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior, [6] making α3β4 a promising target for the development of novel antiaddictive agents. (wikipedia.org)
- 2003). Upon account activation, these receptors, which are distributed throughout the body broadly, modulate an array of mobile features like plasma membrane layer permeabilization, Ca2+ inflow, and cell loss of life (Surprenant and North, 2009). (abt-888.net)
- 2009). In this scholarly study, we determined whether ATP and purinergic receptors may modulate HIV-1 an infection. (abt-888.net)
- This ability is thought to be mediated by locally released substances that modulate the effect of noradrenaline (NA) on the α-receptor. (researchgate.net)
Ionotropic2
- These ligand-gated ion channels are nonselective cation channels responsible for mediating excitatory postsynaptic responses, similar to nicotinic and ionotropic glutamate receptors. (wikipedia.org)
- 2006), whereas ionotropic G2A receptors are linked with skin pores that open up upon ATP holding, enabling Ca2+ inflow and T+ efflux (Ralevic and Burnstock, 1998). (abt-888.net)
Regulation3
- The purinergic P2X 7 receptor: regulation of uterine function in labour and preterm labour. (nottingham.ac.uk)
- [ 5 ] confirmed that inflammatory cytokines contribute to foam cell formation by modifying cholesterol-mediated LDL receptor regulation in mesangial cells. (medsci.org)
- Purpose ATP could play an important role in skeletal muscle blood flow regulation by inducing vasodilation via purinergic P2 receptors. (researchgate.net)
Purinoceptors1
- Purinergic receptors, also known as purinoceptors, are a family of plasma membrane molecules that are found in almost all mammalian tissues. (wikipedia.org)
Ligand2
- P2X receptors are distinct from the rest of the widely known ligand-gated ion channels, as the genetic encoding of these particular channels indicates the presence of only two transmembrane domains within the channels. (wikipedia.org)
- This study aimed to determine the effects of the CXC chemokine ligand 16 (CXCL16)/CXC chemokine receptor 6 (CXCR6) pathway on cholesterol accumulation in the radial arteries of end-stage renal disease (ESRD) patients with concomitant microinflammation and to further investigate the potential effects of the purinergic receptor P2X ligand-gated ion channel 7 (P2X7R). (medsci.org)
Perfusion1
- These data are consistent with the notion that purinergic receptors activated by scala tympani perfusion contain subunits of the P2X(2) variant. (edu.au)
Modulates1
- As purinergic signaling modulates dopaminergic and glutamatergic neurotransmission in the brain, the impaired function of this system might be involved in the development of schizophrenia. (semmelweis.hu)
Platelet2
- P2X receptors mediate a large variety of responses including fast transmission at central synapses, contraction of smooth muscle cells, platelet aggregation, macrophage activation, and apoptosis. (wikipedia.org)
- Can platelet purinergic receptors be targeted to safely treat non-thrombotic diseases? (wcp2023.org)
Distinct3
- There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. (wikipedia.org)
- Furthermore, we are interested in the functional analyses of distinct purinergic receptors using patch clamp electrophysiology. (semmelweis.hu)
- CXCL16, which was originally described as a scavenger receptor for phosphatidylserine and oxidized low-density lipoprotein (SR-PSOX), is one of the few scavenger receptors that has two distinct forms: membrane-bound and soluble. (medsci.org)
Neurons5
- These receptors are greatly distributed in neurons and glial cells throughout the central and peripheral nervous systems. (wikipedia.org)
- Moreover, these receptors have been implicated in integrating functional activity between neurons, glial, and vascular cells in the central nervous system, thereby mediating the effects of neural activity during development, neurodegeneration, inflammation, and cancer. (wikipedia.org)
- However, a third of sensory neurons do not express receptors for the neurotrophins. (jneurosci.org)
- Here we show that these neurons express the receptor components for glial-derived neurotrophic factor (GDNF) signaling (RET, GFRα-1, and GFRα-2). (jneurosci.org)
- The trk receptors in general are expressed in a nonoverlapping manner by sensory neurons in combination with the low-affinity neurotrophin receptor p75 ( Wright and Snider, 1995 ). (jneurosci.org)
Neurotransmitter1
- It is believed that ATP functions as a pronociceptive neurotransmitter, acting at specific P2X and P2Y receptors in a systemized manner, which ultimately (as a response to noxious stimuli) serve to initiate and sustain heightened states of neuronal excitability. (wikipedia.org)
Stimuli2
- The stimuli of purinergic receptors decrease the threshold of mechanical allodynia. (nature.com)
- In vertebrates, taste stimuli are detected by taste receptor cells (TRCs). (genome.jp)
P2Y111
- The purinergic receptor P2Y11 choreographs the polarization, mitochondrial metabolism, and migration of T lymphocytes. (nih.gov)
Activate2
- Receptor for ATP and UTP coupled to G-proteins that activate a phosphatidylinositol-calcium second messenger system. (vectorbiolabs.com)
- Bacteria can release endotoxins like lipopolysaccharide (LPS) or other pathogenicity factors such as lipopoteins/peptides (LP) from their cell envelope, even due to treatment with conventional antibiotics, being able to activate Toll-like receptors (TLRs) and induce a strong inflammatory response. (nature.com)
Targets1
- These studies suggest that purinergic receptors as novel drug targets are of great significance for the treatment of diabetic autonomic neuropathy . (bvsalud.org)
Muscarinic1
- Type II taste cells also secrete acetylcholine (ACh) that appears to stimulate muscarinic receptors, specifically M3, on the same or neighboring Type II cells. (genome.jp)
VIVO1
- The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries. (wikipedia.org)
Inhibition1
- A 438079 hydrochloride is a competitive P2X 7 receptor antagonist (pIC 50 = 6.9 for the inhibition of Ca 2+ influx in the human recombinant P2X 7 cell line). (tocris.com)
Expression1
- Our cancer studies have expanded to include oesophageal cancer with emphasis on oestrogen receptor expression and function in this malignancy. (nottingham.ac.uk)
Nicotinic2
- The alpha-3 beta-4 nicotinic receptor , also known as the α3β4 receptor and the ganglion-type nicotinic receptor , [1] is a type of nicotinic acetylcholine receptor , consisting of α3 and β4 subunits . (wikipedia.org)
- As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3) m (β4) n where m + n = 5]. (wikipedia.org)
Mediate1
- The term purinergic receptor was originally introduced to illustrate specific classes of membrane receptors that mediate relaxation of gut smooth muscle as a response to the release of ATP (P2 receptors) or adenosine (P1 receptors). (wikipedia.org)
MRNA1
- Our group is planning to examine the mRNA and protein expressions of purinergic receptors in the different stages of this maturation process by quantitative RT-PCR and immunocytochemistry, respectively. (semmelweis.hu)
Widely distributed1
- P1 and P2Y receptors are known to be widely distributed in the brain, heart, kidneys, and adipose tissue. (wikipedia.org)
Functional1
- also known as the thymic stromal lymphopoietin receptor), which together with IL7 receptor alpha forms a heterodimeric complex that acts at the functional receptor for thymic stromal lymphopoietin (reviewed in Roll and Reuther, 2010). (atlasgeneticsoncology.org)
Lipoprotein1
- The membrane-bound form of CXCL16 binds and internalizes oxidative low-density lipoprotein (oxLDL) and promotes adhesion of cells expressing its cognate receptor, CXCR6 [ 6 , 7 ] . (medsci.org)
Role4
- Purinergic receptors have been suggested to play a role in the treatment of cytotoxic edema and brain infarctions. (wikipedia.org)
- Role of purinergic receptors in cardiac sympathetic nerve injury in diabetes mellitus. (bvsalud.org)
- Purinergic receptors play a crucial role in this process. (bvsalud.org)
- This study investigated the role of P2 receptors in exercise hyperemia in miniature swine. (researchgate.net)