Interleukin 1 Receptor Antagonist Protein: A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.Sialoglycoproteins: Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.Adenosine: 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.Receptors, Interleukin-1: Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.Interleukin-1: A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Receptor, Adenosine A1: 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.Adenosine Deaminase: An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.Receptor, Adenosine A3: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Receptor, Adenosine A2B: A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Adenosine Kinase: An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC 2.7.1.20.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Receptors, Adenosine A2: A subclass of ADENOSINE RECEPTORS that are generally considered to be coupled to the GS, STIMULATORY G-PROTEIN which causes up regulation of CYCLIC AMP.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Receptors, Purinergic P1: 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).Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Xanthines: Purine bases found in body tissues and fluids and in some plants.Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Receptors, Purinergic: 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.Rats, Sprague-Dawley: 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.Theophylline: A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.2-Chloroadenosine: 2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.Phenylisopropyladenosine: N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Piperidines: A family of hexahydropyridines.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.5'-Nucleotidase: 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.Inosine: A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.Serotonin 5-HT1 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.Cells, Cultured: 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.Serotonin 5-HT2 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Tubercidin: An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.Histamine H2 Antagonists: Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.Adenosine Triphosphatases: A group of enzymes which catalyze the hydrolysis of ATP. The hydrolysis reaction is usually coupled with another function such as transporting Ca(2+) across a membrane. These enzymes may be dependent on Ca(2+), Mg(2+), anions, H+, or DNA.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Theobromine: 3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9)Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Adenine NucleotidesNarcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.Kinetics: The rate dynamics in chemical or physical systems.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).Calcium: 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.Triazines: Heterocyclic rings containing three nitrogen atoms, commonly in 1,2,4 or 1,3,5 or 2,4,6 formats. Some are used as HERBICIDES.Receptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.Signal Transduction: 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.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.Benzazepines: Compounds with BENZENE fused to AZEPINES.Hormone Antagonists: Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.Time Factors: Elements of limited time intervals, contributing to particular results or situations.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Histamine Antagonists: Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.Serotonin: A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.Histamine Agonists: Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Muscarinic Antagonists: Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.TriazolesReceptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Nucleoside Deaminases: Catalyze the hydrolysis of nucleosides with the elimination of ammonia.Receptors, Purinergic P2: 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.Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)Histamine H1 Antagonists: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Mice, Inbred C57BLGABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.Neurons: 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.Purines: 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.Coformycin: A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.PyrrolidinesReceptors, N-Methyl-D-Aspartate: A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.Indoles: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.Vasodilator Agents: Drugs used to cause dilation of the blood vessels.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Serotonin 5-HT1 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.PiperazinesDrug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Behavior, Animal: The observable response an animal makes to any situation.Pyrazoles: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.Baclofen: A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Disease Models, Animal: Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Synaptic Transmission: 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.Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Rabbits: The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.Protein Binding: The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.Sulfonamides: A group of compounds that contain the structure SO2NH2.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Dogs: The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)Histamine: An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.Adenine: A purine base and a fundamental unit of ADENINE NUCLEOTIDES.Adenosine Phosphosulfate: 5'-Adenylic acid, monoanhydride with sulfuric acid. The initial compound formed by the action of ATP sulfurylase on sulfate ions after sulfate uptake. Synonyms: adenosine sulfatophosphate; APS.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Substance P: An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... 1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ...
... which is a competitive antagonist of this protein. As with the A1, the A2A receptors are believed to play a role in regulating ... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... "Entrez Gene: ADORA2A adenosine A2A receptor". Ohta A, Sitkovsky M (2001). "Role of G-protein-coupled adenosine receptors in ... 3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists". Journal of Medicinal Chemistry. 46 (7 ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... 3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists". Journal of Medicinal Chemistry 46 (7 ... 1989). "Selective amplification and cloning of four new members of the G protein-coupled receptor family.". Science 244 (4904 ... 1992). "Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature.". Eur. J. ...
CysLTR2, similar to CysLTR1, is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ... "G-protein-coupled receptors and asthma endophenotypes: the cysteinyl leukotriene system in perspective". Molecular Diagnosis & ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... protein binding. • G-protein coupled peptide receptor activity ...
All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor ... ligands). DP (D2). DP1. *Agonists: Prostaglandin D2. *Treprostinil. *Antagonists: Asapiprant ... Thromboxane A2 receptor. TP. TXA=PGH2,,PGD2=PGE2=PGF2α=PGI2[14]. contractile. Gq alpha subunit. stimulates PLC & IP3; raises Ca ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... G protein-coupled receptor. Class A. *Eicosanoid receptor ( ...
G protein-coupled receptors (GPCRs) such as DP2 are integral membrane proteins that, when bound by their cognate ligands (or, ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... prostaglandin D receptor activity. • G-protein coupled receptor ... G-protein coupled receptor signaling pathway. • adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway. • G- ...
G-protein coupled receptor activity. • prostaglandin receptor activity. • signal transducer activity. • prostaglandin E ... ligands). DP (D2). DP1. *Agonists: Prostaglandin D2. *Treprostinil. *Antagonists: Asapiprant ... "Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. * ...
... designated A1, A2A, A2B and A3 are currently known. In this study all human subtypes were stably transfected into Chinese ... Four adenosine receptor subtypes of the family of G protein-coupled receptors, ... Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently ... 8997606 - Repeated treatment with adenosine a1 receptor agonist and antagonist modifies the antic.... 9584206 - Differential ...
... providing Axon Ligands™ for pharmaceutical research as world-wide recognized drug standards ... All four members are coupled to a G-protein (A1 and A3 subtypes to Gi, and A2 subtypes to Gs (GPCR-A18)). As a result, ... Adenosine A1 and A2A agonist €65.00 1423 KW 6002 Adenosine A2A antagonist €85.00 ... Adenosine receptor subtypes listed: A1, A2A, A3. [1] InternationalUnion of Basic and Clinical Pharmacology. LXXXI. Nomenclature ...
... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... 1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ...
... which is a competitive antagonist of this protein. As with the A1, the A2A receptors are believed to play a role in regulating ... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... "Entrez Gene: ADORA2A adenosine A2A receptor". Ohta A, Sitkovsky M (2001). "Role of G-protein-coupled adenosine receptors in ... 3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists". Journal of Medicinal Chemistry. 46 (7 ...
... designated A1, A3, A2a, and A2b (19). All adenosine receptors are G protein-coupled receptors; however, only the A2aR and A2bR ... cells were exposed to the A2bR-specific agonist BAY 60-6583 and the A2-type adenosine receptor selective agonist NECA. TNF-α ... 3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem. Pharmacol. 61: 657-663. ... It is interesting that we observed increased A2br levels in macrophages exposed to TLR ligands or in response to exogenous ...
Although adenosine activates multiple receptor subtypes (A1, A2a, A2b, and A3 receptors), the adenylyl cyclase stimulatory A2a ... based on experiments involving application of an A2-type adenosine receptor ligand, 5′-N-ethylcarboxamidoadenosine and A2bAR ... CXCR4 is the only G protein-coupled seven-transmembrane receptor of stromal cell-derived factor 1. CXCR4 is expressed on the ... an in vivo model of smooth muscle cell proliferation revealed that an A2 receptor agonist, 2-octynyladenosine, inhibited ...
... multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors ... A known adenosine receptor (AR) agonist was conjugated to polyamidoamine (PAMAM) dendrimer carriers for delivery of the intact ... This ligand tool can now be used in pharmacological models of tissue rescue from ischemia and to probe the existence of A3 AR ... Attachment of neutral amide-linked chains or thiourea-containing chains preserved the moderate affinity and efficacy at the A1 ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... 3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists". Journal of Medicinal Chemistry 46 (7 ... 1989). "Selective amplification and cloning of four new members of the G protein-coupled receptor family.". Science 244 (4904 ... 1992). "Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature.". Eur. J. ...
... adenosine, melatonin, ghrelin, galanin, apelin, prokineticin and cannabidiol. We hope to provoke further drug development ... Since G protein coupled receptors (GPCRs) are target of forty percent of clinically used drugs, here we discuss the newly ... Since G protein coupled receptors (GPCRs) are target of forty percent of clinically used drugs, here we discuss the newly ... Discovery and cardioprotective effects of the first non-Peptide agonists of the G protein-coupled prokineticin receptor-1. PLoS ...
However, recent evidence showed that many other receptors, such as G protein-coupled receptors and ligand-gated ion channels, ... induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X ... However, recent evidence showed that many other receptors, such as G protein-coupled receptors and ligand-gated ion channels, ... induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X ...
NECA binding by ligands selective for the Gi-coupled A1 or A3 adenosine receptors or for the Gs-coupled A2A adenosine receptor ... Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists. Can J Physiol Pharmacol 58: 673-691, ... N-ethyl-carboxamido-adenosine ([3H]NECA)-specific binding by adenosine receptor ligands. Membranes (0.5 mg protein/ml) from ... N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor. J Med Chem ...
... renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors ... Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. Am J ... Jacobson KA (1998) Adenosine A3 receptors: novel ligands and paradoxical effects. Trends Pharmocol Sci 19:184-191CrossRefGoogle ... an adenosine A1 receptor antagonist, is mediated by cyclic adenosine monophosphate. Am J Kidney Dis 26:825-830PubMedCrossRef ...
1996). "Phosphorylation of human m1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 and protein ... Ligands. No highly selective agonists or antagonists for the M5 receptor have been discovered as of 2018, but several non- ... Agonists. *Milameline ((E)-1,2,5,6-Tetrahydro-1-methyl-3-pyridinecarboxaldehyde-O-methyloxime, CAS# 139886-32-1) ... Coupling to inhibition of adenylyl cyclase and stimulation of phospholipase A2". J. Biol. Chem. 271 (29): 17476-84. doi:10.1074 ...
Pascoe SJ, Knight H, Woessner R (2007) QAF805, an a2b/A3 adenosine receptor antagonist, does not attenuate AMP challenge in ... The capacity of adenosine to potently regulate inflammation has made the G-protein- coupled adenosine receptors attractive ... Identification of A2a adenosine receptor domains involved in selective coupling to Gs. Analysis of chimeric A1/A2a adenosine ... 2000) Adenosine and selective A(2A) receptor agonists reduce ischemia/reperfusion injury of rat liver mainly by inhibiting ...
... thromboxane/prostanoid receptor; ADP, adenosine diphosphate; GPGR, G-protein-coupled-receptor; 5HT, 5-hydroxytryptamine. Agent ... 53.Vilahur G, Casaní L, Badimon L (2007) A thromboxane A2/prostaglandin H2 receptor antagonist (S18886) shows high ... an important platelet agonist in vivo, has two types of membrane receptors named P2Y1 and P2Y12 [27]. P2Y1 is a Gq linked 7- ... Int J Genomic Med ISSN: 2332-0672 IJGM, an open access journal AJW200 is a humanized monoclonal antibody (mAb) against vWF A1 ...
CysLTR2, similar to CysLTR1, is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ... "G-protein-coupled receptors and asthma endophenotypes: the cysteinyl leukotriene system in perspective". Molecular Diagnosis & ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... protein binding. • G-protein coupled peptide receptor activity ...
All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor ... ligands). DP (D2). DP1. *Agonists: Prostaglandin D2. *Treprostinil. *Antagonists: Asapiprant ... Thromboxane A2 receptor. TP. TXA=PGH2,,PGD2=PGE2=PGF2α=PGI2[14]. contractile. Gq alpha subunit. stimulates PLC & IP3; raises Ca ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... G protein-coupled receptor. Class A. *Eicosanoid receptor ( ...
... ) Routes of administration IntravenousATC codeC01EB10 (WHO)Legal statusLegal statusIn general: ℞ (Prescription only) ... Rapidly cleared from circulation via cellular uptakeProtein binding NoMetabolism Rapidly converted to inosine and adenosine ... Adenosine receptor All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor ... muscarinic antagonist: Atropine Disopyramide Quinidine muscarinic agonist: Digoxin. α receptors. Amiodarone Bretylium Quinidine ...
... thromboxane/prostanoid receptor; ADP, adenosine diphosphate; GPGR, G-protein-coupled-receptor; 5HT, 5-hydroxytryptamine. ... Adenosine diphosphate (ADP), an important platelet agonist in vivo, has two types of membrane receptors named P2Y1 and P2Y12 [ ... Vilahur G, Casaní L, Badimon L (2007) A thromboxane A2/prostaglandin H2 receptor antagonist (S18886) shows high antithrombotic ... ARC1779 (Archemix Corp) is a novel aptamer-based chemical antibody that binds to vWF A1 domain with high affinity and little ...
... methodology to other G protein-coupled receptors could provide a general procedure for analyzing G protein-coupled receptors ... PBMCs were incubated with Ado receptor agonists and antagonist, and measurements were made after 30, 60, and 120 min as ... 1996) Adenosine receptor ligands: Differences with acute versus chronic treatment. Trends Pharmacol Sci 17:108-113. ... 1997) Inosine binds to A3 adenosine receptors and stimulates mast cell degranulation. J Clin Invest 100:2849-2857. ...
Adenosine receptors adenosine A1 adenosine A2A adenosine A2B adenosine A3 Adrenergic receptors noradrenaline α1A-adrenoceptor ... 0176] Red antagonist of the dopamine D2 receptor: Ligand of the Dopamine D2 receptor (Spiperone derivative), coupled to a red ... agonist of the MC3 and MC4 receptors), MIP1alpha (inflammatory protein of macrophages=CCL3, agonist of CCR1 and CCR5), RANTES ... receptors R1 and R2 with FRET acceptor compounds A1 and A2 and the ligand with a donor D1, which corresponds to the format ...
1 of 4 transmembrane G protein-coupled cell-surface adenosine receptors (ARs)-A1, A2A, A2B, and A3 Here, we studied the role of ... MCF-7 cells were used to treat with agonist and antagonist of estrogen and then the mRNA expression of adenosine receptor ... Structure-Based Design of Potent and Selective Ligands at the Four Adenosine Receptors. ... A2-biosensor-evidence-for-an-allosteric-mechanism-of-action-for-the-a-2b-selective-antagonist-psb-603 ...
36 The adenosine A1 receptor is coupled to a Gαi/o protein and the A2a and A2b receptors are coupled to GαS (fig 1). Ligation ... Extracellular adenosine can bind to the seven transmembrane-spanning adenosine surface receptors types A1, A2α, A2β, A3, which ... through adenosine increase and binding to A3 receptors, might promote the IL1 receptor antagonist (IL1ra) transcription and ... 1998) An agonist of adenosine A3 receptors decreases interleukin-12 and interferon-gamma production and prevents lethality in ...
... adenosine A3 receptor agonist) Can-Fite Pharma Waltham, MA rheumatoid arthritis (see also glaucoma) Phase II www.canfite.com ... G protein-coupled receptor 40 agonist) Akros Pharma Princeton, NJ type 2 diabetes Phase II www.akrospharma.com KD026 (MTP ... glucagon receptor antagonist) Ligand Pharmaceuticals La Jolla, CA type 2 diabetes Phase I www.ligand.com LIK066 (SGLT 1/2 ... When that pro- tein interacts with LDL receptors, it promotes degradation of the receptor, ultimately, interfering with the ...
Adenosine receptor A1 (A1). X. X. ADORA3. Adenosine receptor A3 (A3). X. X. ... Purinergic receptor P2Y, G-protein coupled, 11 (P2Y11). X. P2RY2. Purinergic receptor P2Y, G-protein coupled, 2 (P2Y2). X. X. X ... control ligand = control compound (100% activity). % Inhibition. (Antagonist mode) =. 100% x. [. 1- Mean RLU (test sample)- ... To enable a graphic representation and agonist comparison, data was normalized to the reference agonist, [Met5]-Enkephalin in ...
  • 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)
  • A series of novel, potent and selective human ß(2) adrenoceptor agonists incorporating a hydantoin or a uracil ring on the right-hand side phenyl ring of (R)-salmeterol is presented. (bvsalud.org)
  • Baranowski RL, Westenfelder C (1994) Estimation of renal interstitial adenosine and purine metabolites by microdialysis. (springer.com)
  • the purine nucleoside adenosine is involved in many physiological and pathophysiological events ( 35 ). (physiology.org)
  • This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. (wikipedia.org)
  • A number of secreted, transmembrane, and phospho-inositide (PI)-linked proteins from the semaphorin, slit, ephrin, and netrin families are thought to act as axonal guidance cues ( Tessier-Lavigne and Goodman, 1996 ). (jneurosci.org)
  • Seven transmembrane receptors are divided into classic and atypical families. (aspetjournals.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)
  • It was originally thought that almost all allergic events were mediated directly only via the high-affinity immunoglobulin E receptors. (frontiersin.org)
  • No highly selective agonists or antagonists for the M 5 receptor have been discovered as of 2018, but several non-selective muscarinic agonists and antagonists have significant affinity for M 5 . (wikidoc.org)
  • Antiplatelet drugs Agents Targeting vWF Introduction ARC1779 (Archemix Corp) is a novel aptamer-based chemical antibody that binds to vWF A1 domain with high affinity and little immunogenicity [9, (spotidoc.com)
  • At sites of vascular injury, GPVI-collagen interactions initiate intracellular signaling pathway followed by shifting of integrins to high-affinity state and the release of secondarily acting agonists (ie, ADP, serotonin, and calcium), as well as synthesizing thromboxane from arachidonic acid (AA). (spotidoc.com)
  • Typically, prostanoid receptors show somewhat less affinity and responsiveness to the 1 and 3 series prostanoids. (wikipedia.org)
  • In the present paper, a PLD cDNA clone was isolated from tobacco, expressed as a GST fusion in bacteria, and the recombinant protein was purified by glutathione affinity. (embl-heidelberg.de)
  • In this study, we investigated the effect of IFN-γ on TLR-activated macrophages, and we reveal that IFN-γ sustains inflammatory macrophage activation by attenuating their sensitivity to extracellular adenosine. (jimmunol.org)
  • Adenosine receptors also play a major role in several inflammation-associated processes by inhibiting immune activation and preventing excessive tissue damage. (pnas.org)
  • In recent years, it has been realized that purinergic signaling, induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X receptors, plays a significant role in mast cell degranulation. (frontiersin.org)
  • Adenosine 5′-triphosphate (ATP, compound 3 in Figure 1 ) is abundant in mast cells, stored in granules and secreted upon activation. (frontiersin.org)
  • The primary stimulatory processes are considered to be of histaminergic nature via G s -coupled H 2 receptor activation and of cholinergic nature via activation of G q -coupled muscarinic receptors or receptors for gastrin ( 69 ), but other actors are also on the stage. (physiology.org)
  • Adenosine-dependent regulation of renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors (A 1 AR, A 2A AR, A 2B AR, A 3 AR). (springer.com)
  • Moreover, adenosine protects against renal ischemic reperfusion injury by the anti-inflammatory effect of enhancing the activity of regulatory T cell and by attenuating the inflammatory injury produced by neutrophils via A 2 AR activation. (springer.com)
  • Al-Mashhadi RH, Skott O, Vanhoutte PM et al (2009) Activation of A(2) adenosine receptors dilates cortical efferent arterioles in mouse. (springer.com)
  • Awad AS, Huang L, Ye H et al (2006) Adenosine A2A receptor activation attenuates inflammation and injury in diabetic nephropathy. (springer.com)
  • Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
  • 1994). "Signaling through transforming G protein-coupled receptors in NIH 3T3 cells involves c-Raf activation. (wikidoc.org)
  • Platelet activation is subsequently propagated through agonist-receptor interaction, mostly including ADP via P2Y1/P2Y12, thrombin via protease-activated receptor 1(PAR1) and PAR4, and thromboxane via the thromboxane receptor (TP). (spotidoc.com)
  • These pathological conditions can be associated with disturbance in the signaling mediated by nucleotides and nucleosides of adenine, in expression or activity of extracellular ectonucleotidases and in activation of P2X and P2Y receptors. (hindawi.com)
  • Nucleotides and nucleosides act as potent extracellular messengers via the activation of the family of cell-surface receptors termed purinergic receptors. (biomedcentral.com)
  • However, genetic deletion of CD73 in mice is associated with a proinflammatory phenotype and CD73-derived adenosine appears to be quantitatively sufficient to inhibit platelet activation, and leukocyte adhesion to the vascular endothelium in vivo ( 15 ) by acting through the A2aR ( 47 ). (physiology.org)
  • Aside from its action on the endothelium, A2aR agonists inhibit T-cell activation through increasing cAMP levels, which acts immunosuppressive ( 39 ). (physiology.org)
  • Launch Chronic inflammatory discomfort and neuropathic discomfort share a number of common neuroplastic adjustments taking place in the spinal-cord, including changed ion channel appearance in dorsal main ganglion neurons, improved glutamate discharge and glutamate receptor function, aswell as glial cell activation . (immune-source.com)
  • The current antiplatelet drugs used in daily clinical practice include COX-1 inhibitor aspirin, ADP P2Y12 receptor antagonist clopidogrel, and the GPIIb-IIIa antagonists (abciximab, eptifibatide and tirofiban). (spotidoc.com)
  • CD73-derived adenosine acts as potent inhibitor of inflammation, and regulatory T cells (Treg) have been shown to express CD73 as a novel marker. (physiology.org)
  • 1. A method of enhancing an immune response in a host, comprising administering to the host an A.sub.2a receptor antagonist in combination or alternation with a checkpoint inhibitor. (patents.com)
  • Muscarinic receptors mediate many of the effects of acetylcholine in the central and peripheral nervous system. (wikidoc.org)
  • 2014). "Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)-Selective M5 -Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe" . (wikidoc.org)
  • It has been shown that M 1 -Muscarinic receptors cooperate with D 5 receptors and beta-2 adrenergic receptors to consolidate cued fear memory. (wikidoc.org)
  • One exception to this rule is the receptor for thromboxane A2 (TP) which binds and responds to PGH2 and TXA2 equally well. (wikipedia.org)
  • Maps are thromboxane A2, which is on the free switching and traffic theory for integrated broadband networks 1990's numerous essay insights on the Table moderator( perhaps the continuous ' fuel ' impairment), and those of Navient challenges. (elconsultorweb.com)
  • There is indirect evidence for a second PGI2 receptor in BEAS-2B human airway epithelial cells but this finding has not been collaborated and the putative receptor has not been otherwise defined. (wikipedia.org)
  • Just as in A1 receptors, this normally serves as a protective mechanism, but may be destructive in altered cardiac function. (wikipedia.org)
  • Thus, the generation of adenosine by macrophages is an important mechanism that prevents overactive inflammatory responses. (jimmunol.org)
  • Discover novel ligands with unique attributes, determine mechanism of action or uncover potential side effect profiles of novel drug candidates. (discoverx.com)
  • Three recent reports have examined the relationship between the level of extracellular ATP, the mechanisms underlying purinergic receptors participating in the infection mechanism of HIV-1 in the cell. (biomedcentral.com)
  • It has been disclosed that certain naturally occurring macromolecules including the HIV-1 protein Tat enter cells through an active transport mechanism. (justia.com)
  • Downregulation of P2X7 and upregulation of CD73 in Treg after antigenic stimulation may be an important mechanism to maintain the ability of Treg to generate immunosuppressive adenosine. (physiology.org)
  • However the development of more highly selective A2A ligands has led towards other applications, with the most significant focus of research currently being the potential therapeutic role for A2A antagonists in the treatment of Parkinson's disease. (wikipedia.org)
  • They are named based on the prostanoid to which they preferentially bind and respond, e.g. the receptor responsive to PGI2 at lower concentrations than any other prostanoid is named the Prostacyclin receptor (IP). (wikipedia.org)
  • Prostanoid receptors bind and respond principally to metabolites of the straight chain polyunsaturated fatty acid (PUFA), arachidonic acid . (wikipedia.org)
  • In general, receptors for the series 2 prostanoids also bind with and respond to the series 1 and 3 prostanoids. (wikipedia.org)
  • It is therefore the activity of this ecto-nucleotide cascade that determines whether P2 or P1 receptors are preferentially activated. (physiology.org)
  • Beach RE, Watts BA 3rd, Good DW et al (1991) Effects of graded oxygen tension on adenosine release by renal medullary and thick ascending limb suspensions. (springer.com)
  • After TLR stimulation, macrophages alter their metabolism and release low levels of ATP, which is rapidly converted into immunosuppressive adenosine via CD39-mediated hydrolysis. (jimmunol.org)
  • 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)
  • For A2A adenosine receptors CGS 21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadeno sine) and N-ethylcarboxamidoadenosine (NECA) were found to be the most potent agonists followed by R- and S-PIA with minor stereoselectivity. (biomedsearch.com)
  • NECA was the most potent agonist with an EC50-value of 2.3 microM whereas all other compounds tested were active at concentrations in the high micromolar range. (biomedsearch.com)
  • The A3 receptor was characterized utilizing the nonselective agonist [3H]NECA. (biomedsearch.com)
  • We explored Gi, Gq/11 and Gs coupling in 1321 N1 astrocytoma, HEK293, and T24 bladder cancer cells endogenously expressing human A2B AR, using NECA or nonnucleoside BAY60-6583 as agonist, selective Gi, Gs and Gq/11 blockers, and CRISPR/Cas9-based Gq- and Gs-null HEK293 cells. (readbyqxmd.com)
  • The A2b adenosine receptor (A2bAR) is highly abundant in bone marrow macrophages and vascular smooth muscle cells (VSMC). (pnas.org)
  • These results provide a first indication for a direct regulation of PLDalpha by a heterotrimeric G-protein alpha-subunit in plants. (embl-heidelberg.de)
  • Experimental evidence supports the notion that adenosine protects against ischemia-induced acute kidney injury by directly acting on renal endothelial and tubular A 1 AR. (springer.com)
  • In this role, A2AR functions similarly to programmed cell death-1 (PD-1) and cytotoxic t-lymphocyte associated protein-4 (CTLA-4) receptors, namely to suppress immunologic response and prevent associated tissue damage. (wikipedia.org)
  • In general, the A2-type receptors have been described as sensors of tissue damage during an immune response ( 2 ), and A2aARs have been described as having a nonredundant role in the attenuation of inflammation and tissue damage in vivo ( 3 ). (pnas.org)
  • These receptors display broad tissue distribution throughout the body and are involved in several biological events. (biomedcentral.com)
  • Adenosine can be formed from AMP either intracellularly by cytosolic 5′-nucleotidase usually involving tissue hypoxia or extracellularly by ecto-5′-nucleotidase (CD73). (physiology.org)
  • In addition, A2A receptor can negatively regulate overreactive immune cells, thereby protecting tissues from collateral inflammatory damage. (wikipedia.org)
  • Exposure of macrophages to TLR ligands initiates the production of inflammatory cytokines and mediators that can influence immune responses ( 1 ). (jimmunol.org)
  • However, recent evidence showed that many other receptors, such as G protein-coupled receptors and ligand-gated ion channels, are also directly involved in mast cell degranulation, the release of inflammatory mediators such as histamine, serine proteases, leukotrienes, heparin, and serotonin. (frontiersin.org)
  • We Bexarotene also discovered a decreased appearance of 5-HT2A receptors in the dorsal spinal-cord of inflamed pets which could not really end up being rescued by TAT-2ASCV shot, while the quantity of PSD-95 had not been suffering from inflammatory discomfort. (immune-source.com)
  • We hypothesized that having less efficiency of SSRIs in inflammatory persistent pain circumstances might reveal alteration of 5-HT2A receptor-operated signalling. (immune-source.com)