A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.
A purinergic P2X neurotransmitter receptor that plays a role in pain sensation signaling and regulation of inflammatory processes.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.
A subclass of purinergic P2 receptors that signal by means of a ligand-gated ion channel. They are comprised of three P2X subunits which can be identical (homotrimeric form) or dissimilar (heterotrimeric form).
A purinergic P2X neurotransmitter receptor involved in sensory signaling of TASTE PERCEPTION, chemoreception, visceral distension, and NEUROPATHIC PAIN. The receptor comprises three P2X3 subunits. The P2X3 subunits are also associated with P2X2 RECEPTOR subunits in a heterotrimeric receptor variant.
A subclass of purinergic P2Y receptors that have a preference for ATP and UTP. The activated P2Y2 receptor acts through a G-PROTEIN-coupled PHOSPHATIDYLINOSITOL and intracellular CALCIUM SIGNALING pathway.
A widely distributed purinergic P2X receptor subtype that plays a role in pain sensation. P2X4 receptors found on MICROGLIA cells may also play a role in the mediation of allodynia-related NEUROPATHIC PAIN.
A subclass of purinergic P2Y receptors that have a preference for ATP and ADP. The activated P2Y1 receptor signals through the G-PROTEIN-coupled activation of PHOSPHOLIPASE C and mobilization of intracellular CALCIUM.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.
Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.
A subclass of purinergic P2 receptors whose signaling is coupled through a G-PROTEIN signaling mechanism.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
A purinergic P2X neurotransmitter receptor involved in sensory signaling of TASTE PERCEPTION, chemoreception, visceral distension and NEUROPATHIC PAIN. The receptor comprises three P2X2 subunits. The P2X2 subunits also have been found associated with P2X3 RECEPTOR subunits in a heterotrimeric receptor variant.
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
Compounds that bind to and activate PURINERGIC RECEPTORS.
An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.
A subclass of purinergic P2Y receptors that have a preference for ADP binding and are coupled to GTP-BINDING PROTEIN ALPHA SUBUNIT, GI. The P2Y12 purinergic receptors are found in PLATELETS where they play an important role regulating PLATELET ACTIVATION.
A purinergic P2X neurotransmitter receptor found at high levels in the BRAIN and IMMUNE SYSTEM.
A purinergic P2X neurotransmitter receptor found at sympathetically innervated SMOOTH MUSCLE. It may play a functional role regulating the juxtoglomerular apparatus of the KIDNEY.
Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.
A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).
Compounds that bind to and block the stimulation of PURINERGIC P2Y RECEPTORS. Included under this heading are antagonists for specific P2Y receptor subtypes.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Signal transduction mechanisms whereby calcium mobilization (from outside the cell or from intracellular storage pools) to the cytoplasm is triggered by external stimuli. Calcium signals are often seen to propagate as waves, oscillations, spikes, sparks, or puffs. The calcium acts as an intracellular messenger by activating calcium-responsive proteins.
A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).
Compounds that act on PURINERGIC RECEPTORS or influence the synthesis, storage, uptake, metabolism, or release of purinergic transmitters.
A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.
Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
Established cell cultures that have the potential to propagate indefinitely.
A musculomembranous sac along the URINARY TRACT. URINE flows from the KIDNEYS into the bladder via the ureters (URETER), and is held there until URINATION.
Use of electric potential or currents to elicit biological responses.
The excretory duct of the testes that carries SPERMATOZOA. It rises from the SCROTUM and joins the SEMINAL VESICLES to form the ejaculatory duct.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
A uracil nucleotide containing a pyrophosphate group esterified to C5 of the sugar moiety.
An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.
A glycoprotein enzyme present in various organs and in many cells. The enzyme catalyzes the hydrolysis of a 5'-ribonucleotide to a ribonucleoside and orthophosphate in the presence of water. It is cation-dependent and exists in a membrane-bound and soluble form. EC 3.1.3.5.
A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.
Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.
A subclass of phospholipases that hydrolyze the phosphoester bond found in the third position of GLYCEROPHOSPHOLIPIDS. Although the singular term phospholipase C specifically refers to an enzyme that catalyzes the hydrolysis of PHOSPHATIDYLCHOLINE (EC 3.1.4.3), it is commonly used in the literature to refer to broad variety of enzymes that specifically catalyze the hydrolysis of PHOSPHATIDYLINOSITOLS.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
The monomeric units from which DNA or RNA polymers are constructed. They consist of a purine or pyrimidine base, a pentose sugar, and a phosphate group. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
Solutions that have a lesser osmotic pressure than a reference solution such as blood, plasma, or interstitial fluid.
Compounds that contain the triphenylmethane aniline structure found in rosaniline. Many of them have a characteristic magenta color and are used as COLORING AGENTS.
Interstitial space between cells, occupied by INTERSTITIAL FLUID as well as amorphous and fibrous substances. For organisms with a CELL WALL, the extracellular space includes everything outside of the CELL MEMBRANE including the PERIPLASM and the cell wall.
A group of homologous proteins which form the intermembrane channels of GAP JUNCTIONS. The connexins are the products of an identified gene family which has both highly conserved and highly divergent regions. The variety contributes to the wide range of functional properties of gap junctions.

Expression of both P1 and P2 purine receptor genes by human articular chondrocytes and profile of ligand-mediated prostaglandin E2 release. (1/1179)

OBJECTIVE: To assess the expression and function of purine receptors in articular chondrocytes. METHODS: Reverse transcriptase-polymerase chain reaction (RT-PCR) was used to screen human chondrocyte RNA for expression of P1 and P2 purine receptor subtypes. Purine-stimulated prostaglandin E2 (PGE2) release from chondrocytes, untreated or treated with recombinant human interleukin-1alpha (rHuIL-1alpha), was assessed by radioimmunoassay. RESULTS: RT-PCR demonstrated that human articular chondrocytes transcribe messenger RNA for the P1 receptor subtypes A2a and A2b and the P2 receptor subtype P2Y2, but not for the P1 receptor subtypes A1 and A3. The P1 receptor agonists adenosine and 5'-N-ethylcarboxamidoadenosine did not change PGE2 release from chondrocytes. The P2Y2 agonists ATP and UTP stimulated a small release of PGE2 that was potentiated after pretreatment with rHuIL-1alpha. PGE2 release in response to ATP and UTP cotreatment was not additive, but release in response to coaddition of ATP and bradykinin (BK) or UTP and BK was additive, consistent with ATP and UTP competition for the same receptor site. The potentiation of PGE2 release in response to ATP and UTP after rHuIL-1alpha pretreatment was mimicked by phorbol myristate acetate. CONCLUSION: Human chondrocytes express both P1 and P2 purine receptor subtypes. The function of the P1 receptor subtype is not yet known, but stimulation of the P2Y2 receptor increases IL-1-mediated PGE2 release.  (+info)

A2B adenosine and P2Y2 receptors stimulate mitogen-activated protein kinase in human embryonic kidney-293 cells. cross-talk between cyclic AMP and protein kinase c pathways. (2/1179)

Mitogen-activated protein kinase (MAPK) cascades underlie long-term mitogenic, morphogenic, and secretory activities of purinergic receptors. In HEK-293 cells, N-ethylcarboxamidoadenosine (NECA) activates endogenous A2BARs that signal through Gs and Gq/11. UTP activates P2Y2 receptors and signals only through Gq/11. The MAPK isoforms, extracellular-signal regulated kinase 1/2 (ERK), are activated by NECA and UTP. H-89 blocks ERK activation by forskolin, but weakly affects the response to NECA or UTP. ERK activation by NECA or UTP is unaffected by a tyrosine kinase inhibitor (genistein), attenuated by a phospholipase C inhibitor (U73122), and is abolished by a MEK inhibitor (PD098059) or dominant negative Ras. Inhibition of protein kinase C (PKC) by GF 109203X failed to block ERK activation by NECA or UTP, however, another PKC inhibitor, Ro 31-8220, which unlike GF 109203X, can block the zeta-isoform, and prevents UTP- but not NECA-induced ERK activation. In the presence of forskolin, Ro 31-8220 loses its ability to block UTP-stimulated ERK activation. PKA has opposing effects on B-Raf and c-Raf-1, both of which are found in HEK-293 cells. The data are explained by a model in which ERK activity is modulated by differential effects of PKC zeta and PKA on Raf isoforms.  (+info)

A comparison of an A1 adenosine receptor agonist (CVT-510) with diltiazem for slowing of AV nodal conduction in guinea-pig. (3/1179)

1. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-510), and the prototypical calcium channel blocker diltiazem. 2. In the atrial-paced isolated heart, CVT-510 was approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval), a measure of slowing AV nodal conduction (EC50 = 41 nM) than to increase coronary conductance (EC50 = 200 nM). At concentrations of CVT-510 (40 nM) and diltiazem (1 microM) that caused equal prolongation of S-H interval (approximately 10 ms), diltiazem, but not CVT-510, significantly reduced left ventricular developed pressure (LVP) and markedly increased coronary conductance. CVT-510 shortened atrial (EC50 = 73 nM) but not the ventricular monophasic action potentials (MAP). 3. In atrial-paced anaesthetized guinea-pigs, intravenous infusions of CVT-510 and diltiazem caused nearly equal prolongations of P-R interval. However, diltiazem, but not CVT-510, significantly reduced mean arterial blood pressure. 4. Both CVT-510 and diltiazem prolonged S-H interval, i.e., slowed AV nodal conduction. However, the A1 receptor-selective agonist CVT-510 did so without causing the negative inotropic, vasodilator, and hypotensive effects associated with diltiazem. Because CVT-510 did not affect the ventricular action potential, it is unlikely that this agonist will have a proarrythmic action in ventricular myocardium.  (+info)

Purification of A1 adenosine receptor-G-protein complexes: effects of receptor down-regulation and phosphorylation on coupling. (4/1179)

We examined the effects of exposing A1 adenosine receptors (A1ARs) to an agonist on the stability and phosphorylation state of receptor-guanine nucleotide-binding regulatory protein (R-G-protein) complexes. Non-denatured recombinant human A1ARs extended on the N-terminus with hexahistidine (His6) and the FLAG (Asp-Tyr-Lys-Asp-Asp-Asp-Asp-Lys) epitope (H/F) were purified to near homogeneity from stably transfected Chinese-hamster ovary (CHO)-K1 cells. Purified receptors have pharmacological properties similar to receptors in membranes. G-proteins were co-purified with 15+/-2% of H/F-A1AR unless receptor-G-protein (R-G) complexes were uncoupled by pre-treating cell membranes with GTP. By silver staining, purified A1AR-G-protein complexes contain receptors, G-protein alpha and beta subunits and an unidentified 97 kDa protein. Pretreating intact cells with N6-cyclopentyladenosine (CPA) for 24 h decreased both the total number of receptors measured in membranes and the number of purified A1ARs by about 50%. In contrast, pretreating cells with CPA decreased the number of R-G complexes measured in membranes (54+/-6%) significantly less than it decreased the number of purified R-G complexes (78+/-3%) as detected by 125I-N6-(4-aminobenzyl)adenosine binding or by Western blotting Gialpha2. The effect of CPA to decrease the fraction of receptors purified as R-G complexes was not associated with any change in low-level A1AR phosphorylation (found on serine), or low-level phosphorylation of G-protein alpha or beta subunits or the 97 kDa protein. These experiments reveal a novel aspect of agonist-induced down-regulation, namely a diminished stability of receptor-G-protein complexes that is manifested as uncoupling during receptor purification.  (+info)

Patterns of A2A extracellular adenosine receptor expression in different functional subsets of human peripheral T cells. Flow cytometry studies with anti-A2A receptor monoclonal antibodies. (5/1179)

Signaling through A2A adenosine receptors (A2AR) regulates T lymphocyte expansion and modulates T cell receptor (TCR)-mediated effector functions in vitro. To understand the role of A2ARs in the regulation of immune response, we investigated the expression levels of this receptor in different functional lymphocyte subsets. Monoclonal anti-A2AR antibody was used to develop a flow cytometric assay to quantify the expression A2ARs on lymphocytes. We report that detectable levels of expression of A2ARs are much higher among T cells than B cells. More CD4(+) than CD8(+) T cells express A2ARs, but activation of T cells increases A2AR expression, predominantly in CD8(+) T cells. No significant differences were found in the proportion of A2AR+ cells between CD8(low) and CD8(high) T cells or between TCR/CD3(low) and TCR/CD3(high) T cells. Studies of T helper cell subsets (TH1 and TH2) reveal that lymphokine-producing cells are much more likely to express A2ARs than are cells that do not produce lymphokines. These results suggest that A2ARs are variably expressed on T cell subsets and may regulate cytokine production in activated T lymphocytes.  (+info)

Carbamazepine-induced upregulation of adenosine A1-receptors in astrocyte cultures affects coupling to the phosphoinositol signaling pathway. (6/1179)

The anticonvulsant and antibipolar drug carbamazepine (CBZ) is known to act as a specific antagonist at adenosine A1-receptors. After a 3-week application of CBZ, A1-receptors are upregulated in the rat brain. We have investigated the consequences of this upregulation for the A1-receptor-mediated signal transduction in primary astrocyte cultures from different regions of the rat brain. CBZ treatment for 10 days had no effect on adenosine A1-receptor mRNA expression in cultures with high basal A1-receptor mRNA levels, but increased A1-receptor mRNA in cultures exhibiting low basal A1-receptor mRNA levels. This upregulation of A1-receptor mRNA was accompanied by an upregulation or induction of A1-receptor-mediated potentiation of PLC activity, a property that was not found in these cultures before CBZ treatment. Thus, CBZ treatment for 10 days induces a new quality of adenosine A1-receptor-mediated signal transduction in cells that express low basal A1-receptor numbers.  (+info)

Adenosine inhibits the transfected Na+-H+ exchanger NHE3 in Xenopus laevis renal epithelial cells (A6/C1). (7/1179)

1. Adenosine influences the vectorial transport of Na+ and HCO3- across kidney epithelial cells. However, its action on effector proteins, such as the Na+-H+ exchanger NHE3, an epithelial brush border isoform of the Na+-H+ exchanger (NHE) gene family, is not yet defined. 2. The present study was conducted in Xenopus laevis distal nephron A6 epithelia which express both an apical adenosine receptor of the A1 type (coupled to protein kinase C (PKC)) and a basolateral receptor of the A2 type (coupled to protein kinase A (PKA)). The untransfected A6 cell line expresses a single NHE type (XNHE) which is restricted to the basolateral membrane and which is activated by PKA. 3. A6 cell lines were generated which express exogenous rat NHE3. Measurements of side-specific pHi recovery from acid loads in the presence of HOE694 (an inhibitor with differential potency towards individual NHE isoforms) detected an apical resistant Na+-H+ exchange only in transfected cell lines. The sensitivity of the basolateral NHE to HOE694 was unchanged, suggesting that exogenous NHE3 was restricted to the apical membrane. 4. Stimulation of the apical A1 receptor with N 6-cyclopentyladenosine (CPA) inhibited both apical NHE3 and basolateral XNHE. These effects were mimicked by the addition of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) and partially prevented by the PKC inhibitor calphostin C which also blocked the effect of PMA. 5. Stimulation of the basolateral A2 receptor with CPA inhibited apical NHE3 and stimulated basolateral XNHE. These effects were mimicked by 8-bromo-cAMP and partially prevented by the PKA inhibitor H89 which entirely blocked the effect of 8-bromo-cAMP. 6. In conclusion, CPA inhibits rat NHE3 expressed apically in A6 epithelia via both the apical PKC-coupled A1 and the basolateral PKA-coupled A2 adenosine receptors.  (+info)

A3 adenosine receptors regulate Cl- channels of nonpigmented ciliary epithelial cells. (8/1179)

Adenosine stimulates Cl- channels of the nonpigmented (NPE) cells of the ciliary epithelium. We sought to identify the specific adenosine receptors mediating this action. Cl- channel activity in immortalized human (HCE) NPE cells was determined by monitoring cell volume in isotonic suspensions with the cationic ionophore gramicidin present. The A3-selective agonist N6-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (IB-MECA) triggered shrinkage (apparent Kd = 55 +/- 10 nM). A3-selective antagonists blocked IB-MECA-triggered shrinkage, and A3-antagonists (MRS-1097, MRS-1191, and MRS-1523) also abolished shrinkage produced by 10 microM adenosine when all four known receptor subtypes are occupied. The A1-selective agonist N6-cyclopentyladenosine exerted a small effect at 100 nM but not at higher or lower concentrations. The A2A agonist CGS-21680 triggered shrinkage only at high concentration (3 microM), an effect blocked by MRS-1191. IB-MECA increased intracellular Ca2+ in HCE cells and also stimulated short-circuit current across rabbit ciliary epithelium. A3 message was detected in both HCE cells and rabbit ciliary processes using RT-PCR. We conclude that human HCE cells and rabbit ciliary processes possess A3 receptors and that adenosine can activate Cl- channels in NPE cells by stimulating these A3 receptors.  (+info)

The low-affinity A2B receptor is known to mediate proinflammatory effects of adenosine by up-regulating production of cytokines and growth factors. This view has been supported by a large body of evidence provided by pharmacological analysis of adenosine-dependent cytokine and growth factor secretion in various cells, tissues, and organs (8, 11, 13, 18, 31, 32, 33, 34, 35, 36, 37, 38). Pharmacological inhibition of A2B receptors significantly reduced elevations in proinflammatory cytokines as well as mediators of airway remodeling induced by high adenosine levels in the lungs of ADA-deficient mice (8). In the ragweed allergic mouse model, A2B antagonism plays an important role in inhibition of airway reactivity and inflammation (39, 40). In agreement with data obtained in these animal models of pulmonary inflammation, stimulation of A2B receptors in the human mast cell line HMC-1 was shown to induce secretion of proinflammatory Th2 cytokines IL-4 and IL-13 (11, 12), as well as angiogenic factors ...
TY - JOUR. T1 - The effect of development on the pattern of A1 and A2a-adenosine receptor gene and protein expression in rat peripheral arterial chemoreceptors.. AU - Gauda, Estelle B.. AU - Cooper, Reed Z.. AU - Donnelly, David F.. AU - Mason, Ariel. AU - McLemore, Gabrielle L.. PY - 2006. Y1 - 2006. UR - http://www.scopus.com/inward/record.url?scp=33745272264&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=33745272264&partnerID=8YFLogxK. M3 - Article. C2 - 16683708. VL - 580. JO - Advances in Experimental Medicine and Biology. JF - Advances in Experimental Medicine and Biology. SN - 0065-2598. ER - ...
In this report we show that it is possible to detect the expression of a G protein-coupled receptor, the A2AR, in human lymphocytes both on the basis of a functional assay (cAMP accumulation) and by flow cytometry using an antireceptor mAb. We were able to describe for the first time the distribution of A2AR among minor T cell subpopulations through the use of a combination of anti-A2AR mAb and mAbs that recognize T cell surface markers or cytokines. The principle findings of this study are that much higher levels of A2AR expression is found in T cells than in B cells (Fig. 3) and higher levels of cytokines are detected in activated T cells that express A2AR than in activated T cells that do not express these receptors (Figs. 6 and 7).. The detection of higher levels of cytokines among A2AR+ cells is surprising because A2AR-mediated signaling antagonizes the effects of T cell activation (Koshiba et al., 1997; Huang et al., 1997). Therefore, we expected that cytokine secretion would be the lowest ...
It brings a formula with active ingredients and many vitamins that help in improving metabolism and burning fat. It is possible to notice results of muscle gain already in the first weeks, since from the beginning of the use of the Alpha Prime Elite, it is noticeable the reshaping of the measures. The results, of course, depend on diet and training to be accentuated.. Through accelerated metabolism, the adenosine receptors are inhibited, providing a state of alertness and making us feel no tiredness and fatigue. This receptor is responsible for feeling sleepy and tired and acts on controlling blood pressure, heart rate and body temperature. When we are no longer with the feeling of bloating, excess abdominal fat and energy down, our brain tells us that we are well and when we see ourselves in front of a mirror with a more beautiful body we are happier and motivated. This implies even in your mood, because in the Alpha Prime Elite contains ingredients that help the body to feel lighter and giving ...
It brings a formula with active ingredients and many vitamins that help in improving metabolism and burning fat. It is possible to notice results of muscle gain already in the first weeks, since from the beginning of the use of the Alpha Prime Elite, it is noticeable the reshaping of the measures. The results, of course, depend on diet and training to be accentuated.. Through accelerated metabolism, the adenosine receptors are inhibited, providing a state of alertness and making us feel no tiredness and fatigue. This receptor is responsible for feeling sleepy and tired and acts on controlling blood pressure, heart rate and body temperature. When we are no longer with the feeling of bloating, excess abdominal fat and energy down, our brain tells us that we are well and when we see ourselves in front of a mirror with a more beautiful body we are happier and motivated. This implies even in your mood, because in the Alpha Prime Elite contains ingredients that help the body to feel lighter and giving ...
Our work demonstrates that human endothelial cells of disparate origin are characterized by differential expression of adenosine receptor subtypes. HUVECs express mRNA for A2A and A2B receptors at a ratio of 10:1, and this preferential gene expression agrees well with the typical pharmacological phenotype of A2A receptor-mediated simulation of adenylate cyclase by adenosine analogs. Using complementary techniques, RT-PCR, and gene expression array, we found that A1 and A3 adenosine receptors are not expressed in HUVECs. Previous studies in HUVECs have suggested a potential role of A1 receptor in maintaining endothelial barrier function4 and of A1 and A3 receptors in modulation of tissue factors expression.6 The apparent contradiction between these results and ours can be explained by the use of nonselective concentrations of adenosine receptor ligands in previous studies.. HMEC-1 also express only A2A and A2B mRNA, but in contrast to HUVECs, they express predominantly A2B receptor mRNA, with a ...
The review summarizes data evaluating the role of adenosine receptor signaling in murine hematopoietic functions. The studies carried out utilized either non-selective activation of adenosine receptors induced by elevation of extracellular adenosine or by administration of synthetic adenosine analogs having various proportions of selectivity for a particular receptor. Numerous studies have described stimulatory effects of non-selective activation of adenosine receptors, manifested as enhancement of proliferation of cells at various levels of the hematopoietic hierarchy. Subsequent experimental approaches, considering the hematopoiesis-modulating action of adenosine receptor agonists with a high level of selectivity to individual adenosine receptor subtypes, have revealed differential effects of various adenosine analogs. Whereas selective activation of A(1) receptors has resulted in suppression of proliferation of hematopoietic progenitor and precursor cells, that of A(3) receptors has led to ...
Corresponding Author: Anaclet Ngezahayo Department of Cell Physiology and Biophysics, Institute of Cell Biology and Biophysics, Leibniz University Hannover, Herrenhäuser Straße 2, Hannover, 30419 (Germany ...
In the current study, the combination of T62 and clonidine produced a synergistic interaction in rats with incisional pain. Synergy usually indicates that the two drugs have different final pathways to produce their effect, although other levels of interaction, such as altered drug disposition, can also be responsible. We did not measure tissue concentrations of drugs, so we cannot exclude a pharmacokinetic mechanism of synergy in the current study. Nonetheless, the observation of synergy is somewhat surprising if, as indicated by studies with spinal nerve ligation, the effect of T62 relies entirely on stimulating spinal norepinephrine release, which acts on α2adrenoceptors. One would in that case expect an additive interaction, and intrathecal adenosine and clonidine do interact additively in spinal-ligated rats. 14 In contrast, a synthetic adenosine agonist interacts synergistically with clonidine in acute thermal nociception tests in normal rats. 20 In addition, idazoxan only partially ...
Diamond I, Mochly-Rosen D, Gordon AS. In Alcohol and seizures: basic mechanisms and clinical concepts. Porter R, Mattson R, Kramer J and Diamond I (eds). FA Davis, Philadelphia, pp 79-86, (1990). ...
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Since their discovery approximately 25 years ago, adenosine receptors have now emerged as important novel molecular targets in disease and drug discovery. These proteins play important roles in the entire spectrum of disease from inflammation to immune suppression. Because of their expression on a number of different cell types and in a number of different organ systems they play important roles in specific diseases, including asthma, rheumatoid arthritis, Parkinsons disease, multiple sclerosis, Alzheimers disease, heart disease, stroke, cancer, sepsis, and obesity. As a result of intense investigations into understanding the molecular structures and pharmacology of these proteins, new molecules have been synthesized that have high specificity for these proteins and are now entering clinical trials. These molecules will define the next new classes of drugs for a number of diseases with unmet medical needs.
This is Digital Version of (Ebook) 978-9048131433 A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics Product Will Be Delivered
The IUPHAR/BPS Guide to Pharmacology. A1 receptor - Adenosine receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
The IUPHAR/BPS Guide to Pharmacology. A2B receptor - Adenosine receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
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What is the molecular mechanism by which lack of adenosine receptor signaling results in a pro-calcific phenotype, and are these pathways applicable to calcification seen in more common diseases ...
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DESCRIPTION: (Adapted from the Investigators Abstract): Adenosine administered as an aerosol to asthmatics causes bronchoconstriction, while in non-asthmatics adenosine causes bronchodilation. This occurs because the activation of A2B adenosine receptors on sensitized mast cells triggers degranulation, releasing histamine, leukotrienes, and other allergic mediators. A2B adenosine receptors are blocked by theophylline, a xanthine that is effective in treating asthma. However, theophylline is a non-selective antagonist of all four adenosine receptor subtypes and produces side effects due primarily to A1 receptor blockade, including insomnia and diuresis. The incidence of asthma is increasing and current treatment options are limited. New drugs that are potent and selective antagonists of A2B adenosine receptors have great potential for the treatment of asthma and other allergic diseases. Adenosine Therapeutics, LLC owns the first potent and selective A2B antagonists. The purpose of this phase I ...
TY - JOUR. T1 - Chronic exposure to adenosine receptor agonists and antagonists reciprocally regulates the A1 adenosine receptor-adenylyl cyclase system in cerebellar granule cells. AU - Hettinger-Smith, Barbara D.. AU - Leid, Mark. AU - Murray, Thomas F.. PY - 1996/11. Y1 - 1996/11. N2 - Chronic treatment with the adenosine receptor antagonist caffeine evokes an up-regulation of A1 adenosine receptors and increased coupling of the receptor to G proteins in rat brain membranes. However, chronic agonist exposure has not been explored. Primary cultures of cerebellar granule cells were exposed chronically to A1 adenosine receptor agonists and antagonists. Exposure to the A1 adenosine receptor agonist N6-cyclopentyladenosine resulted in (1) a time- and concentration-dependent reduction in the density of receptors labeled by 1,3[3H]dipropyl-8-cyclopentylxanthine, (2) an enhanced ability of guanyl nucleotides to decrease the fraction of A1 adenosine receptor sites displaying high affinity for ...
Several lines of evidence implicate the cholecystokinin B receptor (CCKBR) and the A2a adenosine receptor (A2aAR) in the etiology of panic disorder. To determine the roles each of these receptors...
We examined how the endogenous anticonvulsant adenosine might influence gamma-aminobutyric acid type A (GABA(A)) receptor stability and which adenosine receptors (ARs) were involved. Upon repetitive activation (GABA 500 microM), GABA(A) receptors, microtransplanted into Xenopus oocytes from neurosurgically resected epileptic human nervous tissues, exhibited an obvious GABA(A)-current (I(GABA)) run-down, which was consistently and significantly reduced by treatment with the nonselective adenosine receptor antagonist CGS15943 (100 nM) or with adenosine deaminase (ADA) (1 units/ml), that inactivates adenosine. It was also found that selective antagonists of A2B (MRS1706, 10 nM) or A3 (MRS1334, 30 nM) receptors reduced I(GABA) run-down, whereas treatment with the specific A1 receptor antagonist DPCPX (10 nM) was ineffective. The selective A2A receptor antagonist SCH58261 (10 nM) reduced or potentiated I(GABA) run-down in approximately 40% and approximately 20% of tested oocytes, respectively. The ...
Previous in vitro studies have shown biphasic effects of adenosine on mast cell activity; however, the receptor subtypes that mediate the inhibitory effects of adenosine are still controversial (Peachell et al., 1991; Yip et al., 2009). Mast cells express two distinct Gs-coupled adenosine receptors; their biologic roles have not been comprehensively defined, especially in vivo. Since activation of Gs-coupled adenosine receptors increases intracellular cAMP, we hypothesized that the inhibitory effects of adenosine on mast cells are mediated by the Gs-coupled adenosine receptors. In this study, we used both genetically modified animal models and mast cell cultures to comprehensively investigate the role of Gs-coupled adenosine receptors on mast cells both in vitro and in vivo. First, our data demonstrate a potent inhibitory effect of the nonhydrolyzable adenosine analog NECA on IgE-induced mast cell degranulation; this inhibitory effect of NECA was abolished by the genetic deletion of the A2B but ...
Adenosine receptors (AR) belong to the G-protein coupled receptor family. There are four receptor subtypes: A1, A2A, A2B e A3. Adenosine receptor subtypes show a different distribution in the organism and are implicated in several physiopathological processes. In particular, antagonists towards A1AR are promising in the treatment of cognitive disorders. A2A antagonists seem to be involved in decrease the neurological impairment observed in Parkinson’s disease. A2B antagonists are potential therapeutic agents in asthma and diabetes. Finally, antagonists at the A3AR could be implicated in tumor growth inhibition and in glaucoma treatment. The crystallographic structure acquisition of the human A2A receptor allowed the design of new AR antagonists by the help of computational techniques. Our group is focused on the synthesis of new adenosine receptor antagonists (particularly towards A2A and A3) for their potential therapeutic use, but also as tools for pharmacological investigations on ...
We performed experiments to test the hypothesis that endogenous adenosine acts as an essential cofactor required for eliciting angiotensin II (Ang II)-induced afferent and/or efferent arteriolar vasoconstriction. Enalaprilat (2 mg IV) was administered to anesthetized rats to reduce endogenous Ang II levels. Kidneys and blood were harvested from these animals and used for study of renal microvascular function using the in vitro blood-perfused juxtamedullary nephron technique. Arteriolar inside diameter was monitored videomicroscopically in (1) normal kidneys, (2) kidneys subjected to adenosine receptor blockade (100 mumol/L 1,3-dipropyl-8-p-sulfophenylxanthine), and (3) kidneys continuously exposed to 1 mumol/L adenosine. Under resting conditions, arteriolar diameters were similar in all three groups of kidneys, averaging 24.8 +/- 1.0 microns (n = 23) in afferent arterioles and 24.0 +/- 0.9 microns (n = 16) in efferent arterioles. In normal kidneys, adenosine (10 mumol/L) decreased both afferent ...
A concise synthesis of a series of N6-substituted adenosines with bicyclo[3.2.1]octan-6-yl and polycyclic N6-substituents has been developed. The adenosine A1 receptor (A1R) affinity and potency of these compounds was initially assessed using competitive binding assays and cyclic adenosine monophosphate (cAMP) accumulation assays in DDT1 MF-2 cells. The potency and receptor subtype selectivity of selected examples was further evaluated by measuring their effects on cAMP accumulation at all human adenosine receptor subtypes expressed in CHO cells. The results of these assays indicated that all of the synthesised N6-substituted adenosines are full agonists at A1R and activate this receptor selectively over the other adenosine receptor subtypes. The two standout compounds in terms of potency were N6-(3-thiabicyclo[3.2.1]octan-6-yl)adenosine and N6-(cubanylmethyl)adenosine with EC50 values at human A1R of 2.3 nM and 1.1 nM, respectively. The cubanylmethyl derivative in particular proved to be highly ...
Each type of adenosine receptor has different functions, although with some overlap.[3] For instance, both A1 receptors and A2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A2A receptor also has broader anti-inflammatory effects throughout the body.[4] These two receptors also have important roles in the brain,[5] regulating the release of other neurotransmitters such as dopamine and glutamate,[6][7][8] while the A2B and A3 receptors are located mainly peripherally and are involved in processes such as inflammation and immune responses. Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in hospitals as treatment for severe tachycardia (rapid heart beat),[9] and acting directly to slow the heart through action on all four adenosine receptors in heart tissue,[10] as well as producing a sedative effect through action on A1 and A2A receptors in the brain. Xanthine derivatives ...
Methylxanthines have been the mainstay of pharmacologic treatment of apnea for decades. Adverse effects include tachycardia, emesis, and jitteriness. Both theophylline and caffeine are used, but caffeine citrate is preferred because of its longer half-life, higher therapeutic index, and lack of need for drug-level monitoring. Xanthines have multiple effects on respiration, including increased minute ventilation, improved carbon dioxide sensitivity, decreased periodic breathing, and decreased hypoxic depression of breathing. Their primary mechanism of action is thought to be blockade of inhibitory adenosine A1 receptors, with resultant excitation of respiratory neural output, as well as blockade of excitatory adenosine A2A receptors located on γ-aminobutyric acidergic neurons. Specific polymorphisms in the A1 and A2A adenosine receptor genes have been associated with a higher risk of apnea of prematurity as well as variability in response to xanthine therapy.15 These observations may help ...
Adenosine is a multi-functional physiological molecule found abundantly in the body. It is one of the important components of ATP cellular energy metabolism. Adenosine has diverse actions as a ligand on many different types of cells and tissues acting via specific receptors. Currently, four subtypes of adenosine receptors are described, namely, the A1, A2A, A2B and A3 receptors. Neuroblastoma, mostly found in young children, is a malignant tumor derived from peripheral neurons in the body. Several different types of neuroblastoma cell lines of human origin have been established and contributed to the studies of neuroblastoma itself, neuronal differentiation, neurotransmitters, alcoholism, Alzheimers disease and other neuronal diseases and disorders. In 1987, it was shown by Abbracchio et al. that a human neuroblastoma cell line, IMR32, could be induced to differentiate into cells that have a more neuronal morphology, with long neurites, by an adenosine receptor agonist ...
Effects of adenosine receptor agonists of the A1, A2A and A3 subtypes on the proinflammatory activity of human neutrophils in ...
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Intra- and extracellular adenosine levels rise in response to physiological stimuli and with metabolic/energetic perturbations, inflammatory challenge and tissue injury. Extracellular adenosine engages members of the G-protein coupled adenosine receptor (AR) family to mediate generally beneficial acute and adaptive responses within all constituent cells of the heart. In this way the four AR sub-types - A1, A2A, A2B, and A 3Rs - regulate myocardial contraction, heart rate and conduction, adrenergic control, coronary vascular tone, cardiac and vascular growth, inflammatory-vascular cell interactions, and cellular stress-resistance, injury and death. The AR sub-types exert both distinct and overlapping effects, and may interact in mediating these cardiovascular responses. The roles of the ARs in beneficial modulation of cardiac and vascular function, growth and stress-resistance render them attractive therapeutic targets. However, interactions between ARs and with other receptors, and their ubiquitous
The IUPHAR/BPS Guide to Pharmacology. cyclopentyladenosine ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
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Recent evidence indicates that topical application of adenosine A(2A) receptor agonists, unlike growth factors, increases the rate at which wounds close in normal animals and promotes wound healing in diabetic animals as well as growth factors, yet neither the specific adenosine receptor involved no …
References for Abcams Recombinant Human Adenosine Receptor A2a protein (ab126024). Please let us know if you have used this product in your publication
The adenosinergic system is essential in the mediation of intrinsic protection and myocardial resistance to insult; it may be considered a cardioprotective molecule and adenosine receptors (ARs) represent potential therapeutic targets in the setting of heart failure (HF). The aim of the study was to test whether differences exist between mRNA expression of ARs in the anterior left ventricle (LV) wall (pacing site: PS) compared to the infero septal wall (opposite region: OS) in an experimental model of dilated cardiomyopathy. Cardiac tissue was collected from LV PS and OS of adult male minipigs with pacing-induced HF (n = 10) and from a control group (C, n = 4). ARs and TNF-α mRNA expression was measured by Real Time-PCR and the results were normalized with the three most stably expressed genes (GAPDH, HPRT1, TBP). Immunohistochemistry analysis was also performed. After 3 weeks of pacing higher levels of expression for each analyzed AR were observed in PS except for A1R (A1R: C = 0.6±0.2, PS = ...
Read A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics by with Rakuten Kobo. This book, with its 16 chapters, documents the present state of knowledge of the adenosine A receptor. It covers a wide ...
Caffeine Acts via A1 Adenosine Receptors to Disrupt Embryonic Cardiac Function. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Vidarabine, CAS: 5536-17-4, is A neurotransmitter that acts as the preferred endogenous agonist at all adenosine receptor subtypes. Cited in 2 publications
Adenosine acts as a break in biological systems, having inhibiting effects, but caffeine doesnt just stop this break, it also makes other neurotransmitters more active. For instance, it prevents breakdown of acetylcholine (ACh), so ACh sticks around longer, increasing its effect ...
Adenosine is a ubiquitous signaling molecule whose physiological functions are mediated by its interaction with four G-protein-coupled receptor subtypes, termed A(1), A(2A), A(2B) and A(3). As a result of increased metabolic rates, this nucleoside is released from a variety of cells throughout the b …
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Child mortality rate is the probability of dying between the exact ages of one and five, if subject to current age-specific mortality rates. The probability is expressed as a rate per 1,000.This page has the latest values, historical data, forecasts, charts, statistics, an economic calendar and news for Mortality rate - female child (per 1;000 female children age one) in Guatemala.
A review. The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain G protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various species, including rat and human, and its sequences are highly similar across species, ranging from 85% identity between human and mouse and 95% identity between rat and mouse. The A2B receptors show a ubiquitous distribution, the highest levels are present in cecum, colon and bladder, followed by blood vessels, lung, eye and mast cells. Through A2B receptors adenosine seems to cause mast cells degranulation, vasodilation, cardiac fibroblast proliferation, inhibition of Tumor Necrosis Factor (TNF-α), increased synthesis of interleukin-6 (IL-6), stimulation of Cl- secretion in intestinal epithelia and hepatic glucose prodn. Hence, A2B adenosine receptor agonists could be useful ...
Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients.1-4 In addition, both adenosine and dipyridamole produce severe bronchoconstriction when given to asthmatics. Because of its ultrashort half-life, adenosine must be administered by a constant IV infusion.. Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A1, A2B, and A3.5 The discovery of highly selective and relatively short-acting adenosine receptor A2A agonists6-9 has opened the ...
Disclosed are processes for the synthesis of novel compounds that are A.sub.2B adenosine receptor antagonists, having the structure of Formula I or Formula II: ##STR00001## by cyclizing a compound of the formula (3): ##STR00002##
Caffeine, an adenosine receptor antagonist, blocks various receptors in the brain which are activated by adenosine. Initial results of the team of researchers had already indicated that the blockade of the adenosine receptor subtype A2A in particular could play an important role. Initially, Prof. Müller and her colleagues developed an A2A antagonist in ultrapure and water-soluble form (designated MSX-3). This compound had fewer adverse effects than caffeine since it only blocks only the A2A adenosine receptor subtype, and at the same time it is significantly more effective. Over several weeks, the researchers then treated genetically altered mice with the A2A antagonist. The mice had an altered tau protein which, without therapy, leads to the early development of Alzheimers symptoms ...
The involvement of a guanine-nucleotide-binding regulatory protein (G protein) in the relaxing responses to adenosine receptor agonists was investigated in bovine coronary vessels. Ring segments of left anterior descending artery branches were suspended in organ baths for measurement of isometric tension. The adenosine analogs, 5-N-ethylcarboxamidoadenosine (NECA) and 2-chloroadenosine (CAD) caused concentration-dependent relaxations of coronary rings contracted with KCl. The relaxing effects of NECA and CAD were antagonized by the adenosine receptor antagonist 8-phenyltheophylline indicating the involvement of an adenosine receptor. In a separate series of experiments, incubation with cholera toxin inhibited the relaxing responses to NECA, CAD and isoproterenol but not those produced by sodium nitroprusside. Treatment with forskolin did not reduce the relaxing responses to NECA or CAD. N-ethylmaleimide and NaF/AlCl3 caused significant inhibition of the relaxations produced by both NECA and ...
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Summary 1. The effect of the adenosine A2 receptor (AdoA2R) agonist N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)-ethyl]adenosine (DPMA) on adenosine A1 receptor (AdoA1R)-mediated negative inotropic responses was investigated in rat heart. 2. Hearts from male Wistar rats (250-350 g) were perfused with Krebs-Henseleit solution at constant flow in non-recirculating Langendorff mode. Hearts were paced at 5 Hz (5 ms duration, supramaximal voltage) via ventricular electrodes. After 30 min equilibration, (R)-N6-phenylisopropyl adenosine (R-PIA) concentration-response curves were constructed in the absence or presence of DPMA. 3. In paced hearts, R-PIA induced concentration-dependent decreases in triple product (heart rate נpeak systolic developed pressure נdP?/?dtmax), which were significantly attenuated by 1 nmol?/?L DPMA with a shift in pEC50 from 8.0 ᠰ.5 (n = 9) in control hearts to 6.63 ᠱ.03 (n = 5) in treated tissues (P , 0.05). The AdoA2AR antagonist 8-(3-chlorostyryl)caffeine (1 ...
A2A and A2B extracellular adenosine receptors. There are four different adenosine receptors: A1, A2A, A2B, and A3 (25). The high-affinity A1 receptor and the low-affinity A3 receptor are Gi protein coupled. The cAMP-elevating Gs protein-coupled A2 receptors are subdivided into high-affinity A2AR and low-affinity A2BR. Adenosine receptors are known to be immunosuppressive. The CD8+ and CD4+ T cells, including antitumor CD8+ and human T cells, predominantly express A2AR and A2BR (12, 14, 26). The cAMP-elevating signaling through A2AR results in inhibition of TCR-triggered effector functions, including proliferation, expansion, and secretion by T cells of such important antitumor cytokines as IFN-γ and tumor necrosis factor-α (14, 22).. Tumor hypoxia and accumulation of extracellular adenosine. Many solid tumors are characterized by an insufficient oxygen supply and transient or chronic hypoxia in some microenvironments (27). Tumor hypoxia may contribute to the propagation of oncogenic signals in ...
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Home » Adenosine monophosphate. Definition noun (1) A nucleotide composed of adenine, ribose and a phosphate group. (2) An ester of phosphoric acid and the nucleoside adenosine, and with a molecular formula: C10H14N5O7P ...
The protein encoded by this gene is an adenosine receptor that belongs to the G-protein coupled receptor 1 family. There are 3 types of adenosine receptors, each with a specific pattern of ligand binding and tissue distribution, and together they regulate…
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... s modulate P2 purinergic signaling, and P1 receptors. In addition, ectonucleotidases generate extracellular ... Impact of Ectoenzymes on P2 and P1 Receptor Signaling", Advances in Pharmacology, Pharmacology of Purine and Pyrimidine ... Beldi, G; Enjyoji, K; Wu, Y; Miller, L; Banz, Y; Sun, X; Robson, SC (Jan 1, 2008). "The role of purinergic signaling in the ... The contribution of ectonucleotidases in the modulation of purinergic signaling depends on the availability and preference of ...
"Impact of ectoenzymes on p2 and p1 receptor signaling". Pharmacology of Purine and Pyrimidine Receptors. Advances in ... "Comparative hydrolysis of P2 receptor agonists by NTPDases 1, 2, 3 and 8". Purinergic Signalling. 1 (2): 193-204. doi:10.1007/ ... NTPDase1 hydrolyzes P2 receptor ligands, namely ATP, ADP, UTP and UDP with similar efficacy. NTPDase1 can therefore effect P2 ... Sepúlveda C, Palomo I, Fuentes E (2016). "Role of adenosine A2b receptor overexpression in tumor progression". Life Sciences. ...
Histological staining by another research group examined the distribution of purinergic receptor subtypes throughout the RVM. ... a large majority were co-labeled with purinergic antibodies. Fifty-five percent of TPH+ neurons stained for P1, 63% for P2X1, ... Close, L.N. (January 2009). "Purinergic Receptor Immunoreactivity in the Rostral Ventromedial Medulla". Neuroscience. 158 (2): ... NK1 agonism induced hypersensitivity is dependent on 5-HT3 receptors, and modulated by GABAA and NMDA receptors as well. ...
Similarly, adenosine triggers degranulation through P1 receptors. Uric acid is also an endogenous danger signal released by ... that have reached the extracellular space can also serve as danger signals by signaling through purinergic receptors. ATP and ... DAMPs and their receptors are characterized as: Two papers appearing in 1994 presaged the deeper understanding of innate immune ... Blocking the DAMP receptors or their signaling - RAGE small molecule antagonists, TLR4 antagonists, antibodies to DAMP-R DAMPs ...
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. This receptor has an inhibitory function ... Adenosine receptors play a key role in the homeostasis of bone. The A1 receptor has been shown to stimulate osteoclast ... The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors ...
P is for purinergic, P2 refers to ATP receptors, as opposed to P1 adenosine adenosine receptors. P2X receptors are ATP ... P2X receptors are ionotropic receptors while P2Y are GPCR type receptors. P2X receptor family encompasses 7 genes. P2Y family ... Depending on the nature of the receptor they are found to be of two types: P2Y receptors (metabotropic) P2X receptors ( ... Almost every cell type expresses P2 receptors. Purinergic signalling also has a pathophysiological role in several immune cells ...
There are two main types of purinergic receptors, P1 binding to adenosine, and P2 binding to ATP or ADP, presenting different ... Therefore, there are four main transmembrane receptor types: G protein coupled receptors (GPCRs), tyrosine kinase receptors ( ... PAR1 and PAR4 receptors), platelet-derived thromboxane A2 (TxA2) (TP receptor) and ADP (P2Y1 and P2Y12 receptors) that is ... Adenosine acts by binding to purinergic receptors and influencing adenylyl cyclase activity and the formation of cAMP and PKA ...
There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. [What about P2Z,U,T?] P2X ... P1 receptors are preferentially activated by adenosine and P2Y receptors are preferentially more activated by ATP. P1 and P2Y ... IUPHAR GPCR Database - Adenosine receptors IUPHAR GPCR Database - P2Y receptors Purinergic+Receptors at the US National Library ... P2 receptors) or adenosine (P1 receptors). P2 receptors have further been divided into five subclasses: P2X, P2Y, P2Z, P2U, and ...
There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. Cell signalling events ... The purinergic signalling complex of a cell is sometimes referred to as the "purinome". Purinergic receptors, represented by ... Purinergic receptors are specific classes of membrane receptors that mediate various physiological functions such as the ... There are currently four types of adenosine receptors found in the heart. After binding onto a specific purinergic receptor, ...
... biosafety-level-2 laboratory P2 receptor, a purinergic and pyrimidinergic cell surface receptor P2, a pulmonic valve closure ... a variant of the 1923 P-1 Hawk biplane fighter of the United States Army Air Corps P-2 Neptune, known as "P2V Neptune" until ...
... receptor, par-1 MeSH D12.776.543.750.810.150 - receptors, cyclic amp MeSH D12.776.543.750.810.700 - receptors, purinergic p1 ... purinergic MeSH D12.776.543.750.720.700.150 - receptors, cyclic amp MeSH D12.776.543.750.720.700.700 - receptors, purinergic p1 ... receptors, purinergic p1 MeSH D12.776.543.750.100.700.700.100 - receptor, adenosine a1 MeSH D12.776.543.750.100.700.700.200 - ... receptors, purinergic p2 MeSH D12.776.543.750.725.500 - receptor, notch1 MeSH D12.776.543.750.725.750 - receptor, notch2 MeSH ...
... purinergic P1 receptor - purinergic P2 receptor - purinergic receptor - pyridine - pyrimidine - pyruvate - pyruvate oxidation ... interleukin receptor - interleukin-1 receptor - interleukin-2 receptor - interleukin-3 - interleukin-3 receptor - intermediate ... G protein-coupled receptor - G3P - GABA - GABA receptor - GABA-A receptor - gag-onc fusion protein - galanin - gamete - gamma- ... IgE receptor - IGF type 1 receptor - IGF type 2 receptor - IgG - IgM - immediate-early protein - immune cell - immune system - ...
Harden TK, Boyer JL, Nicholas RA (1995). „P2-purinergic receptors: subtype-associated signaling responses and structure". ... P1 receptori. adenozin. G protein spregnuti receptori P2Y receptori. nukleotidi *ATP. *ADP ... Biogeno aminski receptor - Eikozanoidni receptor (Prostaglandinski receptor) - G protein-spregnuti receptor - Imunski receptor ... Neurotransmiterski receptor - Mirisni receptori - Proteazom-aktivirani receptor - Purinski receptor - Transferinski receptor ...
Receptorji P1 imajo podtipe A1, A2a, A2b in A3 (A je ostalo od stare nomenklature, kot adenozinski receptor) in vsi so ... Fields, R.D. and Burnstock G. (2006). "Purinergic signalling in neuron-glia interactions". Nature Reviews Neuroscience 7 (6): ... purinergični nukleotidi niso močni agonisti receptorjev P1. ...
... and neurokinin 1 receptor (NK1R), as well as activation of metabotropic glutamate receptors and release of BDNF. Persistent ... The resultant patterning along the neuraxis leads to segmentation of the neuroepithelium into progenitor domains (p0, p1 p2, p3 ... October 2005). "Astrocytic purinergic signaling coordinates synaptic networks". Science. 310 (5745): 113-6. Bibcode:2005Sci... ... and kainate subtypes of ionotropic glutamate receptors follows. It is the activation of these receptors that potentiates the ...
Klasifikacija transporter/receptor[uredi , uredi izvor]. *GluT tip ispoljva se kaoglutamatski transporteri (EAAT1/SLC1A3 i ... Studije koje je sa suradnicima objavio Hoechst, pokazale su da iz astrocita proizilaze tri različite skupine domena p1, p2 i p3 ... "Astrocytic purinergic signaling coordinates synaptic networks". Science 310 (5745): 113-6. PMID 16210541. doi:10.1126/science. ... Rezultanta se ispoljava u segmentaciji neuroepitela u progenitorne domene (p0, p1 p2, p3 and pMN) za razne tipove neurona i ...
Eicosanoid receptor (Prostaglandin receptor). *Protease-activated receptor. *Neurotransmitter receptor. *Purinergic receptor. * ... Rats rely heavily on olfactory sensory input from olfactory receptors for behavioral attitudes.[28] Studies show that bilateral ... The olfactory tubercle has been shown to be concerned primarily with the reception of sensory impulses from olfactory receptors ... receptor D3 is abundant in this two areas [6]). In addition, the OT contains tightly packed cell clusters known as the islands ...
Transporter/receptor classification[edit]. *GluT type: these express glutamate transporters (EAAT1/SLC1A3 and EAAT2/SLC1A2) and ... The resultant patterning along the neuraxis leads to segmentation of the neuroepithelium into progenitor domains (p0, p1 p2, p3 ... "Astrocytic purinergic signaling coordinates synaptic networks". Science. 310 (5745): 113-6. Bibcode:2005Sci...310..113P. doi: ... of the effects of marijuana on short term memories found that THC activates CB1 receptors of astrocytes which cause receptors ...
Eicosanoid receptor (Prostaglandin receptor). *Protease-activated receptor. *Neurotransmitter receptor. *Purinergic receptor. * ... GABA receptors: GABA-A, GABA-C. GABA. Cl− , HCO−3 [11]. Glutamate receptors: NMDA receptor, AMPA receptor, and Kainate receptor ... toll-like receptors (TLRs), killer activated and killer inhibitor receptors (KARs and KIRs), complement receptors, Fc receptors ... receptors, G protein-linked (metabotropic) hormone receptors, and enzyme-linked hormone receptors.[1] Intracellular receptors ...
Receptor. (ligands). P0 (adenine). *Agonists: 8-Aminoadenine. *Adenine. P1. (adenosine). *Agonists: 2-(1-Hexynyl)-N- ... Purinergic signalling. *Pyrophosphates. Hidden categories: *Chemical articles with multiple compound IDs. *Multiple chemicals ... ADP interacts with a family of ADP receptors found on platelets (P2Y1, P2Y12, and P2X1), which leads to platelet activation.[14 ... P2Y1 receptors initiate platelet aggregation and shape change as a result of interactions with ADP. ...
Eicosanoid receptor (Prostaglandin receptor). *Protease-activated receptor. *Neurotransmitter receptor. *Purinergic receptor. * ... An example of membrane receptors. *Ligands, located outside the cell. *Ligands connect to specific receptor proteins based on ... The receptor releases a messenger once the ligand has connected to the receptor. ... Wikipedia:MeSH D12.776#MeSH D12.776.543.750 - receptors.2C cell surface. അവലംബം[തിരുത്തുക]. *↑ Hall, JE (2016). Guyton and Hall ...
... of the effects of marijuana on short term memories found that THC activates CB1 receptors of astrocytes which cause receptors ... The resultant patterning along the neuraxis leads to segmentation of the neuroepithelium into progenitor domains (p0, p1 p2, p3 ... "Astrocytic purinergic signaling coordinates synaptic networks". Science. 310 (5745): 113-6. Bibcode:2005Sci...310..113P. doi: ... Transporter/receptor classificationEdit. *GluT type: these express glutamate transporters (EAAT1/SLC1A3 and EAAT2/SLC1A2) and ...
... ResearchSpace/Manakin Repository. Login ... Purinergic Signalling and Aminoglycoside Ototoxicity: The role of P1 and P2 receptors. Lin, Ching Yu ... Activation of P1/adenosine receptors (AR), on the other hand, partially protected the organ of Corti against neomycin-induced ... Both adenosine-sensitive P1 and nucleotide-sensitive P2 receptors are extensively distributed in the sensory and supporting ...
Category: Purinergic P1 Receptors Data Availability StatementThe datasets used and/or analyzed during the current research. ... Nevertheless, the receptors that YKL-40 might bind to initiate signaling transduction remain elusive, with the exception of ... For instance, Cav channels directly interact with another type of calcium channel, the ryanodine receptor, on the sarcoplasmic ... which includes four Cav1.1 subunits and a INK 128 inhibitor database tetrameric ryanodine receptor calcium-release route, RyR1 ...
Purinergic P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. To Top ...
Purinergic Agents. *Purinergic Agonists. *Purinergic P1 Receptor Agonists. *Purines. *Ribonucleosides. *Sensory System Agents ... Adenosine receptor A2a. MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAA.... yes. agonist. Adenosine receptor A2b. ... Adenosine receptor A1. MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVS.... yes. agonist. Adenosine receptor A3. ... This effect may be mediated through the drugs activation of cell-surface A,sub,1,/sub, and A,sub,2,/sub, adenosine receptors. ...
Purinergic P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. Analgesics. Sensory ... The adenosine receptor is known for its anti-inflammatory actions and could therefore be a potential target in the treatment of ... Antagonism of the adenosine receptor by caffeine leads to an increased LPS-induced inflammatory reaction and an increase in ( ... Stimulation of the adenosine receptor could potentially lead to a decrease in inflammation and tissue damage. ...
Purinergic P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. To Top ...
Purinergic P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. To Top ...
Purinergic Agents. *Purinergic Agonists. *Purinergic P1 Receptor Agonists. *Purines. *Ribonucleosides. *Sensory System Agents ... Adenosine receptor A1 MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVS... yes. agonist. Adenosine receptor A2b ... Adenosine receptor A3 MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYF... yes. agonist. Adenosine receptor A2a ... Adenosine may exert its pharmacologic effects by activation of purine (cell surface A1 and A2 adenosine) receptors, as well as ...
... signaling molecule whose physiological functions are mediated by its interaction with four G-protein-coupled receptor subtypes ... Receptors, Purinergic P1 / metabolism* Substances * Receptors, Purinergic P1 ... Adenosine receptors and cancer Biochim Biophys Acta. 2011 May;1808(5):1400-12. doi: 10.1016/j.bbamem.2010.09.020. Epub 2010 Oct ... by addressing the question of whether adenosine receptors are present in cancer tissues, and, if so, which receptor subtype ...
... receptor. The aim of the present study was to elucidate the effects of PD81,723 both as a … ... Purinergic P1 Receptor Agonists * Purinergic P1 Receptor Antagonists * Receptors, Purinergic P1 / genetics ... receptor. We investigated its effect on the human wild-type in relation to a mutant (T277A) adenosine A(1) receptor for which ... The effect of PD81,723 on the mutant receptor was much less pronounced. Mutation of Thr277 to Ala not only decreased agonist ...
Ectonucleotidases modulate P2 purinergic signaling, and P1 receptors. In addition, ectonucleotidases generate extracellular ... Impact of Ectoenzymes on P2 and P1 Receptor Signaling", Advances in Pharmacology, Pharmacology of Purine and Pyrimidine ... Beldi, G; Enjyoji, K; Wu, Y; Miller, L; Banz, Y; Sun, X; Robson, SC (Jan 1, 2008). "The role of purinergic signaling in the ... The contribution of ectonucleotidases in the modulation of purinergic signaling depends on the availability and preference of ...
Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently ... Receptors, Purinergic P1 / biosynthesis, drug effects*, genetics. Stereoisomerism. Structure-Activity Relationship. ... Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently ... 0/Phenethylamines; 0/Receptors, Purinergic P1; 0/Xanthines; 120225-54-9/CGS 21680; 29193-86-0/Phenylisopropyladenosine; 35788- ...
0/Receptors, Purinergic P1; 50-99-7/Glucose; 56-65-5/Adenosine Triphosphate; 58-61-7/Adenosine; 58-63-9/Inosine; 7782-44-7/ ... The selective A(3) adenosine receptor antagonist MRS 1523 attenuated the protective effects of adenosine and inosine, while an ... Next Document: P2Y(1) receptors mediate inhibitory neuromuscular transmission in the rat colon.. ... A(3) adenosine receptor agonist provided a partial protective effect. Adenosine deaminase inhibition attenuated the ...
Receptors, Purinergic P1. 2. 2019. 111. 0.920. Why? Autoantigens. 6. 2014. 940. 0.900. Why? ... Nuclear Receptor Subfamily 1, Group F, Member 3. 1. 2012. 106. 0.130. Why? ... NK Cell Lectin-Like Receptor Subfamily B. 1. 2014. 71. 0.160. Why? ...
There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. Cell signalling events ... The purinergic signalling complex of a cell is sometimes referred to as the "purinome". Purinergic receptors, represented by ... Purinergic receptors are specific classes of membrane receptors that mediate various physiological functions such as the ... There are currently four types of adenosine receptors found in the heart. After binding onto a specific purinergic receptor, ...
Adenosine acts directly by stimulating adenosine purinergic P1 receptors on the arterial wall. Dipyridamole is believed to work ... Adenosine receptor agonists for the promotion of wound healing. US5942497. 2 Jun 1997. 24 Ago 1999. Fukunaga; Atsuo F.. Purine ... Adenosine receptor agonists for the promotion of wound healing. US6221669. 13 Feb 1996. 24 Abr 2001. Lifecell Corporation. ... At this point in time, no difference in the occurrence of A2 receptor-related side effects, or severity of symptoms, has become ...
... which could lead to activation of P1 purinergic receptors. As one approach to assess the involvement of P2 and P1 receptors in ... and concentration-dependent manner and was inhibited by antagonists of P2 and P1 purinergic receptors. Agonist studies revealed ... Activation of Astrocytic Purinergic Receptors Stimulates Expression and Release of TSP-1.. To determine whether TSP-1 ... 2 Bb). This finding indicates that, although P1 receptors may be coupled to TSP-1 production, degradation of ATP to AMP or ...
Previously, we found that the expression of purinergic P2Y2 receptor (P2Y2R) is increased in GC samples as compared to adjacent ... Taken together, these results demonstrate the involvement of different purinergic receptors and signaling in GC, and the ... we detected the expression of several purinergic receptors, and found important differences as compared to GES-1 cells. ... we detected the expression of several purinergic receptors, and we found important differences compared to GES-1 cells. ...
Purinergic receptors (P1, P2Y, and P2X) and ectonucleotidases (CD39 and CD73) have been widely implicated in health and disease ... Purinergic receptors are amongst the most abundant receptor type in living organisms and are widely found in the immune system ... In recent years, there has been increased interest in the roles of purinergic receptors as key mediators of inflammation and ... There is now growing evidence that purinergic signaling is involved in the immune response against mycobacteria, viruses, fungi ...
Purinergic P1 Receptors (Adenosine Receptor) Related Therapies and Procedures. 1. Transplants (Transplant) ... decreased behavior induced by putative pain neurotransmitters providing additional support for an endogenous purinergic system ...
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. ... Purinergic P1 Receptors (Adenosine Receptor) 4. 2- (4- (2- carboxyethyl)phenethylamino)- 5- N- ethylcarboxamidoadenosine ... 05/01/1998 - "The effect of serotonergic agents was studied on the adenosine A2 receptor agonist NECA-induced catalepsy in mice ... A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. ...
... purinergic nucleotides like ATP are not strong agonists of P1 receptors which are strongly activated by adenosine and other ... P1 receptors have A1, A2a, A2b, and A3 subtypes (A as a remnant of old nomenclature of adenosine receptor), all of which are ... axons and glia activates purinergic membrane receptors known as P2. The P2Y receptors are metabotropic, i.e. G protein-coupled ... purinergic receptors.. In humans, this signaling role is important in both the central and peripheral nervous system. Activity- ...
Adenosine is a signaling molecule that regulates cellular activity in the CNS through P1 purinergic receptor (Kaster et al., ... PPADS is a nonselective (but nonuniversal) P2 receptor antagonist and does not block P1 receptor (Lambrecht, 2000; Lambrecht et ... 4E,F) and PPADS blocks P2 receptors but not P1 receptors (Lambrecht, 2000). ... The P2 purinergic receptors comprise seven P2X receptor subunits (P2X1-7), which are ligand-gated ion channels (North, 2002), ...
P1 or Adenosine receptors GraphId=aba11, ,Graphics CenterX=845.8450842431788 CenterY=587.9216367603486 Width= ... Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications.,/bp:TITLE, ,bp: ... nucleotide signaling via the purinergic P2Y receptors.,/bp:TERM, ,bp:ID xmlns:rdf=http://www.w3.org/1999/02/22-rdf-syntax-ns# ... Purinergic signalling is involved in several processes including neurologic, endocrine, and immune system signalling. ,/Comment ...
Purinergic P1 Receptor Antagonists. Not Applicable. Interventional clinical trials:. #. Name. Status. NCT ID. Phase. Drugs. ...
Purinergic P1 Receptors (Adenosine Receptor): 4 studies in 23 results : IBA. *Adenosine: 4 studies in 22 results : FDA 19 ... Drug Receptors (Drug Receptor): 1 study in 1 result : IBA. *T-Cell Antigen Receptors (T-Cell Receptor): 1 study in 1 result : ... MT2 Melatonin Receptor: 1 outcome in 1 result : IBA. *Melanocortin Receptors (Melanocortin Receptor): 1 outcome in 1 result : ... Androgen Receptors (Androgen Receptor): 1 study in 43 results : IBA. *RNA-Binding Proteins (RNA-Binding Protein): 1 study in 42 ...
Purinergic receptors activated by extracellular nucleotides (adenosine 5′-triphosphate (ATP) and uridine 5′-triphosphate (UTP ... ATP P2X receptors P2Y receptors P1 receptors Rat embryo Heart Cardiomyocyte FLIPR Calcium mobilization ... and P2Y receptors: ligand design and receptor interactions. Purinergic Signal 8:419-436CrossRefPubMedCentralPubMedGoogle ... A basis for distinguishing two types of purinergic receptor. In: Straub RW, Bolis L (eds) Cell membrane receptors for drugs and ...
These receptors are critical to normal cell physiology. *Adenosine is thought to act predominantly via P1 receptors, which are ... ATP and its major metabolite adenosine interact with specific purinergic receptors. ... P1 receptors are located on endothelial cells and mediate a vasodilatation response ... ATP binds to P2 receptors, which are subclassified into *P2Y - G protein coupled receptors. ...
Both P1 and P2 receptors participate in neurone-glia interactions. Purinergic signalling is involved in control of cerebral ... Both P1 and P2 receptors participate in neurone-glia interactions. Purinergic signalling is involved in control of cerebral ... P2 receptors. Abstract: There is a widespread presence of both adenosine (P1) and P2 nucleotide receptors in the brain on both ... nucleotide receptors, presynaptic neuromodulation, P2X receptors, Purinergic signalling, purinoceptors, Parkinsons disease, P2 ...
In 1978, Burnstock proposed two types of purinergic receptors: P1 receptors selective for adenosine and P2 receptors selective ... While early studies focused on the role of purinergic receptors in neurotransmission, it soon became obvious that extracellular ... G. Burnstock, "Purinergic nerves.," Pharmacological Reviews, vol. 24, no. 3, pp. 509-581, 1972. View at Google Scholar · View ... A. Battastini and colleagues present an overview of the various roles of purinergic signaling in gliomas. In gliomas, the ...
  • Paradoxically, A(3) receptor antagonists also appear to be promising candidates in human cancer treatment of regimes. (nih.gov)
  • Binding (saturation and displacement experiments) and functional adenosine 3',5'-cyclic monophosphate studies were performed, and differential effects of allosteric enhancer PD81,723 on agonists and antagonists were observed on the wild-type (wt) and mutant adenosine A(1) receptor. (nih.gov)
  • Within the concept of a simplified two-state receptor model, it is possible that the effects of PD81,723 are mainly "allosteric", enhancing the binding of adenosine A(1) agonists and inhibiting the binding of antagonists/inverse agonists. (nih.gov)
  • It further supported a differential binding mode of PD81,723 compared to competitive antagonists for the adenosine A(1) receptor. (nih.gov)
  • 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)
  • In GES-1 cells, ATP and UTP induced similar responses and the combination of P2X and P2Y receptor antagonists was able to block them. (frontiersin.org)
  • The effects of UTP and ATP were prevented by both wide-range and specific purinergic antagonists. (frontiersin.org)
  • Notably, the isolated application of purinergic antagonists was sufficient to change the basal proliferation of AGS cells, indicating that nucleotides released by the cells can act as paracrine/autocrine signals. (frontiersin.org)
  • Treatment of primary cultures of rat cortical astrocytes with extracellular ATP caused an increase in TSP-1 expression in a time- and concentration-dependent manner and was inhibited by antagonists of P2 and P1 purinergic receptors. (pnas.org)
  • 100 nM), or the purinoceptor antagonists 8- phenyltheophyline (P1 receptors) or suramin (P2 receptors). (edu.au)
  • Described are uses of A.sub.2a adenosine receptor antagonists and agonists to provide long term modulation of immune responses. (patents.com)
  • A.sub.2a receptor antagonists in particular are provided to enhance immune responses by reducing T-cell mediated tolerance to antigenic stimuli and agonists are provided to enhance effectiveness of immunosuppressive agents. (patents.com)
  • 0004] This application relates to uses of A.sub.2a adenosine receptor agonists and antagonists to modulate T-cell mediated tolerance to antigenic stimuli. (patents.com)
  • Receptor antagonists are very useful tools for evaluating the role of LPA and its receptors in biological actions and for controlling specific diseases ( Tigyi, 2001 ). (aspetjournals.org)
  • Based on their ability to inhibit Ca 2+ response to LPA in A431 cells or LPA-responsive cells, we have screened 150,000 low-molecular-weight compounds developed by the Kirin Brewery Co. Ltd, for LPA receptor antagonists, and found that some isoxazole derivatives showed such an inhibitory activity against the LPA action. (aspetjournals.org)
  • Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications. (wikipathways.org)
  • Potent adenosine receptor antagonists that are selective for the A1 receptor subtype. (wikipathways.org)
  • Adenosine receptors: development of selective agonists and antagonists. (wikipathways.org)
  • Two of these strategies, the development of selective adenosine kinase inhibitors and P2X 3 receptor-selective antagonists, are highlighted in this review of the recent developments in the pharmacology of purinergic modulation of nociceptive signaling. (cognizantcommunication.com)
  • This involvement suggests the possible use of purinergic agonists and antagonists as therapeutic targets for ocular inflammation. (ucm.es)
  • In contrast, inhibition of NF-κB activation by MTX was not mediated via BH 4 depletion and JNK activation in FLSs, but rather was completely prevented by adenosine receptor antagonists.Conclusion. (elsevier.com)
  • This effect was likely mediated via adenosine A1 receptor (A1R), as the selective A1R agonist ADAC (1 µM) conferred a higher degree of hair cell protection than adenosine, which activates all AR. (auckland.ac.nz)
  • The 2-amino-benzoylthiophene derivative PD81,723 [(2-amino-4,5-dimethyl-trienyl)[3-(trifluoromethyl) phenyl]methanone] has been shown to allosterically enhance agonist binding and function at the adenosine A(1) receptor. (nih.gov)
  • The A3 receptor was characterized utilizing the nonselective agonist [3H]NECA. (biomedsearch.com)
  • The selective A(3) adenosine receptor antagonist MRS 1523 attenuated the protective effects of adenosine and inosine, while an A(3) adenosine receptor agonist provided a partial protective effect. (biomedsearch.com)
  • 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 stable adenosine A1 and A2 receptor agonist. (curehunter.com)
  • The extracellular adenosine formed acts as an agonist of purinergic P1 receptors. (scienceopen.com)
  • 2-Chloro-N6-[3H]cyclopentyladenosine ([3H]CCPA)--a high affinity agonist radioligand for A1 adenosine receptors. (wikipathways.org)
  • An A1 adenosine receptor agonist. (nih.gov)
  • Over the last decade, new concepts have been gradually substantiated, such as receptor preference for the regulation of certain classes of G-proteins in cells, agonists' selection of G-protein classes for internalizing their effects, and the regulation of the functional state of G a subunits and G bg dimers shuttling between activated receptors and effectors during agonist signal propagation. (cognizantcommunication.com)
  • SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. (elsevier.com)
  • P1 receptors are preferentially activated by adenosine and P2Y receptors are preferentially more activated by ATP. (wikipedia.org)
  • P1 are G-protein-coupled receptors activated by adenosine. (alzforum.org)
  • Adenosine is a ubiquitous signaling molecule whose physiological functions are mediated by its interaction with four G-protein-coupled receptor subtypes, termed A(1), A(2A), A(2B) and A(3). (nih.gov)
  • Although all adenosine receptors now have an increasing number of recognised biological roles in tumors, it seems that the A(2A) and A(3) subtypes are the most promising as regards drug development. (nih.gov)
  • Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. (biomedsearch.com)
  • Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently known. (biomedsearch.com)
  • In this study we present for the first time the comparative pharmacology of all known human adenosine receptor subtypes. (biomedsearch.com)
  • These cells are valuable systems for further characterization of specific receptor subtypes and for the development of new ligands. (biomedsearch.com)
  • 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)
  • Immunofluorescence data indicated that only P2X2 and P2X4 receptor proteins were expressed in E14 cardiomyocytes while protein for all the P2X receptor subtypes was expressed in E18, except for P2X3 and P2X6. (springer.com)
  • Responses mediated by agonists specific for P2Y receptors subtypes showed that P2Y receptors (P2Y 1 , P2Y 2 , P2Y 4 and P2Y 6 ) were also present in both E14 and E18 cardiomyocytes. (springer.com)
  • Our results show that specific P2 receptor subtypes are present in embryonic rat cardiomyocytes, including P2X7 and P2Y 4 receptors that have not been identified in adult rat cardiomyocytes. (springer.com)
  • Burnstock G, Knight GE (2004) Cellular distribution and functions of P2 receptor subtypes in different systems. (springer.com)
  • Four subtypes of P1 (adenosine) receptors, 7 subtypes of P2X ion channel receptors and 8 subtypes of P2Y G protein-coupled receptors have currently been identified. (springer.com)
  • Since P2 receptors were first cloned in the early 1990's, there is clear evidence for the widespread distribution of both P1 and P2 receptor subtypes in neuronal and non-neuronal cells, including glial, immune, bone, muscle, endothelial, epithelial and endocrine cells. (springer.com)
  • Several subtypes of P2Y receptor mRNA were identified including P2Y 1 , P2Y 2 , P2Y 4 , and P2Y 6 receptors. (umn.edu)
  • These results indicate that human mammary epithelial cells express multiple P2 receptor subtypes and that Ca 2+ mobilization evoked by P2Y receptor agonists stimulates Na + absorption by increasing the activity of Ca 2+ -activated K + channels located in the basolateral membrane. (umn.edu)
  • Several subtypes of P2Y receptor mRNA were identified including P2Y1, P2Y2, P2Y4, and P2Y6 receptors. (umn.edu)
  • Lysophosphatidic acid (LPA) exerts a variety of biological responses through specific receptors: three subtypes of the EDG-family receptors, LPA 1 , LPA 2 , and LPA 3 (formerly known as EDG-2, EDG-4, and EDG-7, respectively), and LPA 4 /GPR23, structurally distinct from the EDG-family receptors, have so far been identified. (aspetjournals.org)
  • The difference in the inhibition profile of Ki16425 and DGPP 8:0 was exploited for the evaluation of receptor subtypes involved in responses to LPA in A431 cells. (aspetjournals.org)
  • therefore, it may be useful in evaluating the role of LPA and its receptor subtypes involved in biological actions. (aspetjournals.org)
  • There are four subtypes within the P1 receptor class: A1, A2a, A2b, and A3. (acris-antibodies.com)
  • So far, the P2Y receptor family is composed of several cloned and functionally defined subtypes. (acris-antibodies.com)
  • and a division of P2 into P2X and P2Y with seven subtypes of P2X ion channel receptors and eight subtypes of P2Y G-protein-coupled receptors. (whfoods.com)
  • This rapid breakdown results in the activation of a multiplicity of receptor subtypes, which can mediate physiological processes such as proliferation, differentiation, migration, and cell death [16]. (thefreelibrary.com)
  • Four distinct subtypes of P1 receptors have been identified: adenosine A1, A2a, A2b, and A3 receptors (R) which are G protein coupled ( 10 ). (physiology.org)
  • P2Y(1) receptors mediate inhibitory neuromuscular transmission in the rat colon. (biomedsearch.com)
  • Purinergic receptors are specific classes of membrane receptors that mediate various physiological functions such as the relaxation of gut smooth muscle, as a response to the release of ATP or adenosine. (wikipedia.org)
  • 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)
  • 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)
  • Astrocytes express both P2Y and P2X receptors ( 13 - 18 ), and these receptors are coupled to protein kinase cascades, including mitogen-activated protein kinases (MAPKs) and protein kinase B/Akt ( 14 , 15 , 19 , 20 ), that mediate gene expression ( 21 , 22 ). (pnas.org)
  • P2Y receptors largely mediate presynaptic activities. (eurekaselect.com)
  • Macrophages express specific receptors for these signals (P2Y 2 for ATP and UTP, CX3CR1 for fractalkine, and S1PR1 for S1P), which may mediate migration to the dying cells ( Ravichandran, 2011 ). (elifesciences.org)
  • Adenosine A2A receptors mediate GABAergic inhibition of respiration in immature rats. (wikipathways.org)
  • Membrane-bound P2-receptors mediate the actions of extracellular nucleotides in cell-to-cell signalling. (acris-antibodies.com)
  • Studies using local administration of cannabinoid agonists have shown that peripheral, spinal, and supraspinal cannabinoid receptors mediate cannabinoid-induced antinociception. (cognizantcommunication.com)
  • LPA1 receptors mediate stimulation, whereas LPA2 receptors mediate inhibition, of migration of pancreatic cancer cells in response to lysophosphatidic acid and malignant ascites. (ebscohost.com)
  • However, few studies have been performed on the expression of purinergic receptors in SCN. (pubmedcentralcanada.ca)
  • In obese and diabetic states, macrophage expression of purinergic receptors MMP9 and IL-10 is reduced. (diabetesjournals.org)
  • Previous studies of the expression of purinergic receptors in subsets of lymphocytes have been limited to receptors for ATP. (aspetjournals.org)
  • Purinergic signalling (or signaling: see American and British English differences) is a form of extracellular signalling mediated by purine nucleotides and nucleosides such as adenosine and ATP. (wikipedia.org)
  • Released nucleotides can be hydrolyzed extracellularly by a variety of cell surface-located enzymes referred to as ectonucleotidases that control purinergic signalling. (wikipedia.org)
  • Purinergic signaling is a growing area of research investigating the diverse roles of receptors and enzymes that interact with nucleotides and nucleosides such as ATP and adenosine. (frontiersin.org)
  • Purinergic receptors activated by extracellular nucleotides (adenosine 5′-triphosphate (ATP) and uridine 5′-triphosphate (UTP)) are well known to exert physiological effects on the cardiovascular system, whether nucleotides participate functionally in embryonic heart development is not clear. (springer.com)
  • The balance of these two molecules can be generated by extracellular nucleotides, such as adenosine 5'-triphosphate (ATP) and adenosine (Ado), which activate the purinergic receptors system. (biomedcentral.com)
  • Dendritic cells (DCs) express functional purinergic receptors, but the effects of purine nucleotides on DC functions have been marginally investigated. (jimmunol.org)
  • 9 These P2Y receptors are expressed in a variety of tissues and can be differentiated pharmacologically on the basis of their selectivity for adenosine (ATP, ADP) and uridine (UTP, UDP) nucleotides. (ahajournals.org)
  • These observations have suggested that there exist specific cell surface receptors for extracellular ATE Until fairly recently, most studies involving the actions of extracellular ATP and adenine nucleotides were performed on preparations of smooth muscle. (cdc.gov)
  • Macrophages and thymocytes express various purinergic nucleotide receptors that, in the presence of ATP and other nucleotides, regulate immune development and microbial infections ( 3 , 10 ). (asm.org)
  • They hydrolyze extracellular nucleotides and thus can control their availability at purinergic P2 receptors. (scienceopen.com)
  • Biological actions of NTPDases are a consequence (at least in part) of the regulated phosphohydrolytic activity on extracellular nucleotides and consequent effects on P2-receptor signaling. (scienceopen.com)
  • Physiological, pharmacological and molecular biological data generated over the past three decades have demonstrated the existence of two major families of extracellular receptors, the P1, a family of four G-protein coupled receptors and the P2, a family of at least 12 receptors responsive to purine (ATP, ADP) and pyrimidine (UTP) nucleotides through which adenosine and ATP can function as extracellular messengers. (springer.com)
  • Several cell membrane receptors, which preferentially bind extracellular nucleotides, and their analogs have been identified. (acris-antibodies.com)
  • Purinergic receptors are a family of ubiquitous transmembrane receptors comprising of two main classes: those stimulated by adenosine are classified as P1 receptors and those that respond to extracellular nucleotides (i.e. (acris-antibodies.com)
  • The nucleoside adenosine and nucleotides including adenine mononucleotides like ADP and ATP and dinucleotides such as P1,P4-diadenosine tetraphosphate (Ap4A), and P1,P5-diadenosine pentaphosphate (Ap5A) are present in different ocular locations and therefore they may contribute/modulate inflammatory processes. (ucm.es)
  • In summary, adenosine and nucleotides can activate receptors in ocular structures susceptible to suffer from inflammatory processes. (ucm.es)
  • The control of the levels of extracellular nucleotides adenine and adenosine and the consequent signaling by purinergic receptors induced by them is critical in maintaining the physiological processes [5]. (thefreelibrary.com)
  • The release of endogenous nucleotides represents a critical first step for the initiation of purinergic signaling. (physiology.org)
  • P2X receptors are ligand-gated ion channels, whereas the P1 and P2Y receptors are G protein-coupled receptors. (wikipedia.org)
  • The actions of extracellular ATP are a result of stimulation of P2-type purinergic receptors, which are categorized into ligand-gated ion channels (P2X 1-7 ) or metabotropic heptahelical G protein-coupled receptors (P2Y 1,2,4,6,11-14 ) ( 12 ). (pnas.org)
  • P2Y - G protein coupled receptors. (anaesthetist.com)
  • P2 receptors are activated by ATP or ADP, and can be either ionotropic, in which case they are called P2X, or G-protein-coupled, called P2Y. (alzforum.org)
  • Update and subclassification of the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapy. (springer.com)
  • A G protein-coupled receptor for UDP-glucose. (springer.com)
  • but these techniques are difficult to apply to low-density G protein-coupled receptors such as adenosine receptors. (aspetjournals.org)
  • P2X-receptors are ligand-gated ion channels, whereas P2Yreceptors belong to the superfamily of G-protein-coupled receptors (GPCR). (acris-antibodies.com)
  • Fig.1: Schematic view of a G-Protein coupled P2Y receptor and an 'ionotropic' P2X receptor. (acris-antibodies.com)
  • Uridine 5'-diphosphate induces intracellular Ca(2+) responses and oscillations in HeLa cells, due to the activation of P2Ys (G-protein coupled ATP receptors). (hmdb.ca)
  • The metabolic degradation of ATP to adenosine (ADO) provides an array of purinergic signaling molecules that can interact with a large population of cell surface receptors that include the ATP-sensitive ionotropic P2X and metabotropic P2Y receptor superfamilies, as well as the P1 ADO-sensitive G-protein-coupled receptors. (cognizantcommunication.com)
  • The present understanding of opioid pharmacology has been influenced by discoveries relating to the mechanisms that operate on G-protein-coupled receptor (GPCR) signaling. (cognizantcommunication.com)
  • Advances in the pharmacology of purinergic neurotransmission has led to the development of new strategies to enhance the endogenous actions of ADO and to limit the neuroexcitatory effects of ATP. (cognizantcommunication.com)
  • Inhibitors of purinergic receptors include clopidogrel, prasugrel and ticlopidine, as well as ticagrelor. (wikipedia.org)
  • Using specific inhibitors for each purinergic receptor subtype, Delekate found that blocking P2Y1 returned astrocyte signaling to normal in the APPPS1 mice. (alzforum.org)
  • Comprehensive examination of adenosine receptor-knockout mice exposed to AKI demonstrated that renal protection by ENT inhibitors involves the A2B adenosine receptor. (elsevier.com)
  • The clinical efficacy of epidermal growth factor receptor (EGFR) kinase inhibitors in EGFR-mutant non-small-cell lung cancer (NSCLC) is limited by the development of drug-resistance mutations, including the gatekeeper T790M mutation. (ebscohost.com)
  • There is increasing evidence of purinergic signalling in regulating cochlear response to injury. (auckland.ac.nz)
  • On the other hand, adenosine receptor signalling is known to increase cellular antioxidant responses and this could be the main mechanism underlying protection from neomycin-induced hair cell death. (auckland.ac.nz)
  • Based on these studies, it was postulated that ATP and adenosine regulate different aspects of the cochlear response to stress and injury, and that the balance of P1 and P2 receptor signalling is important for cochlear survival under stress. (auckland.ac.nz)
  • The purinergic signalling system consists of transporters, enzymes and receptors responsible for the synthesis, release, action, and extracellular inactivation of (primarily) ATP and its extracellular breakdown product adenosine. (wikipedia.org)
  • Cell signalling events initiated by P1 and P2Y receptors have opposing effects in biological systems. (wikipedia.org)
  • The regulation of vascular tone in the endothelium of blood vessels is mediated by purinergic signalling. (wikipedia.org)
  • Within the field of purinergic signalling, these receptors have been implicated in learning and memory, locomotor and feeding behavior, and sleep. (wikipedia.org)
  • Purinergic signalling is involved in several processes including neurologic, endocrine, and immune system signalling. (wikipathways.org)
  • Purinergic signalling is involved in control of cerebral vascular tone and remodelling. (eurekaselect.com)
  • There is both short-term purinergic signalling in transmission and secretion and long-term (trophic) signalling in controlling cell proliferation, differentiation, motility and death in development and regeneration and there is increasing interest in the roles of purines and pyrimidines in pathophysiological conditions and their therapeutic potential in disease. (springer.com)
  • At the molecular level, rapid progress has been made in understanding the mechanisms of nucleotide and nucleoside release, their extracellular metabolism, the intracellular signalling cascades elicited by receptor activation and the cross-talk with other essential signalling pathways. (springer.com)
  • The rapidly growing interest in purinergic signalling with its exceptionally wide spectrum of signalling functions in health and disease makes this journal devoted to purinergic signalling attractive to both basic scientists and clinicians. (springer.com)
  • Purinergic P2X and P2Y receptors are involved in mediating intercellular signalling via purines such as adenosine triphosphate (ATP). (pubmedcentralcanada.ca)
  • Evidence exists for a role of purinergic signalling in intercellular coupling within SCN. (pubmedcentralcanada.ca)
  • 2001 ). Purinergic signalling has been implicated in brain development (Oliveira et al. (pubmedcentralcanada.ca)
  • For example these receptors play a significant role in regulating ion transport in epithelial tissues through a variety of intracellular signalling pathways. (acris-antibodies.com)
  • Going from 2 basic families to 19 different receptor types has allowed researchers to get much more specific about the potential of purines to influence our health, and dozens of studies are underway to determine exactly how "purinergic signalling" serves to impact our blood flow, heart function, inflammatory responses, experience of pain, digestive function, and absorption of nutrients. (whfoods.com)
  • Using meta-analysis across case-control and family trio (affected child and parental controls) studies of severe malaria from The Gambia and Malawi, we sought evidence of association in six Gs pathway candidate genes: adenosine receptor 2A (ADORA2A) and 2B (ADORA2B), beta-adrenergic receptor kinase 1 (ADRBK1), adenylyl cyclase 9 (ADCY9), G protein beta subunit 3 (GNB3), and regulator of G protein signalling 2 (RGS2). (edu.au)
  • Both adenosine-sensitive P1 and nucleotide-sensitive P2 receptors are extensively distributed in the sensory and supporting cells of the mammalian cochlea, where they regulate various physiological processes and homeostatic response to stress, such as environmental noise. (auckland.ac.nz)
  • In addition, ectonucleotidases generate extracellular adenosine, which abrogates nucleotide-mediated effects and activates adenosine receptors, often with opposing (patho-) physiological effects. (wikipedia.org)
  • Taken together, these results demonstrate the involvement of different purinergic receptors and signaling in GC, and the pattern of expression changes in tumoral cells, and this change likely directs ATP and nucleotide signaling from antiproliferative effects in healthy tissues to proliferative effects in cancer. (frontiersin.org)
  • 4) The functional investigation of single nucleotide polymorphisms in purinergic receptors/enzymes associated with altered susceptibility to inflammatory disorders or infection. (frontiersin.org)
  • In this study, we show that extracellular ATP, through the activation of P2Y 4 receptors, stimulates TSP-1 expression and release in astrocytes and that this nucleotide-induced increase is mediated by protein kinase signaling pathways. (pnas.org)
  • There is a widespread presence of both adenosine (P1) and P2 nucleotide receptors in the brain on both neurones and glial cells. (eurekaselect.com)
  • Loss of mouse P2Y6 nucleotide receptor is associated with physiological macrocardia and amplified pathological cardiac hypertrophy. (springer.com)
  • Cloning and functional expression of a human uridine nucleotide receptor. (springer.com)
  • Effect of loss of P2Y 2 receptor gene expression on nucleotide regulation of murine epithelial Cl − transport. (springer.com)
  • These receptors are collectively known as nucleotide receptors or "purinergic" receptors. (acris-antibodies.com)
  • The receptor plays a crucial role in platelet aggregation and mediates the adenine nucleotide- induced release of NO. P2Y2 transcripts are abundantly distributed. (acris-antibodies.com)
  • It is therefore the activity of this ecto-nucleotide cascade that determines whether P2 or P1 receptors are preferentially activated. (physiology.org)
  • Recent research has identified a role for microglial P2X receptors in neuropathic pain and inflammatory pain, especially the P2X4 and P2X7 receptors. (wikipedia.org)
  • RT-PCR showed the presence of P2X2 and P2X4 receptor transcripts on E14 cardiomyocytes with a lower expression of P2X3 and P2X7 receptors. (springer.com)
  • suggesting a differentiation-dependent regulation of p2x7 receptor expression. (aspetjournals.org)
  • In addition, activation of the P2X7 receptor, present on immune cells, triggers membrane permeabilization to medium-sized molecules and thereby may permit the cellular exit of ATP ( 28 ). (physiology.org)
  • Furthermore, we showed that A1, A2A, P2Y1, P2Y11, and P2X7 purine receptor agonists modulated the TGF-β1-induced EMT through the involvement of PKA and/or MAPK/ERK signaling. (unich.it)
  • Differently, P2X7 receptor induced, per se, similar and not additive effects compared to TGF-β1, after prolonged cell exposure to BzATP. (unich.it)
  • Burnstock G (1978) A basis for distinguishing two types of purinergic receptor. (springer.com)
  • Burnstock G. A basis for distinguishing two types of purinergic receptor. (springer.com)
  • These results strongly imply that the secreted ATP-utilizing enzymes of V. cholerae modulate the external ATP levels of the macrophage and mast cells, leading to their accelerated death, presumably through activation of P2Z receptors. (asm.org)
  • The Impact of Purinergic System Enzymes on Noncommunicable, Neurological, and Degenerative Diseases. (thefreelibrary.com)
  • This study explored the role of endogenously formed adenosine in modulating NF-κB activity and cytokine/chemokine release from murine Treg and effector T cells (Teff) including key enzymes/purinergic receptors of extracellular ATP catabolism. (physiology.org)
  • Stimulation of the adenosine receptor could potentially lead to a decrease in inflammation and tissue damage. (clinicaltrials.gov)
  • 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)
  • In recent years, there has been increased interest in the roles of purinergic receptors as key mediators of inflammation and immunity following the reception of damage-associated ATP release. (frontiersin.org)
  • The purpose of this collection is therefore to compile key advances in the understanding of purinergic signaling within inflammation and immunity and generate a comprehensive resource for all purinergic researchers and immunologists alike. (frontiersin.org)
  • In this Research Topic, we aim to bring together researchers investigating all aspects of purinergic signaling (P1, P2Y, P2X, CD39, and CD73) and produce a comprehensive overview of the recent developments concerning purinergic signaling within infection and inflammation. (frontiersin.org)
  • It is now recognized that purinergic signaling not only regulates neurotransmission and inflammation, but also influences diverse biological pathways, such as cell survival, proliferation, differentiation, lipid synthesis, and cell motility. (hindawi.com)
  • Is a receptor for leukotriene B4, a potent chemoattractant involved in inflammation and immumne response. (acris-antibodies.com)
  • Adenosine receptors, in particular adenosine receptors, present anti-inflammatory action in acute and chronic retinal inflammation. (ucm.es)
  • Mechanisms of disease: Purinergic signaling during inflammation. (asahq.org)
  • There are many instances in which signaling events through adenosine P1 versus adenosine triphosphate receptors of the P2 type have opposing effects in biological systems, and shifting the balance between purinergic signaling seems to be an important therapeutic concept in dampening inflammation and promoting healing. (asahq.org)
  • The contribution of ectonucleotidases in the modulation of purinergic signaling depends on the availability and preference of substrates and on cell and tissue distribution. (wikipedia.org)
  • Ectonucleotidases modulate P2 purinergic signaling, and P1 receptors. (wikipedia.org)
  • Purinergic receptors (P1, P2Y, and P2X) and ectonucleotidases (CD39 and CD73) have been widely implicated in health and disease. (frontiersin.org)
  • As highlighted by P. Chernogorova and R. Zeiser, these studies suggest potential clinical use of recombinant ectonucleotidases or adenosine receptor agonists for regulation of alloimmune responses which can be tailored according to the clinical situation. (hindawi.com)
  • Although extracellular ATP enhances immune cell chemotaxis and activation through engagement with P2 purinergic receptors, it is rapidly degraded to adenosine by ectonucleotidases. (aacrjournals.org)
  • While early studies focused on the role of purinergic receptors in neurotransmission, it soon became obvious that extracellular ATP and its hydrolyzed derivative adenosine had important roles in immune regulation. (hindawi.com)
  • Thus, full characterisation of the role of adenosine in tumor development, by addressing the question of whether adenosine receptors are present in cancer tissues, and, if so, which receptor subtype mediates its effects in cancer growth, is a vital research goal. (nih.gov)
  • To this end, this review focuses on the most relevant aspects of adenosine receptor subtype activation in tumors reported so far. (nih.gov)
  • however, the precise role of each LPA receptor subtype has not yet been fully characterized. (aspetjournals.org)
  • Molecular cloning and expression of the cDNA for a novel A2-adenosine receptor subtype. (umassmed.edu)
  • While ATP primarily acts as a proinflammatory signal on purinergic P2 receptors, its degradation product adenosine signals through P1 purinergic receptors, mediating both anti- and proinflammatory effects depending on the receptor subtype. (physiology.org)
  • There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. (wikipedia.org)
  • The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP. (umassmed.edu)
  • CONCLUSIONS AND IMPLICATIONS: The cytoprotection elicited by adenosine and inosine in a model of renal ischaemia involved both interactions with cell surface adenosine receptors on renal tubular epithelial cells and intracellular metabolism and conversion of adenosine to ATP. (biomedsearch.com)
  • The effects on chloride transport are mediated via P2Y2 receptors, which activates inositol phospholipid hyrolysis and calcium metabolism. (anaesthetist.com)
  • In 1978, Burnstock proposed two types of purinergic receptors: P1 receptors selective for adenosine and P2 receptors selective for ATP and ADP. (hindawi.com)
  • The future of pharmacologic stress: selective A2A adenosine receptor agonists. (wikipathways.org)
  • The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. (wikipathways.org)
  • Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. (umassmed.edu)
  • Regarding the A3 receptor, selective agonists like N6-(3-iodobenzyl)-5′-N-methylcarboxamidoadenosine (CF101) have been used for the treatment of inflammatory ophthalmic diseases such as dry eye and uveoretinitis. (ucm.es)
  • 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)
  • In 1985, a pharmacological approach was proposed to distinguish between two types of P2 receptors: ionotropic P2X and metabotropic P2Y receptors [ 3 ]. (hindawi.com)
  • She first confirmed that the astrocytes were hyperactive, then tested whether these star-shaped cells were simply responding to neuronal activity by blocking either neuronal transmission or the astrocyte metabotropic glutamate receptors that sense it. (alzforum.org)
  • The function of the AMPA and NMDA receptors is associated with long-term potentiation, LTP, which is caused by the stimulation of protein kinases by Ca 2+ ions, and long-term depression, LTD, which results from the low influx of Ca 2+ ions and the activation of phosphatases. (scirp.org)
  • The results showed that neither the stimulation nor the blockade of adenosine A2A receptors modified the progressive loss of motor skills or survival of mSOD1G93A mice. (elsevier.com)
  • On murine T lymphocytes the A2aR is highly expressed ( 20 ), and after T-cell receptor (TCR) stimulation, A2aR mRNA levels increase by a factor of ∼10 ( 16 ). (physiology.org)
  • The stimulation of A2A receptor reduced the overexpression of the EMT-related markers, mainly through the cAMP-dependent PKA pathway, as confirmed by cell pre-treatment with Myr-PKI. (unich.it)
  • Both A1 and P2Y1 receptor stimulation exacerbated the TGF-β1-driven effects, which were reduced by cell pre-treatment with the MAPK inhibitor PD98059, according to the increased ERK1/2 phosphorylation upon receptor activation. (unich.it)
  • The relative potencies of agonists for the A2B adenosine receptor could only be tested by measurement of receptor-stimulated adenylyl cyclase activity. (biomedsearch.com)
  • Cloning of a human purinergic P2Y receptor coupled to phospholipase C and adenylyl cyclase. (springer.com)
  • The present two-part volume represents an integrated compendium of invited chapters by leading researchers in the area focusing on advances in the understanding of purinergic and pyrimidinergic signaling systems, their role(s) in tissue function and pathophysiology and advances in developing potential new medications based on the modulation of P1 and P2 receptor signaling processes. (springer.com)
  • Thus, serosal afferents (putative nociceptors) were used to investigate the effect of tegaserod, and transient receptor potential channel, vanilloid 4 (TRPV 4 ) modulation on mechanical responses. (bmj.com)
  • May be the cardiac P2Y receptor involved in the regulation of cardiac muscle contraction through modulation of L-type calcium currents. (acris-antibodies.com)
  • Our data confirm that the modulation of adenosine receptors can elicit very different (and even opposite) effects during the progression of ALS course, thus strengthens the importance of further studies to elucidated their real therapeutic potential in this pathology. (elsevier.com)
  • P2X receptors are activated by ATP, leading to the opening of K + , Na + and Ca 2+ permeable channels and subsequently to increased intracellular Ca 2+ . (pubmedcentralcanada.ca)
  • adenosine) receptors, as well as relax vascular smooth muscles through the reduction in calcium uptake by inhibition of slow inward calcium current and activation of adenylate cyclase in smooth muscle cells. (rcsb.org)
  • characterization of stably transfected receptors in CHO cells. (biomedsearch.com)
  • The CHO cells with stably transfected adenosine receptors provide an identical cellular background for such a pharmacological characterization. (biomedsearch.com)
  • It involves the activation of purinergic receptors in the cell and/or in nearby cells, thereby regulating cellular functions. (wikipedia.org)
  • These receptors are greatly distributed in neurons and glial cells throughout the central and peripheral nervous systems. (wikipedia.org)
  • In GC-derived cells, we detected the expression of several purinergic receptors, and found important differences as compared to GES-1 cells. (frontiersin.org)
  • ATP binds to the P2Y receptor on the pulmonary endothelial cells, activating the nitric oxide system. (anaesthetist.com)
  • Here, we emphasize the two-way communication that goes on between these cells, beginning with how neurons can modulate microglial state and activity, for example, by specific chemokine, classic neurotransmitters, and purinergic signaling. (hindawi.com)
  • In particular, ATP can affect the functions of B cells, T cells, macrophages, and eosinophils ( 7 , 8 , 9 ) via activation of plasma membrane receptors known as P2 purinoceptors ( 10 , 11 , 12 ). (jimmunol.org)
  • Although T cells express inhibitory adenosine A 2A receptors (A 2A R) that suppress their activation and inhibit immune killing of tumors, a role for myeloid cell A 2A Rs in suppressing the immune response to tumors has yet to be investigated. (aacrjournals.org)
  • Depletion of CD8 + T cells or NK cells in tumor-bearing mice indicates that both cell types initially contribute to slowing melanoma growth in mice lacking myeloid A 2A receptors, but tumor suppression mediated by CD8 + T cells is more persistent. (aacrjournals.org)
  • The results indicate that tumor-associated myeloid cells, including macrophages, DCs, and MDSCs all express immunosuppressive A 2A Rs that are potential targets of adenosine receptor blockers to enhance immune killing of tumors. (aacrjournals.org)
  • 2016 ). ATP and its metabolites are co-transmitters in the brain and P2 receptors are abundantly present in the brain on both neurons and glial cells (Burnstock 2013 ). (pubmedcentralcanada.ca)
  • Biver G, Wang N, Gartland A, Orriss I, Arnett TR, Boeynaems JM, Robaye B. Role of the P2Y 13 Receptor in the differentiation of bone marrow stromal cells into osteoblasts and adipocytes. (springer.com)
  • periodate-oxidized-ATP (oATP)-treated macrophage and mast cells or such cells exposed to 0.1 mM Mg 2+ , where surface-associated P2Z receptors could not be activated, were not susceptible to subsequent ATP addition. (asm.org)
  • in the presence of millimolar concentrations of external ATP effluxed from the macrophages or other mammalian cells ( 1 , 7 , 9 , 25 ), the surface-associated P2Z receptors of macrophages and other phagocytic or inflammatory cells are activated, thereby altering the permeability of the plasma membrane. (asm.org)
  • Patterns of A2A Extracellular Adenosine Receptor Expression in Different Functional Subsets of Human Peripheral T Cells. (aspetjournals.org)
  • as the functionally predominant purinergic receptors on murine T cells. (aspetjournals.org)
  • Information about the lymphocyte subset-specific expression of adenosine receptors would be useful, but it has been difficult to obtain sufficient quantities of cells to analyze expression of Ado receptors in biochemical or radioligand binding assays, particularly in the minor subpopulations of lymphocytes. (aspetjournals.org)
  • Purinergic receptors were identified by RT-PCR and quantitative RT-PCR from mRNA isolated from primary and immortalized cells grown to confluence on membrane filters. (umn.edu)
  • RT-PCR experiments also revealed expression of A 2b adenosine receptor mRNA in primary and immortalized cells. (umn.edu)
  • With the cells overexpressing LPA 1 , LPA 2 , or LPA 3 , we examined the selectivity and mode of inhibition by Ki16425 against the LPA-induced actions and compared them with those of dioctyl glycerol pyrophosphate (DGPP 8:0), a recently identified antagonist for LPA receptors. (aspetjournals.org)
  • Ki16425 inhibited LPA-induced guanosine 5′- O -(3-thio)triphosphate binding as well as LPA receptor binding to membrane fractions with a same pharmacological specificity as in intact cells. (aspetjournals.org)
  • Activation of these receptors is partially dependent on ATP (or UTP) release from cells, often in the setting of cellular damage. (acris-antibodies.com)
  • Thanks to extensive research on the role of purines in the health of our cardiovascular system and digestive system (including our mouth, stomach, and intestines), we now know that purines have their own special receptor system on our cells that allow them to connect up with the cell membranes and have far-reaching effects. (whfoods.com)
  • Treatment of stimulated CD4 + T-cells with adenosine (25 μM) potently reduced IFN-γ release which is mediated by adenosine A2a receptors (A2aR). (physiology.org)
  • The test could accurately measure levels of epidermal growth factor receptor on three types of oral cancer cells. (ebscohost.com)
  • Background: In an attempt to identify markers of resistance to trastuzumab, we evaluated both the profiling of human epidermal growth factor receptor 2 (HER2)-positive tumor cells measuring the relative levels of EGFR, pMAPK, pAkt and PTEN and their correlations with clinical outcome in. (ebscohost.com)
  • Malignant ascites from pancreatic cancer patients has been reported to stimulate migration of pancreatic cancer cells through lysophosphatidic acid (LPA) and LPA1 receptors. (ebscohost.com)
  • Association of constitutively activated hepatocyte growth factor receptor (Met) with resistance to a dual EGFR/Her2 inhibitor in non-small-cell lung cancer cells. (ebscohost.com)
  • Urokinase receptor primes cells to proliferate in response to epidermal growth factor. (ebscohost.com)
  • We report that murine embryonic fibroblasts (MEFs) proliferate in response to EGF only when these cells express the urokinase receptor (uPAR). (ebscohost.com)
  • Remodeling of Purinergic Receptor-Mediated Ca2+ Signaling as a Consequence of EGF-Induced Epithelial- Mesenchymal Transition in Breast Cancer Cells. (ebscohost.com)
  • Adenosine acts through an A3 receptor to prevent the induction of murine anti-CD3-activated killer T cells. (nih.gov)
  • AK-T cells express mRNA coding for A(2A), A(2B) and A(3) receptors, but little or no mRNA coding for A(1) receptors. (nih.gov)
  • The nucleoside adenosine is also a key signaling molecule that modulates multiple physiological processes through interaction with cell-surface P1 purinergic receptors. (springer.com)
  • Cannabinoid agonists, which act at the cannabinoid 1 (CB 1 ) receptor and cannabinoid 2 (CB 2 ) receptor, have a number of physiological effects and considerable therapeutic potential, in particular as analgesics. (cognizantcommunication.com)
  • Intracellularly, ATP is stored at very high levels (from 5 to 10mmol/l), which can quickly be degraded by ubiquitous extracellular nucleotidases after connecting to specific receptors under physiological conditions. (thefreelibrary.com)
  • Platelet-derived growth factor stimulated synthesis of TSP in a human glial cell line ( 28 ) and transforming growth factor-β1 induced TSP-1 mRNA in astrocytes ( 29 ), but the potential role of extracellular ATP and P2 receptor signaling in TSP-1 expression and release in astrocytes has not been investigated. (pnas.org)
  • P2X1 and a low level of P2X5 receptor messenger RNA (mRNA) were also expressed at E18. (springer.com)
  • We measured the myocyte size, the area of interstitial fibrosis, SR Ca 2+ -ATPase, and ryanodine receptor mRNA abundance. (elsevier.com)
  • There were no significant differences in ryanodine receptor mRNA levels among the three groups. (elsevier.com)
  • Purinergic receptors, also known as purinoceptors, are a family of plasma membrane molecules that are found in almost all mammalian tissues. (wikipedia.org)
  • Examples of the roles of purinoceptors in neuropathology involve: A2A receptors in Parkinsons disease and epilepsy, P2 receptors in trauma, ischaemia, neuroinflammatory and neuropsychiatric disorders, and neuropathic pain. (eurekaselect.com)
  • [4] [5] For example, NTPDase1 hydrolyzes P2 receptor ligands, namely ATP , ADP , UTP and UDP with similar efficacy. (wikidoc.org)
  • The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. (elsevier.com)
  • Geoffrey Burnstock, Bertil B. Fredholm and Alexei Verkhratsky, " Adenosine and ATP Receptors in the Brain", Current Topics in Medicinal Chemistry (2011) 11: 973. (eurekaselect.com)
  • In 1970, Geoffrey Burnstock described the release of extracellular adenosine triphosphate (ATP) as a transmitter substance by nonadrenergic inhibitory nerves, and later in 1972, he formulated the hypothesis of purinergic neurotransmission [ 1 ]. (hindawi.com)
  • In these studies of Burnstock and colleagues, the use of the term P2-purinergic was introduced to designate the putative receptor(s) for ATP and to distinguish them from so-called P1-purinergic receptors for adenosine. (cdc.gov)
  • Although, only in 1970, Burnstock proposed the term "purinergic" and presented his hypothesis about ATP as an independent neurotransmitter released from nonadrenergic noncholinergic neurons in the intestines, bladder, and gut [11, 12]. (thefreelibrary.com)
  • Using an in vitro model of CNS trauma that stimulates release of ATP, we found that TSP-1 expression increased after mechanical strain and was completely blocked by a P2 receptor antagonist and by inhibition of p38/mitogen-activated protein kinase and Akt, thereby indicating a major role for P2 receptor/protein kinase signaling in TSP-1 expression induced by trauma. (pnas.org)
  • The effects induced by P2Y11 receptor activation were oppositely modulated by PKA or MAPK inhibition, in line with the dual nature of the Gs- and Gq-coupled receptor. (unich.it)
  • In the presence of GTP all receptors were converted to a single low affinity state indicating functional coupling to endogenous G proteins. (biomedsearch.com)
  • Expressed by neurons and astroglia, the A2A receptor couples to Gs proteins that raise the levels of the second messenger cAMP in the cytosol. (alzforum.org)
  • Macrophages express membrane proteins that function as receptors for PtdSer (e.g. (elifesciences.org)
  • The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. (acris-antibodies.com)
  • P2Y14 is a receptor for UDP-glucose and other UDP-sugar coupled to G-proteins. (acris-antibodies.com)
  • Abstract  Members of the epidermal growth factor receptor (EGFR) family of proteins are frequently overactive in solid tumors. (ebscohost.com)
  • Abstract -Renin secretion can be stimulated by ATP via purinergic P2Y receptors. (ahajournals.org)
  • While exogenous ATP can be rapidly catabolized to adenosine by a number of ectophosphohydrolases, many of the observed actions of extracellular ATP can be distinguished from those triggered by occupation of the well characterized A1- and A2-receptors for extracellular adenosine. (cdc.gov)
  • These ligand-gated ion channels are nonselective cation channels responsible for mediating excitatory postsynaptic responses, similar to nicotinic and ionotropic glutamate receptors. (wikipedia.org)
  • 1) The roles of purinergic signaling in the regulation of innate and adaptive immune responses. (frontiersin.org)
  • The responsiveness of embryonic cardiomyocytes (E) 12 to P2 receptor agonists by measuring Ca 2+ influx did not present response to ATP, but responses to P2 agonists were detected in cardiomyocytes taken from E14 and E18 rats. (springer.com)
  • Interestingly, recent evidence suggests that purinergic signaling influences the severity of alloimmune responses. (hindawi.com)
  • Contractile responses of the sphincter to EFS were unaffected by the muscarinic receptor antagonist atropine (1 µM), but were almost completely abolished by the adrenergic neuron blocker guanethidine (10 µM). (edu.au)
  • Ki16425 inhibited several responses specific to LPA, depending on the cell types, without any appreciable effect on the responses to other related lipid receptor agonists, including sphingosine 1-phosphate. (aspetjournals.org)
  • Therefore, purinergic responses in the perivascular retinal tissue during relaxation of VSMCs were studied. (arvojournals.org)
  • 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)
  • Only in 2006, ATP was finally recognized as a cotransmitter in both the peripheral and central nervous systems (CNS) [9, 10, 14], and the purinergic signaling was recognized as a system involved in many nonneuronal and neuronal mechanisms [12]. (thefreelibrary.com)
  • The Pannexin-1 channel (PANX1) is an integral component of the P2X/P2Y purinergic signaling pathway and the key contributor to pathophysiological ATP release. (wikipedia.org)
  • Furthermore, we found that the protective role of ATP is mediated by the P2 purinergic receptor signaling pathway. (jneurosci.org)
  • In this article, we report that purinergic signaling participates in the production and secretion of TSP-1. (pnas.org)
  • 6 ATP stimulates renin secretion from rat renal cortical slices, the relative response to ATP analogues being in accord with a P2Y, rather than a P1, purinergic effect. (ahajournals.org)
  • Macrophage production and secretion of these homeostatic factors are controlled by endogenous purinergic signals. (diabetesjournals.org)
  • The proteinase also changes the function of receptors, and consequently, the secretion of neurotransmitter/neuromodulator from the presynaptic glutamatergic and/or purinergic elements are either strengthened or weakened. (scirp.org)
  • Extracellular purines, particularly adenosine-5'-tri-phosphate (ATP) and adenosine are potent regulators of many cellular and tissue processes through pathways activated by action on the P1 and P2 receptors. (auckland.ac.nz)
  • We conclude that TSP-1 expression can be regulated by activation of P2Y receptors, particularly P2Y 4 , coupled to protein kinase signaling pathways and suggest that purinergic signaling may be an important factor in TSP-1-mediated cell-matrix and cell-cell interactions such as those occurring during development and repair. (pnas.org)
  • Therefore, a complete understanding of purinergic system could potentially unveil possible markers or relevant pathways for pathological processes, mainly related to human degeneration. (thefreelibrary.com)
  • To understand the role of A 2A Rs in the regulation of immune response, we investigated the expression levels of this receptor in different functional lymphocyte subsets. (aspetjournals.org)
  • 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)
  • P1 and P2Y receptors are known to be widely distributed in the brain, heart, kidneys, and adipose tissue. (wikipedia.org)
  • Purinergic receptors have been suggested to play a role in the treatment of cytotoxic edema and brain infarctions. (wikipedia.org)
  • Neuroglia involved in homeostasis, melanin synthesis and defense of the brain contain different combinations of purinergic receptors, which contributes to many neurotransmitters. (scirp.org)
  • This review summarizes a concept of brain plasticity, the role of ATP and P2 receptors interaction with glutamatergic system during plasticity of the brain in the one hand and after physical exercise in the other, which may be triggering phenomena facilitative synaptic plasticity as well as potentiates an personal efficiency to react to biobehavioral adaptation and disorders. (scirp.org)
  • In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416. (wikipathways.org)
  • Molecular cloning and characterization of a rat A1-adenosine receptor that is widely expressed in brain and spinal cord. (umassmed.edu)
  • The distribution of the P2Y6-receptor is widespread including heart, blood vessels and brain. (acris-antibodies.com)
  • 3) The deleterious or protective roles of purinergic signaling during pathogenic challenge. (frontiersin.org)
  • A. Battastini and colleagues present an overview of the various roles of purinergic signaling in gliomas. (hindawi.com)
  • We also found that exogenous ATP protected Aβ42-mediated reduction in synaptic molecules, such as NMDA receptor 2A and PSD-95, through P2 purinergic receptors and prevented Aβ42-induced spine reduction in cultured primary hippocampal neurons. (jneurosci.org)
  • Adenosine receptors play a major role in presynaptic neuromodulation, while P2X receptors are involved in fast synaptic transmission and synaptic plasticity. (eurekaselect.com)
  • The adenosine receptor is known for its anti-inflammatory actions and could therefore be a potential target in the treatment of sepsis and septic shock. (clinicaltrials.gov)
  • Antagonism of the adenosine receptor by caffeine leads to an increased LPS-induced inflammatory reaction and an increase in (subclinical) tissue damage? (clinicaltrials.gov)
  • 2) The contribution of purinergic signaling to the pathophysiology of inflammatory disorders. (frontiersin.org)
  • In gliomas, the presence of an inflammatory infiltrate is directly correlated with tumor malignancy, and this appears to be regulated in part by purinergic signaling. (hindawi.com)
  • The importance of peripheral CB 2 receptors, however, in mediating cannabinoid-induced antinociception, in particular in models of inflammatory pain, has recently been demonstrated. (cognizantcommunication.com)
  • In this review article from the New England Journal of Medicine , Dr. Eltzschig from the Department of Anesthesiology at the University of Colorado-together with Drs. Sitkovsky and Robson from Harvard Medical School-discuss the therapeutic functions of purinergic signaling during inflammatory diseases. (asahq.org)
  • In this work, we studied in detail purinergic signaling in the gastric adenocarcinoma-derived cell lines: AGS, MKN-45, and MKN-74, and compared them to a nontumoral epithelial cell line: GES-1. (frontiersin.org)
  • The notion of xanthine-insensitivity of the A3 receptor should be dropped at least for the human receptor as xanthines with submicromolar affinity were found. (biomedsearch.com)
  • Xanthines (e.g. caffeine) specifically block adenosine receptors, and are known to induce a stimulating effect to one's behavior. (wikipedia.org)
  • A nucleotidase inhibitor and A2a adenosine receptor antagonist inhibited the apoptotic supernatant-induced gene expression, suggesting AMP was metabolized to adenosine by an ecto-5'-nucleotidase expressed on macrophages, to activate the macrophage A2a adenosine receptor. (elifesciences.org)
  • Neurons can regulate microglial activation state through the unique ligand-receptor pairs (CX3CL1-CX3CR1 and CD200-CD200R), microRNA-124 (mir-124), neurotransmitters (glutamate and GABA), and purinergic signaling. (hindawi.com)
  • In: Straub RW, Bolis L (eds) Cell membrane receptors for drugs and hormones: a multidisciplinary approach. (springer.com)
  • Purinergic receptors sit on the plasma membrane and are activated by ATP or its breakdown products ADP, AMP, and adenosine. (alzforum.org)
  • Cell membrane receptors for drugs and hormones: a multidisciplinary approach. (springer.com)
  • We are particularly interested in further uncovering these roles and highlighting the importance of purinergic signaling within pathophysiological processes. (frontiersin.org)
  • Elements of the purinergic signaling system are involved in many processes in health and disease conditions [3]. (thefreelibrary.com)