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.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.BH3 Interacting Domain Death Agonist Protein: A member of the Bcl-2 protein family that reversibly binds MEMBRANES. It is a pro-apoptotic protein that is activated by caspase cleavage.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.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 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.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).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 A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 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.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.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.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)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.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.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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.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.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Phenylisopropyladenosine: N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.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.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.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).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.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.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.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.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)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.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.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.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.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.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.Adenine NucleotidesReceptors, 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.Receptors, 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.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).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)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 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.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.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.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.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.Quinpirole: A dopamine D2/D3 receptor agonist.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.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.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.Nicotinic Agonists: Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.Piperidines: A family of hexahydropyridines.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Kinetics: The rate dynamics in chemical or physical systems.Nucleoside Deaminases: Catalyze the hydrolysis of nucleosides with the elimination of ammonia.Benzazepines: Compounds with BENZENE fused to AZEPINES.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)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.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.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.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.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.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.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.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.Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.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.Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.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.Vasodilator Agents: Drugs used to cause dilation of the blood vessels.PyrrolidinesTime Factors: Elements of limited time intervals, contributing to particular results or situations.Purinergic P2Y Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.Naphthalenes: Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.TriazolesPurinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Cholinergic Agonists: Drugs that bind to and activate cholinergic receptors.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.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.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.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.Mice, Inbred C57BLPurinergic Agonists: Compounds that bind to and activate PURINERGIC RECEPTORS.Thioinosine: Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503)Adenine: A purine base and a fundamental unit of ADENINE NUCLEOTIDES.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)Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.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 P2X Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.Receptors, Glucagon: Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Benzoxazines: OXAZINES with a fused BENZENE ring.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Receptor, Cannabinoid, CB2: A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.Behavior, Animal: The observable response an animal makes to any situation.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.PiperazinesPyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Venoms: Poisonous animal secretions forming fluid mixtures of many different enzymes, toxins, and other substances. These substances are produced in specialized glands and secreted through specialized delivery systems (nematocysts, spines, fangs, etc.) for disabling prey or predator.Serotonin 5-HT3 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.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.Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC 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.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.Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.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.Enkephalins: One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.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.Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.Tetrahydronaphthalenes: Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.Receptors, GABA-B: A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.Norepinephrine: Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.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)MorpholinesMethylhistamines: Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.Nucleoside Transport Proteins: Proteins involved in the transport of NUCLEOSIDES across cellular membranes.Deoxyadenosines: Adenosine molecules which can be substituted in any position, but are lacking one hydroxyl group in the ribose part of the molecule.Receptor, Serotonin, 5-HT1B: A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Receptors, Serotonin, 5-HT4: A subtype of G-protein-coupled SEROTONIN receptors that preferentially couple to GS STIMULATORY G-PROTEINS resulting in increased intracellular CYCLIC AMP. Several isoforms of the receptor exist due to ALTERNATIVE SPLICING of its mRNA.Receptors, Prostaglandin E: Cell surface receptors which bind prostaglandins with a high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin E receptors prefer prostaglandin E2 to other endogenous prostaglandins. They are subdivided into EP1, EP2, and EP3 types based on their effects and their pharmacology.Benzeneacetamides: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.Receptors, sigma: A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.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.Muscle, Smooth: 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)Uridine Triphosphate: Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.Mice, Knockout: 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.Receptors, Metabotropic Glutamate: Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.Myocardium: The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.Receptors, Drug: Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.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.Receptors, Histamine: Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.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.Cyclic AMP-Dependent Protein Kinases: A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.Thionucleotides: Nucleotides in which the base moiety is substituted with one or more sulfur atoms.Receptor, Serotonin, 5-HT1A: A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.Bicyclo CompoundsRats, Inbred Strains: Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.Membrane Potentials: 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).Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Vasodilation: The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.Receptor, Serotonin, 5-HT2A: A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.Patch-Clamp Techniques: An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.Receptors, Histamine H3: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)NorbornanesStructure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Extracellular Space: 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.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.Microdialysis: A technique for measuring extracellular concentrations of substances in tissues, usually in vivo, by means of a small probe equipped with a semipermeable membrane. Substances may also be introduced into the extracellular space through the membrane.Bucladesine: A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)Apyrase: 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.Enzyme Activation: Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.Pertussis Toxin: One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.Corpus Striatum: Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Receptor, Serotonin, 5-HT2C: A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.Bicyclo Compounds, Heterocyclic: A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)Nucleotidases: A class of enzymes that catalyze the conversion of a nucleotide and water to a nucleoside and orthophosphate. EC 3.1.3.-.Impromidine: A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.Hippocampus: A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.Receptors, Histamine H2: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Hypoxanthine: A purine and a reaction intermediate in the metabolism of adenosine and in the formation of nucleic acids by the salvage pathway.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Dopamine Agents: Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.Imidazoles: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).Electrophysiology: The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.Coronary Circulation: The circulation of blood through the CORONARY VESSELS of the HEART.8-Bromo Cyclic Adenosine Monophosphate: A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
AdenosineAll adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... "Anti-Inflammatory Preconditioning by Agonists of Adenosine A1 Receptor". PLoS ONE. 3 (5): e2107. Bibcode:2008PLoSO...3.2107N. ... Adenosine is an endogenous agonist of the ghrelin/growth hormone secretagogue receptor. However, while it is able to increase ...
... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. In a mouse model of ... 1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ...
... 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 ... Development of potent and selective human A3 adenosine receptor agonists". Nucleic Acids Symposium Series (2004). 49 (49): 31-2 ...
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... "Entrez Gene: ADORA2A adenosine A2A receptor". Ohta A, Sitkovsky M (2001). "Role of G-protein-coupled adenosine receptors in ... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... Makujina SR, Sabouni MH, Bhatia S, Douglas FL, Mustafa SJ (Oct 1992). "Vasodilatory effects of adenosine A2 receptor agonists ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... 1992). "Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature.". Eur. J. ... a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". Eur. J. Pharmacol. 213 ... 3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists". Journal of Medicinal Chemistry 46 (7 ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... protein binding. • G-protein coupled peptide receptor activity. • signal transducer activity. • G-protein coupled receptor ... discovery of a subtype selective agonist". Mol. Pharmacol. 58 (6): 1601-8. PMID 11093801.. ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... G-protein coupled receptor signaling pathway. Sources:Amigo / ...
prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ... TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... a selective agonist for PGE2 receptor subtype 3". Journal of Leukocyte Biology. 68 (2): 187-93. PMID 10947062.. ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... "Prostanoid Receptors: EP3". IUPHAR Database of Receptors and ...
... thromboxane A2. The cyclopentenone prostaglandins, PGJ2, Δ12-PGJ2, and 15-d-Δ12,14-PGJ2 are spontaneously formed or protein- ... is a full agonist of chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2) in human eosinophils and ... 11beta-PGF2 and its stereoisomer PGF2alpha are novel agonists of the chemoattractant receptor, CRTH2". FEBS Letters. 580 (2): ... Adenosine (A1. *A2A. *A2B. *A3). *P2Y (1. *2. *4. *5. *6. *8 ... prostaglandin D receptor activity. • G-protein coupled receptor ...
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 ...
Adenosine monophosphate deaminase deficiency type 1, also called myoadenylate deaminase deficiency (MADD), is a recessive genetic metabolic disorder that affects ...
The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G ...
The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This protein is a member of the G ...
5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR) is an intermediate in the generation of inosine monophosphate. AICAR is an analog of adenosine ...
Diprophylline (INN) or dyphylline (USAN) (trade names Dilor, Lufyllin), is a xanthine derivative with bronchodilator and vasodilator effects. It is used in the treatment of respiratory disorders like asthma, ...
Adenosine diphosphate (or ADP) is the chemical that plants make ATP from, during photosynthesis. A chemical compound that can be converted to ATP with the addition of one phosphate group. ...
The pre-Bötzinger complex (preBötC) is a cluster of interneurons in the ventral respiratory centre of the medulla of the brainstem. This complex has been proven to be essential for the generation of respiratory rhythm in mammals. The exact mechanism of the rhythm generation ...
Dipyridamole (trademarked as Persantine and others) is a medication that inhibits blood clot formation when given chronically and causes blood vessel dilation when given at high doses over a short time. ...
Bevan N, Butchers PR, Cousins R, Coates J, Edgar EV, Morrison V, Sheehan MJ, Reeves J, Wilson DJ (2007). „Pharmacological characterisation and inhibitory effects of ...
The ATP molecule is very versatile, meaning that it can be used for many things. Energy is stored in its chemical bonds. When ATP binds with another phosphate, energy is stored that can be used later. In other words, when a bond is made, energy is stored. ...
Greenberg B, Thomas I, Banish D, Goldman S, Havranek E, Massie BM, Zhu Y, Ticho B, Abraham WT (August 2007). "Effects of multiple oral doses of an A1 adenosine antagonist, BG9928, in ...
Johnson, M., Kaye, M.A.G., Hems, R. and Krebs, H.A. (1953). „Enzymic hydrolysis of adenosine phosphates by cobra venom". Biochem. J. 54: 625-629. PMID 13058963 ...
All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... "Anti-Inflammatory Preconditioning by Agonists of Adenosine A1 Receptor". PLoS ONE. 3 (5): e2107. Bibcode:2008PLoSO...3.2107N. ... Adenosine is an endogenous agonist of the ghrelin/growth hormone secretagogue receptor. However, while it is able to increase ...
WikiGenes - Adora2a - adenosine A2a receptorSpecies-dependent hemodynamic effects of adenosine A3-receptor agonists IB-MECA and Cl-IB-MECA. Lasley, R.D., Narayan, P., ... Adenosine receptor subtypes and vasodilatation in rat skeletal muscle during systemic hypoxia: a role for A1 receptors. Bryan, ... The adenosine A2A receptor-mediated facilitation was not changed by inhibitors of protein kinase A, protein kinase G or ... Activation of adenosine A2 receptors enhances high K(+)-evoked taurine release from rat hippocampus: a microdialysis study. ...
Protective effect of adenosine receptors against lipopolysaccharide-induced acute lung injury | Lung Cellular and Molecular...Adenosine A1 and A2 receptor agonists reduce endotoxin-induced cellular energy depletion and oedema formation in the lung. Eur ... Furthermore, adenosine prevents the degradation of A2A and A3 receptors on the protein level induced by LPS. Collectively, our ... Comparison of the potency of adenosine as an agonist at human adenosine receptors expressed in Chinese hamster ovary cells. ... LPS treatment significantly decreased transcription of A1 and A2B receptors but not A2A and A3 receptors (Fig. 7). Adenosine ...
The mechanism of pharmacological preconditioning of rat myocardium with beta-adrenergic agonists... the respective roles of the A1-, A2-, A3-adenosine receptors as well as the involvement of the PI3-K/PKB/Akt and ERKp44/p42 ... Harte is geprekondisioneer vir 5 min met isoproterenol 0.1 μM ( 1/ 2-AR agonist), of formoterol 1 nM ( 2-AR agonist) of BRL ... and 3-AR receptors as well as the contribution of Gi protein and PKA to -adrenergic preconditioning, (ii) the role of the ... The role of adenosine and the adenosine A1, A3, A2A and A2B receptors was studied by using adenosine deaminase and the ...
Contributions of Adenosine Receptor Activation to the Ocular Actions of Epinephrine | IOVS | ARVO JournalsImmunoprecipitation of A1 adenosine receptor-GTP-binding protein complexes in ciliary epithelial cells. Invest Ophthalmol Vis ... Molecular cloning and characterization of an adenosine receptor: the A3 adenosine receptor. Proc Natl Acad Sci USA. 1992;89: ... Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes. Mol Pharmacol. 1986;29:331-346. [ ... Crosson CE, Gray T. Modulation of intraocular pressure by adenosine agonists. J Ocul Pharmacol. 1994;10:379-383. [CrossRef] [ ...
... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. In a mouse model of ... 1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ...
... 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 ...
Adenosine A2A Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2A Receptor Antagonists (0) see Adenosine A2 ... Adenosine A1 Receptor Antagonists (3) • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. MeSH ... Adenosine A3 Receptor Antagonists (1). Adenosine Deaminase Inhibitors (8) • Drugs that inhibit ADENOSINE DEAMINASE activity. ... An alpha7 neuronal nicotinic receptor agonist. (1). Anabolic Agents (25) • These compounds stimulate anabolism and inhibit ...
Differential expression of adenosine A1 and A2 receptors in preadipocytes and adipocytes. ... N-[3-(R)-tetrahydrofuranyl]-6-aminopurine riboside, an A1 adenosine receptor agonist, antagonizes catecholamine-induced ... The increase in adenosine activates membrane receptors (AdoR) associated with protein G, which reduces the production of ... 46 It is thus believed that A1 receptor agonists may prove useful in managing the metabolic complications observed in obese ...
... 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 ... Development of potent and selective human A3 adenosine receptor agonists". Nucleic Acids Symposium Series (2004). 49 (49): 31-2 ...
IFN-γ Prevents Adenosine Receptor (A2bR) Upregulation To Sustain the Macrophage Activation Response | The Journal of Immunology... 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 ... B and D) Unprimed BMDMs (black bars) and IFN-γ-primed BMDMs (gray bars) were stimulated with the indicated TLR agonists for 4 h ... Extracellular adenosine can signal through four different adenosine receptors, designated A1, A3, A2a, and A2b (10). The ...
Renal Adenosine in Health and Disease | Springer for Research & Development... 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 ... Shneyvays V, Nawrath H, Jacobson KA et al (1998) Induction of apoptosis in cardiac myocytes by an A3 adenosine receptor agonist ... receptor blockade in normotensive and spontaneously hypertensive rats: role of pertussis toxin-sensitive G-proteins. J ...
![Full text] Current treatments for acute heart failure: focus on serelaxin | RRCC](data:image/png;base64,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)
Full text] Current treatments for acute heart failure: focus on serelaxin | RRCCe3.. 52.. Albrecht-Kupper BE, Leineweber K, Nell PG. Partial adenosine A1 receptor agonists for cardiovascular therapies. ... rolofylline has the lowest specificity for the A1 receptor, with 32-fold preference for the A1 receptor over the A2 receptor, ... 52 A phase II trial is currently underway to study the effect of a partial adenosine A1 agonist in chronic heart failure ( ... 97 One of the best characterized functions of relaxin is in remodeling of extracellular matrix proteins and protection from ...
The Adenosine Receptor and Serum Deprivation-Induced Neuronal DifferentiationCurrently, four subtypes of adenosine receptors are described, namely, the A1, A2A, A2B and A3 receptors. Neuroblastoma, mostly ... 059 and adenosine agonists did not show any further enhancement of differentiation. On the contrary, a selective protein kinase ... No additive or synergistic effects of 10 nM H-89 with either the A1 or A2A receptor agonist were seen. A selective mitogen- ... resembling human neuroblastoma cell lines and also expressing the A2 subtype of adenosine receptors, was shown not to ...
Adenosine... ) 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 ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ...
Frontiers | Targeting GPCRs Against Cardiotoxicity Induced by Anticancer Treatments | Cardiovascular Medicine... 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 ... 3-Aminoadenosine-5-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor. J Med Chem ...
Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates | Journal of Nanobiotechnology | Full...A known adenosine receptor (AR) agonist was conjugated to polyamidoamine (PAMAM) dendrimer carriers for delivery of the intact ... Attachment of neutral amide-linked chains or thiourea-containing chains preserved the moderate affinity and efficacy at the A1 ... multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors ... The A3 AR selective G2.5 dendrimer was also visualized binding the membrane of cells expressing the A3 receptor but did not ...
G-protein coupled adenosine receptor activity. • G-protein coupled receptor activity. • signal transducer activity. ... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ...
Gs-Coupled Adenosine Receptors Differentially Limit Antigen-Induced Mast Cell Activation | Journal of Pharmacology and...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 ... 2006) A3 adenosine receptor signaling contributes to airway mucin secretion after allergen challenge. Am J Respir Cell Mol Biol ... 2000) Adenosine and selective A(2A) receptor agonists reduce ischemia/reperfusion injury of rat liver mainly by inhibiting ...
4 B). Much weaker effects were obtained using compounds with somewhat nonselective A1 and A3 receptor agonist activity (Fig. 4 ... Adenosine exerts its effects by binding to adenosine type 1 purinergic G protein-coupled cell surface receptors, which are ... a panel of adenosine agonists with defined selectivity toward the full array of adenosine receptors was tested. The ... The danger sensors that STOP the immune response: the A2 adenosine receptors? Trends Immunol. 26:299-304. ...
A Three-Dimensional Collagen Gel Contraction Monitoring System that Uses A Porcine Trabecular Meshwork for Screening of Anti...The adenosine A2 agonist metrifudil caused inhibition at a concentration of 10-6 M (Figure 5A). The adenosine A3 agonist N6- (2 ... Adenosine reportedly affects IOP and ocular blood circulation. Adenosine agonists subtype A1 and A2a decreased IOP as result of ... and by adenosine A2 (metrifudil), and cannabinoid receptor (CP-55940) agonists. In addition, BIM I, simvastatin, BQ-123, and CP ... 2000) Protein kinase C isozymes and the regulation of diverse cell responses. Am J Physiol Lung Cell Mol Physiol 279: L429-438. ...
Four distinct subtypes of P1 receptors have been identified: adenosine A1, A2a, A2b, and A3 receptors (R) which are G protein ... Neutrophil adherence to endothelium is enhanced via adenosine A1 receptors and inhibited via adenosine A2 receptors. J Immunol ... A2a adenosine receptor agonist CGS21680 was 10 pM to 1 μM. ... A2aR agonists inhibit T-cell activation through increasing cAMP ... Inhibition of adenosine-mediated IFN-γ release is due to A2a adenosine receptor activation.. Among the specific adenosine ...
... induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X ... 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, ... However, recent evidence showed that many other receptors, such as G protein-coupled receptors and ligand-gated ion channels, ...
Muscarinic acetylcholine receptor M5 - wikidocAgonists. *Milameline ((E)-1,2,5,6-Tetrahydro-1-methyl-3-pyridinecarboxaldehyde-O-methyloxime, CAS# 139886-32-1) ... 1996). "Phosphorylation of human m1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 and protein ... "Muscarinic acetylcholine receptor subtypes as agonist-dependent oncogenes". Proc. Natl. Acad. Sci. U.S.A. 88 (11): 4703-7. doi: ... Coupling to inhibition of adenylyl cyclase and stimulation of phospholipase A2". J. Biol. Chem. 271 (29): 17476-84. doi:10.1074 ...
... a very selective agonist with high affinity for the human adenosine A1 receptor. J Med Chem 46: 1492-1503, 2003. ... The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia. J Biol Chem ... N-ethyl-carboxamido-adenosine ([3H]NECA)-specific binding by adenosine receptor ligands. Membranes (0.5 mg protein/ml) from ... Molecular cloning and characterization of the human A3 adenosine receptor. Proc Natl Acad Sci USA 90: 10365-10369, 1993. ...
AntagonistEffects of adenosineAntagonistsPurine nucleosidePurinergic receptorsPharmacologicalLigandsEndogenousSubtypeSubtypesCyclic adenosine monNECAExpression of adenosineEffect of adenosineSignal transductionInhibitionRole of adenosineLevels of adenosineMRNAPotent and selective humanStimulationBiochemicalModulationRadioligandInhibitGPCRsAffinityTransientFunctionalActivationNonselectiveLigand-gated ioAdenylateNucleoside adenosineAdenylyl cyclase activityIschemia-reperfusion injuryA2arCellularGeneDegradationMuscarinicPlateletMyocardialChemokine receptorsInflammationMiceIntracellularModulatesMembrane receptorsPharmacologyEffectorAdenozinski receptorInhibitorsDeaminaseProtects
- DPCPX (A1-AdoR antagonist) had no effect on the 1/ 2-PC-induced reduced infarct size or ERK p44/p42 and PKB activation. (sun.ac.za)
- MRS-1191 (A3-AdoR antagonist) blocked 1/ 2-PC when applied prior to index ischaemia or when added during early reperfusion, significantly inhibiting both ERK p44 and PKB activation. (sun.ac.za)
- Rabbits were pretreated topically with the moderately selective adenosine A 1 antagonist 8-(p-sulfophenyl)theophyline (8-SPT) or the adenosine A 2 antagonist 3,7-dimethyl-l-propargylxanthine (DMPX). (arvojournals.org)
- In competition with antagonist radioligand biphasic curves were observed for agonists. (biomedsearch.com)
- Aki Y, Tomohiro A, Nishiyama A et al (1997) Effects of KW-3902, a selective and potent adenosine A1 receptor antagonist, on renal hemodynamics and urine formation in anesthetized dogs. (springer.com)
- a ligand of M1 and M5, a ligand of M2 and M5, and a ligand of M3 and M5), but until both a selective agonist and a selective antagonist of the M5 receptor are developed this data must be considered merely theoretical. (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)
- The intradermal injection of the PAR-2 peptide agonist SLIGRL-NH2 (8-80nmol) caused a dose-dependent scratching that was unaffected by intraperitoneal pre-treatment with the histamine H1 antagonist pyrilamine (30mg/kg). (bvsalud.org)
- Structure of native agonists of the purinergic receptors, including both P2Rs (1-8) and ARs (9), and structures of agonist (10-20) and antagonist (21-37) ligands developed for the ARs, as described in the text. (frontiersin.org)
- 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)
- Numerous antihypertensive drugs are used to control hypertension including beta-blocking agents, angiotensin converting enzyme inhibitors (ACEI), angiotensin II receptor antagonists, diuretics, calcium antagonist and alpha-receptor blocking agents. (rroij.com)
- In order to uncover the estrogen effects on adenosine receptor expression, estrogen-positive MCF-7 cells were used to treat with agonist and antagonist of estrogen and then the mRNA expression of adenosine receptor subtypes were evaluated. (readbyqxmd.com)
- Estrogen-positive MCF-7 cells were treated with various concentrations of 17β estradiol (E2) as an estrogen agonist, and ICI 182,780 as an estrogen antagonist. (readbyqxmd.com)
- We also hypothesized that pretreating the comNTS with CTAP (d-Phe-Cys-Tyr-d-Trp-Arg-Thr-Pen-Thr-NH2), a μ-receptor antagonist, would largely diminish the systemic administration of DAMGO-induced HVR depression. (asahq.org)
- Tbe 2',3'-dideoxy analogue of the potent A\(_1\) receptor agonist, N\(^6\)-cyclohexyladenosine (CHA), was synthesized as a potential antagonist for the A\(_1\) adenosine receptor. (uni-wuerzburg.de)
- Competition of 2-alkynyladenosines 2a-d for the antagonist radioligand [\(^3\)H]DPCPX and for the agonist [\(^3\)H]CCPA gave K\(_i\) values in the nanomolar range, and the compounds showed moderate A\(_2\) selectivity. (uni-wuerzburg.de)
- Because of the effects of adenosine on AV node-dependent SVTs, adenosine is considered a class V antiarrhythmic agent. (wikipedia.org)
- Several studies have also suggested that the beneficial effects of adenosine occur through the effects of the A2AR and A2BR ( 7 , 22 , 27 , 43 ). (physiology.org)
- Thus, we propose a novel mechanism whereby IFN-γ contributes to host defense by desensitizing macrophages to the immunoregulatory effects of adenosine. (jimmunol.org)
- Effects of adenosine on tubular transport are most pronounced in the proximal tubule where the nucleoside stimulates NaCl reabsorption in the subnormal concentration range while inhibiting transport at elevated levels. (springer.com)
- Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. (springer.com)
- Beach RE, Good DW (1992) Effects of adenosine on ion transport in rat medullary thick ascending limb. (springer.com)
- The mechanism(s) of these confusing effects of adenosine on neuronal differentiation require examination. (edu.au)
- Regadenoson is an selective low-affinity (Ki= 1.3 µM) A2A receptor agonist that mimics the effects of adenosine in causing coronary vasodilatation and increasing myocardial blood flow. (drugbank.ca)
- The role of adenosine and the adenosine A1, A3, A2A and A2B receptors was studied by using adenosine deaminase and the selective antagonists DPCPX (1 μM), MRS 1191(1 μM), ZM241385 (1 μM) and MRS1754 (1 μM). (sun.ac.za)
- Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18). (wikipedia.org)
- These enhancing effects of agonists were blocked by selective antagonists, 8-cyclophenyl-1,3-dipropylxanthine (DPCPX) and 9-chloro-2-(2-furyl)[1,2,riazolo[1,5-c]quinalzolin-5-amine (CGS15943), respectively. (edu.au)
- 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)
- In addition, both acid production and radioligand binding of adenosine analogs to isolated cell membranes were potently blocked by selective A2BR antagonists, whereas ligands for A 1 , A 2A , and A 3 adenosine receptors failed to abolish activation. (physiology.org)
- This review provides an overview of the medicinal chemistry and therapeutic potential of various agonists/partial agonists, antagonists and allosteric modulators of A1 AR, with a particular emphasis on their current status and future perspectives in clinical settings. (eurekaselect.com)
- A1 adenosine receptors, A1 AR agonists, partial agonists, antagonists and allosteric modulators, pharmacology of A1 AR, structure- activity relationships of A1 AR. (eurekaselect.com)
- A1 adenosine receptor agonists, antagonists, and allosteric modulators. (eurekaselect.com)
- Therefore, we discussed in this review various receptors agonists, antagonists, activators and inhibitors which will have effects on cardiovascular system. (rroij.com)
- 6-9 Second, the HVR was abolished by microinjecting glutamate receptor antagonists into the comNTS, but the HVR was increased by injecting glutamate into this area. (asahq.org)
- In confirmation of this mechanism of action, recent studies in both animals and patients suggest that adenosine-receptor antagonists, among which is caffeine, reverse or prevent the anti-inflammatory effects of methotrexate. (biomedcentral.com)
- Adenosine is a purine nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond. (wikipedia.org)
- As a breakdown product of ATP, adenosine is an endogenous purine nucleoside that modulates many physiological processes in all cells of the body. (physiology.org)
- the purine nucleoside adenosine is involved in many physiological and pathophysiological events ( 35 ). (physiology.org)
- Adenosine is a purine nucleoside, responsible for the regulation of a wide range of physiological and pathophysiological conditions by binding with four G-protein-coupled receptors (GPCRs), namely A1, A2A, A2B and A3 adenosine receptors (ARs). (eurekaselect.com)
- For instance, Adenosine is a purine nucleoside, involved in different physiological and metabolic activities [ 6 , 7 ]. (rroij.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)
- 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)
- as the functionally predominant purinergic receptors on murine T cells. (aspetjournals.org)
- Previous studies of the expression of purinergic receptors in subsets of lymphocytes have been limited to receptors for ATP. (aspetjournals.org)
- Purinergic receptors are implicated in the pathogenesis of gastrointestinal disorders and are being explored as potential therapeutic targets. (readbyqxmd.com)
- Nucleotides and nucleosides act as potent extracellular messengers via the activation of the family of cell-surface receptors termed purinergic receptors. (biomedcentral.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)
- Although preliminary, these results indicate that purinergic receptors are putative pharmacological targets that should be further explored in future studies. (biomedcentral.com)
- In this study all human subtypes were stably transfected into Chinese hamster ovary (CHO) cells in order to be able to study their pharmacological profile in an identical cellular background utilizing radioligand binding studies (A1, A2A, A3) or adenylyl cyclase activity assays (A2B). (biomedsearch.com)
- The A1 subtype showed the typical pharmacological profile with 2-chloro-N6-cyclopentyladenosine (CCPA) as the agonist with the highest affinity and a marked stereoselectivity for the N6-phenylisopropyladenosine (PIA) diastereomers. (biomedsearch.com)
- Overall, the pharmacological characteristics of the human receptors are similar to other species with some species-specific characteristics. (biomedsearch.com)
- The CHO cells with stably transfected adenosine receptors provide an identical cellular background for such a pharmacological characterization. (biomedsearch.com)
- This is the first example showing that it is feasible to modulate and even enhance the pharmacological profile of a ligand of a GPCR based on conjugation to a nanocarrier and the precise structure of the linking group, which was designed to interact with distal extracellular regions of the 7 transmembrane-spanning receptor. (biomedcentral.com)
- Presently, most pharmacological agents for the treatment of allergic disease target receptors for inflammatory mediators. (aspetjournals.org)
- The renewed interest in the adenosine A 2B receptor (A2BR) subtype can be traced by studies in which the introduction of new genetic and chemical tools has widened the pharmacological and structural knowledge of this receptor as well as its potential therapeutic use in cancer and inflammation- or hypoxia-related pathologies. (physiology.org)
- Considering that the activation of proteinase-activated receptor 2 (PAR-2) is involved in pruritus both in rodents and humans, in this study we investigated the effect of H2S donors on the acute scratching behavior mediated by PAR-2 activation in mice, as well as some of the possible pharmacological mechanisms involved. (bvsalud.org)
- Biochemical and pharmacological role of A1 adenosine receptors and their modulation as novel therapeutic strategy In: ed Protein Reviews. (eurekaselect.com)
- These cells are valuable systems for further characterization of specific receptor subtypes and for the development of new ligands. (biomedsearch.com)
- A number of selective A3 ligands are available. (wikipedia.org)
- The lack of selective M5 receptor ligands is one of the main reasons that the medical community has such a limited understanding of the M5 receptors effects as the possibility that any and/or all effects of non-selective ligands may be due to interactions with other receptors can not be ruled out. (wikidoc.org)
- CysLTR2, similar to CysLTR1, is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq alpha subunit and/or Ga subunit of its coupled G protein, depending or the cell type. (wikipedia.org)
- Access to the same GPCR target in different technology formats enables identification of G-protein or Arrestin biased ligands. (discoverx.com)
- In the brain, AEA was shown to exert inhibitory ac- from inhibition of adenylate cyclase and protein kinase A. These ef- Endogenous Ligands (Endocannabinoids) fects probably result from the capability of AEA to induce, by activation of CB1 receptors, modulation of neurotrans- Since the mid-1990s, several fatty acid derivatives have been mitter (e. (oldparn.com)
- This neuromodula- substances, however, can displace high-affinity cannabinoid tory action may also underlie AEA regulation of hormone ligands from selective binding sites in membrane prepara- release at the level of the hypothalamus-pituitary-adrenal tions containing the CB1 or the CB2 receptor. (oldparn.com)
- Release of endogenous catecholamines and activation of the beta-adrenergic receptors (b-AR) have also been shown to be involved in ischaemic preconditioning. (sun.ac.za)
- The A2AR is expressed in lung tissues, where it is activated by endogenous/exogenous adenosine or A2AR agonists and where it exerts anti-inflammatory effects ( 24 , 39 , 45 ). (physiology.org)
- This rise in endogenous levels of adenosine then leads to the activation of ocular adenosine receptors and is in part responsible for the ocular hypotensive action of epinephrine. (arvojournals.org)
- In the presence of GTP all receptors were converted to a single low affinity state indicating functional coupling to endogenous G proteins. (biomedsearch.com)
- Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
- Binding of the endogenous ligand acetylcholine to the M 5 receptor triggers a number of cellular responses such as adenylate cyclase inhibition, phosphoinositide degradation, and potassium channel modulation. (wikidoc.org)
- This nucleoside, acting at one or more of its receptors, is a potent endogenous anti-inflammatory mediator. (biomedcentral.com)
- Unlike IMR32, PC12 cells, a rat adrenal pheochromocytoma cell line, resembling human neuroblastoma cell lines and also expressing the A2 subtype of adenosine receptors, was shown not to differentiate under stimulation of the A2A subtype of adenosine receptors 3. (edu.au)
- Moreover, adenosine inhibited neuronal differentiation in mouse dorsal root ganglion cells presumably via the A1 subtype 4. (edu.au)
- In the acid-secreting parietal cells of the gastric mucosa, the use of various radioligands for adenosine receptors suggested the presence of the A 2 adenosine receptor subtype(s) on the cell surface. (physiology.org)
- In detail, the synaptic channels are NMDA receptors, GABAA receptors, glutamate receptors of the neuromuscular junction, and presynaptic glutamate receptors of the kainate subtype as well as glycine receptors of the spinal chord. (uni-jena.de)
- 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)
- First, a detection method for each of the adenosine receptor subtypes was developed using reverse transcriptase polymerase chain reaction (RT-PCR). (edu.au)
- Optimization of conditions for multiplex PCR was conducted, allowing it to detect several adenosine receptor subtypes simultaneously, and it was proven to be partially successful. (edu.au)
- Treatment of cells with selective adenosine analogues for the A1 and A2A subtypes, 2-chloro-N6-cyclopentyladenosine (CCPA, 100 nM) and 2-[4-(2-carboxylethyl)phenylamino]-5'-N-ethylcarboxamido (CGS21680, 30 and 100 nM), respectively, enhanced the differentiation induced by serum deprivation at day 7 by approximately 60% and 70%, respectively. (edu.au)
- 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)
- Estrogen stimulates adenosine receptor expression subtypes in human breast cancer MCF-7 cell line. (readbyqxmd.com)
- The P2YR subtypes are typical G protein-coupled receptors (GPCRs), which typically consist of seven transmembrane domains connected by three extracellular and three intracellular loops. (biomedcentral.com)
- Derivatives of adenosine are widely found in nature and play an important role in biochemical processes, such as energy transfer-as adenosine triphosphate (ATP) and adenosine diphosphate (ADP)-as well as in signal transduction as cyclic adenosine monophosphate (cAMP). (wikipedia.org)
- To test this hypothesis, we examined the effects of pre- and posttreatment of adenosine and 5′- N -ethylcarboxamidoadenosine (NECA), a nonselective stable AR agonist, on LPS-induced lung injury. (physiology.org)
- Mice were given vehicle or LPS intratracheally followed by adenosine, NECA, or vehicle instilled via the internal jugular vein. (physiology.org)
- Importantly, posttreatment with adenosine or NECA recovers lung vascular barrier and reduces inflammation induced by LPS challenge. (physiology.org)
- 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)
- 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 5'-N-ethylcarboxamideadenosine (NECA) 2. (edu.au)
- 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)
- Binding of [\(^3\)H]NECA to A\(_2\) receptors of rat striatal membranes was inhibited by compounds 2a-d with K\(_i\) values ranging from 2.8 to 16.4 nM. (uni-wuerzburg.de)
- 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)
- Effects of electroacupuncture on the expression of adenosine receptors in the heart tissue of myocardial ischemia rats]. (readbyqxmd.com)
- To explore the impact of electroacupuncture (EA) on the protein expression of adenosine receptors in the heart of the rats with myocardial ischemia (MI). (readbyqxmd.com)
- Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
- the respective roles of the A1-, A2-, A3-adenosine receptors as well as the involvement of the PI3-K/PKB/Akt and ERKp44/p42 signal transduction pathways, in the cardioprotective phenomemon of -adrenergic preconditioning and (iv) the contribution of the mitochondrial KATP channels (mKATP), reactive oxygen species and NO to the mechanism of -AR-induced cardioprotection. (sun.ac.za)
- Although the signal transduction mechanisms associated with adrenergic receptor activation are diverse, studies have identified a relationship between the ocular hypotensive action of adrenergic agonists in their ability to stimulate adenylate cyclase. (arvojournals.org)
- Adenosine Receptors: Structure, Distribution, and Signal Transduction. (eurekaselect.com)
- Members of this calcium-dependent phospholipid-binding protein family play a role in the regulation of cellular growth and in signal transduction pathways. (cancerindex.org)
- Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
- Here, using a panel of mice lacking various combinations of adenosine receptors, and mast cells derived from these animals, we show that adenosine receptor agonists provide an effective means of inhibition of mast cell degranulation and induction of cytokine production both in vitro and in vivo. (aspetjournals.org)
- We identify A 2B as the primary receptor limiting mast cell degranulation, whereas the combined activity of A 2A and A 2B is required for the inhibition of cytokine synthesis. (aspetjournals.org)
- It is well documented that opioids are able to profoundly depress and even eliminate the HVR mainly via activating central μ-opioid receptors in both animals and humans, 11-14 but the central site(s) responsible for this inhibition remains unknown. (asahq.org)
- This study evaluated the role of adenosine receptor activation in epinephrine-induced changes in ocular function. (arvojournals.org)
- In the study of differentiation, the use of the designed PCR primers was not quantitative to measure the levels of adenosine receptors due to variations of the expressions levels of the glyceraldehyde-3-phosphate dehydrogenase (GAPDH) gene, a house-keeping gene commonly used as the internal control in PCR or northern blot analysis. (edu.au)
- 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)
- Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
- In this study, we demonstrate that, following TLR stimulation, macrophages upregulate the adenosine 2b receptor (A2bR) to enhance their sensitivity to immunosuppressive extracellular adenosine. (jimmunol.org)
- 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)
- 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, stimulation of this receptor is known to effectively decrease cyclic AMP levels and downregulate the activity of protein kinase A (PKA). (wikidoc.org)
- In contrast to nitric oxide and similar to angiotensin II, sympathoadrenergic stimulation by phenylephrine or by baroreflex activation only slightly enhanced MR [ A2 ]. (uni-freiburg.de)
- We conclude that CD39 and CD73 are surface markers of T reg cells that impart a specific biochemical signature characterized by adenosine generation that has functional relevance for cellular immunoregulation. (rupress.org)
- Furthermore, tetrahydrofolate plays a part in a second important biochemical step: the methionine-homocysteine cycle, which is necessary to provide a methyl group for several downstream reactions such as methylation of DNA, RNA proteins, and others. (bmj.com)
- In this review we propose that adenosine could be a key element in the development of new strategies for limit lipoinflammation and regulate metabolic homeostasis through modulation of adipocyte-macrophage dialog. (elsevier.es)
- This modulation is mediated through CXCR4, the receptor of SDF-1, and a pertussis toxin-sensitive G-protein-coupled signaling pathway that induces an elevation of cAMP. (jneurosci.org)
- Likewise, bly in part because of the rapid metabolism of this com- CB1-induced activation of focal adhesion kinase in hippo- pound both in vitro and in vivo (59), and because AEA is campal slices, an effect suggested to lead to modulation by a partial agonist in some functional assays of CB activity 1 cannabinoids of synaptic plasticity and learning, results (60). (oldparn.com)
- showed that radioligand binding to A2 receptors dramatically increases during monocyte differentiation in vitro. (aspetjournals.org)
- In the search for more selective A2-receptor agonists and on the basis that appropriate substitution at C2 is known to impart selectivity for A\(_2\) receptors, 2-alkynyladenosines 2a-d were resynthesized and evaluated in radioligand binding, adenylate cycla.se, and platelet aggregation studies. (uni-wuerzburg.de)
- The tritiated analogue of 2-chloro-N6-cyclopentyladenosine (CCPA), an adenosine derivative with subnanomolar affinity and a 10000-fold selectivity for A1 adenosine receptors, has been examined as a new agonist radioligand. (uni-wuerzburg.de)
- Drugs that inhibit ADENOSINE DEAMINASE activity. (nih.gov)
- 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)
- 15-17 Interestingly enough, morphologic 15,18-20 and electrophysiologic 21-24 studies have demonstrated that μ-receptors exist on both fibers' terminals and neurons in the comNTS, and activating these receptors can inhibit the presynaptic glutamate release and hyperpolarize comNTS neurons. (asahq.org)
- Since G protein coupled receptors (GPCRs) are target of forty percent of clinically used drugs, here we discuss the newly identified cardioprotective agents that bind GPCRs of adrenalin, adenosine, melatonin, ghrelin, galanin, apelin, prokineticin and cannabidiol. (frontiersin.org)
- An approach to use multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors (GPCRs) was recently introduced. (biomedcentral.com)
- 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)
- Furthermore, it has negligible affinity to A2B and A3 adenosine receptors. (drugbank.ca)
- It was originally thought that almost all allergic events were mediated directly only via the high-affinity immunoglobulin E receptors. (frontiersin.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)
- When it is administered intravenously, adenosine causes transient heart block in the atrioventricular (AV) node. (wikipedia.org)
- Recently, our laboratory found that PF could produce a dose-dependent decrease in both neurological impairment and infarct volume in acute transient cerebral ischemia through activating adenosine A 1 receptor in a manner different from its classic agonists (Liang et al. (aspetjournals.org)
- Adenosine is a multi-functional physiological molecule found abundantly in the body. (edu.au)
- In this study, we show that A2BR is functional in primary rabbit gastric parietal cells, as indicated by the fact that agonist binding to A2BR increased adenylate cyclase activity and acid production. (physiology.org)
- We conclude that rabbit gastric parietal cells possess functional A2BR proteins that are coupled to G s and stimulate HCl production upon activation. (physiology.org)
- Whether adenosine- and A2BR-mediated functional responses play a role in human gastric pathophysiology is yet to be elucidated. (physiology.org)
- Patterns of A2A Extracellular Adenosine Receptor Expression in Different Functional Subsets of Human Peripheral T Cells. (aspetjournals.org)
- 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)
- DiscoverX is proud to be the only outsourced GPCR service provider that can offer complete compound characterization by providing multiple, functional readouts for the same receptor. (discoverx.com)
- We have recently shown that extracellular adenosine enhances human pulmonary (EC) barrier via activation of adenosine receptors (ARs) in cell cultures. (physiology.org)
- 19 ) showed that activation of the A2AR ameliorated lung permeability and protein levels in bronchoalveolar lavage fluid (BALF) in traumatic hemorrhagic shock. (physiology.org)
- 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-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)
- 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)
- 1994). "Signaling through transforming G protein-coupled receptors in NIH 3T3 cells involves c-Raf activation. (wikidoc.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)
- Furthermore, TRPA1 receptors mediate the pruritus induced by activation of PAR-2, but H2S does not interfere with this pathway. (bvsalud.org)
- However, treatment with full A1 AR agonists has been associated with numerous challenges like cardiovascular side effects, off-target activation as well as desensitization of A1 AR leading to tachyphylaxis. (eurekaselect.com)
- Allosteric enhancer of A1 AR is found to be potent for the treatment of neuropathic pain, culminating the side effects related to off-target tissue activation of A1 AR. (eurekaselect.com)
- 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)
- 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)
- A2B adenosine receptor (A2B AR) activation induces Gs-dependent cyclic AMP accumulation. (readbyqxmd.com)
- 1 2 3 Pharmacologically, epinephrine is a nonselective adrenergic agonist that can activate both α- andβ -adrenergic receptors. (arvojournals.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)
- In project area B eight projects are summarized that use high-end light microscopy to unravel the function of ligand-gated ion channels, i.e. ionotropic receptors. (uni-jena.de)
- In sturlies on adenylate cyclase 2',3'-dideoxy-N\(^6\)-cyclohexyladenosine (ddCHA) did not show agonist properties at A\(_1\) or at A\(_2\) receptors. (uni-wuerzburg.de)
- A 30- to 45-fold selectivity for platelet A\(_2\) receptors compared to A\(_1\) receptors was found for compounds 8a-c in adenylate cyclase studies. (uni-wuerzburg.de)
- In this regard, the level of nucleoside adenosine is increased in individuals with obesity. (elsevier.es)
- The relative potencies of agonists for the A2B adenosine receptor could only be tested by measurement of receptor-stimulated adenylyl cyclase activity. (biomedsearch.com)
- It has been shown that an A2AR agonist protects against ischemia-reperfusion injury in porcine allogeneic lung transplantation ( 23 ). (physiology.org)
- 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)
- Extra- and/or immediate pericellular accumulation of adenosine elicits immunosuppressive cellular responses that are mediated through several type 1 purinergic (adenosine) receptors, including A2A ( 18 ). (rupress.org)
- The evidences indicate a dual function of these receptors, depending on the microorganism and the cellular model involved. (biomedcentral.com)
- Methotrexate-induced metabolic changes lead to increased extra-cellular adenosine. (biomedcentral.com)
- The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it. (wikipedia.org)
- The human muscarinic acetylcholine receptor M 5 , encoded by the CHRM5 gene, is a member of the G protein-coupled receptor superfamily of integral membrane proteins . (wikidoc.org)
- CysLTR2 encodes a protein composed of 347 amino acids and shows only modest similarity to the CysLTR1 gene in that its protein shares only 31% amino acid identity with the CysLTR1 protein. (wikipedia.org)
- To characterize the third regulatory mechanism in more detail, mice were studied that are genetically deficient in TGF due to targeted deletion of the gene coding for A1 adenosine receptors (A1AR), the major signaling pathway of TGF [ O19 ]. (uni-freiburg.de)
- What does this gene/protein do? (cancerindex.org)
- Furthermore, adenosine significantly attenuated protein degradation of A2A and A3 receptors induced by LPS. (physiology.org)
- Muscarinic receptors mediate many of the effects of acetylcholine in the central and peripheral nervous system. (wikidoc.org)
- 1996). "Phosphorylation of human m1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 and protein kinase C. (wikidoc.org)
- In vitro, ARC1779 inhibits vWF A1-dependent or shear stress-induced platelet aggregation as well as platelet adhesion to collagen-coated matrices . (spotidoc.com)
- 2-Alkynyladenosines also exhibited high-affmity binding at solubilized A\(_2\) receptors from human platelet membranes. (uni-wuerzburg.de)
- Adenosine is used as an adjunct to thallous (thallium) chloride TI 201 or Tc99m myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
- In a mouse model of infarction the A3 selective agonist CP-532,903 protected against myocardial ischemia and reperfusion injury. (wikipedia.org)
- Preconditioning of cardiomyocytes with either A 1 or A 3 AR agonists protects against myocardial ischemia. (biomedcentral.com)
- Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. (drugbank.ca)
- This superfamily includes the chemokine receptors. (jneurosci.org)
- 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)
- Cell counts, EBDA extravasation, as well as levels of proteins and inflammatory cytokines were decreased in adenosine-treated mice. (physiology.org)
- In vitro studies using cultured human and mouse mast cells, and studies of mice lacking A 2B receptors, suggest that adenosine receptors, specifically the G s -coupled A 2A and A 2B receptors, might provide such a target. (aspetjournals.org)
- a) cells expressing both CysLTR1 and GPR17 receptors exhibit a marked reduction in binding and responding to LTD4 and b) mice lacking GPR17 are hyper-responsive to igE in a model for passive cutaneous anaphylaxis. (wikipedia.org)
- Adenosine A3 receptors are G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. (wikipedia.org)
- CB1 receptors are rectifying potassium channels through CB1 receptors (49), associated with nerve fibers and axon terminals, but not may not be the sole intracellular signaling messages deliv- in the neuronal soma. (oldparn.com)
- Signaling through A 2A adenosine receptors (A 2A R) regulates T lymphocyte expansion and modulates T cell receptor (TCR)-mediated effector functions in vitro. (aspetjournals.org)
- Globally, a collection of neural stimuli, efferent and afferent, endocrine and paracrine agents, acting directly at apical and basolateral membrane receptors/transporters of the parietal cell or acting indirectly through the other cells of the gastric mucosa, as well as mechanical and chemical stimuli participate in acid secretion physiology (e.g., see recent reviews in Refs. (physiology.org)
- The common aim of the five projects in project area A is to elaborate and/or optimize high-end light microscopy methods designed to learn more about the function of membrane receptors. (uni-jena.de)
- Black-lipid-membrane platform with diffusion suppression for confocal single-molecule FLIM-FRET analysis of gated membrane receptors and transporters. (uni-jena.de)
- This project will target specifically the development for a nanoscale and label-free structure-investigation of membrane receptors, potentially even more specific membrane receptor surfaces. (uni-jena.de)
- Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pharmacology of adenosine receptors: the state of the art. (eurekaselect.com)
- The coordinated expression of CD39/CD73 on T reg cells and the adenosine A2A receptor on activated T effector cells generates immunosuppressive loops, indicating roles in the inhibitory function of T reg cells. (rupress.org)
- Seminal, important genetic data indicate that adenosine, which is operative via the A2A adenosine receptor, plays critical, nonredundant, autonomous, and autochthonous roles in inhibiting effector functions of activated T cells ( 19 , 20 ). (rupress.org)
- Adenozinski A 3 receptor ( ADORA3 ) je adenozinski receptor . (wikipedia.org)
- Adenozinski A 2A receptor ( ADORA2A ) je adenozinski receptor . (wikipedia.org)
- Various kinase inhibitors, especially inhibitors of cell cyclin-dependent kinase (rescovitine), rho and Ca2+-dependent protein kinase (Y-27632), tyrosine kinase (tyrphostin AG879), phosphatidylinositol 3-kinase (bisindolylmaleimide I, BIM I), and Ca2+/calmodulin kinase (chelerythrine), strongly inhibited collagen gel contraction. (omicsonline.org)
- This contraction was also inhibited by ethacrynic acid, by inhibitors of Na+, K+-ATPase (ouabain), Ca2+- ATPase (thapsigargin), and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, by a non-selective phosphodiesterase inhibitor (papaverine), and by adenosine A2 (metrifudil), and cannabinoid receptor (CP-55940) agonists. (omicsonline.org)
- 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)