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.
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.
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.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
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.
An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.
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.
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).
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.
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.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
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.
Drugs that bind to and activate dopamine receptors.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
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.
Purine bases found in body tissues and fluids and in some plants.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
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.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
The relationship between the dose of an administered drug and the response of the organism to the drug.
Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
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.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
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.
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.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
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.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
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.
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.
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.
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.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
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.
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.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
A selective D1 dopamine receptor agonist used primarily as a research tool.
Drugs that bind to and activate adrenergic receptors.
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.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A dopamine D2/D3 receptor agonist.
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.
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.
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.
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.
Drugs that bind to and activate excitatory amino acid receptors.
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.
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)
A family of hexahydropyridines.
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.
Drugs that selectively bind to and activate beta-adrenergic receptors.
Compounds with BENZENE fused to AZEPINES.
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.
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
Drugs that selectively bind to and activate alpha adrenergic receptors.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
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.
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.
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)
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.
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.
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.
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.
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.
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.
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.
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.
Drugs that bind to and activate cholinergic receptors.
Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.
The rate dynamics in chemical or physical systems.
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.
A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.
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.
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.
OXAZINES with a fused BENZENE ring.
Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.
A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
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.
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.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.
Elements of limited time intervals, contributing to particular results or situations.
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)
The observable response an animal makes to any situation.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
Compounds that bind to and activate PURINERGIC RECEPTORS.
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.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
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.
A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.
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.
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.
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.
A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.
A series of structurally-related alkaloids that contain the ergoline backbone structure.
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.
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.
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.
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)
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
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.
Catalyze the hydrolysis of nucleosides with the elimination of ammonia.
Established cell cultures that have the potential to propagate indefinitely.
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.
A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.
Drugs used to cause dilation of the blood vessels.
Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.
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.
Agents inhibiting the effect of narcotics on the central nervous system.
The physical activity of a human or an animal as a behavioral phenomenon.
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.
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.
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.
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.
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.
A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.
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.
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.
Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
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)
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
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.
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.
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)
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.
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)
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.
A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.
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.
The most common inhibitory neurotransmitter in the central nervous system.
Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.
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.
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.
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.
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)
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.
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.
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
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.-.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
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.
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.
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)
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).
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.
A purine base and a fundamental unit of ADENINE NUCLEOTIDES.
One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.
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.
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)
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.
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
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.
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.
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.
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
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.
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.
An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.
Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.
Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.
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.
A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.
Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.

Involvement of adenosine A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of cocaine and methamphetamine in rats. (1/229)

Adenosine, by acting on adenosine A1 and A2A receptors, is known to antagonistically modulate dopaminergic neurotransmission. We have recently reported that nonselective adenosine receptor antagonists (caffeine and 3,7-dimethyl-1-propargylxanthine) can partially substitute for the discriminative-stimulus effects of methamphetamine. In the present study, by using more selective compounds, we investigated the involvement of A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of both cocaine and methamphetamine. The effects of the A1 receptor agonist N6-cyclopentyladenosine (CPA; 0.01-0.1 mg/kg) and antagonist 8-cyclopentyl-1,3-dimethylxanthine (CPT; 1.3-23.7 mg/kg) and the A2A receptor agonist 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine hydrochloride (CGS 21680; 0.03-0.18 mg/kg) and antagonist 3-(3-hydroxypropyl)-8-(3-methoxystyryl)-7-methyl-1-propargylxanthin phosphate disodium salt (MSX-3; 1-56 mg/kg) were evaluated in rats trained to discriminate either 1 mg/kg methamphetamine or 10 mg/kg cocaine from saline under a fixed-ratio 10 schedule of food presentation. The A1 and A2A receptor antagonists (CPT and MSX-3) both produced high levels of drug-lever selection when substituted for either methamphetamine or cocaine and significantly shifted dose-response curves of both psychostimulants to the left. Unexpectedly, the A2A receptor agonist CGS 21680 also produced drug-appropriate responding (although at lower levels) when substituted for the cocaine-training stimulus, and both CGS 21680 and the A1 receptor agonist CPA significantly shifted the cocaine dose-response curve to the left. In contrast, both agonists did not produce significant levels of drug-lever selection when substituted for the methamphetamine-training stimulus and failed to shift the methamphetamine dose-response curve. Therefore, adenosine A1 and A2A receptors appear to play important but differential roles in the modulation of the discriminative-stimulus effects of methamphetamine and cocaine.  (+info)

Comparative pharmacological studies on the A2 adenosine receptor agonist 5'-n-ethyl-carboxamidoadenosine and its F19 isotope labelled derivative. (2/229)

Adenosine receptors are expressed in various mammalian tissues where they mediate the effects of adenosine on cellular functions through a number of signalling mechanisms. 18F-NECA is the positron-emitting derivative of the A(2)-receptor agonist NECA (5'-n-ethyl-carboxamidoadenosine) and is a radioligand for PET imaging of adenosine receptors. Contractility and relaxation studies were performed on guinea pig atrial myocardium, pulmonary artery, and thoracic aorta to compare the pharmacological effects of NECA and F-NECA (a non-emitting derivative) on tissues. Furthermore, the effect of NECA and F-NECA on the potassium conductance was investigated in DDT1 MF-2 smooth muscle cells with the patch-clamp technique. Both NECA and F-NECA reduced the contractile force in atrial myocardium and evoked phasic contraction in pulmonary artery (A(1) adenosine-receptor-mediated actions) in a dose dependent manner; however, the apparent affinity was lower for F-NECA. No difference was found in relaxation induced by these compounds in 1 microM noradrenaline-precontracted aorta and pulmonary artery (in the presence of DPCPX, an A(1) adenosine receptor antagonist, tissue containing A(2B) adenosine receptors). NECA (5 microM) and F-NECA (5 microM) also decreased the peak current and accelerated activation and inactivation properties of the potassium channels, but F-NECA was less effective. These results suggest that while NECA and F-NECA are equivalent agonists of vascular A(2B) receptors, they mediate different changes of some parameters. When evaluating the data obtained by the use of radiolabelled ligands, one has to take into consideration the possible physiological effects of the ligands besides its binding properties to tissues.  (+info)

Protection from ischemic liver injury by activation of A2A adenosine receptors during reperfusion: inhibition of chemokine induction. (3/229)

Ischemia-reperfusion (I/R) injury occurs as a result of restoring blood flow to previously hypoperfused vessels or after tissue transplantation and is characterized by inflammation and microvascular occlusion. We report here that 4-[3-[6-amino-9-(5-ethylcarbamoyl-3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2 -yl]-prop-2-ynyl]-cyclohexanecarboxylic acid methyl ester (ATL146e), a selective agonist of the A(2A) adenosine receptor (A(2A)AR), profoundly protects mouse liver from I/R injury when administered at the time of reperfusion, and protection is blocked by the antagonist ZM241385. ATL146e lowers liver damage by 90% as assessed by serum glutamyl pyruvic transaminase and reduces hepatic edema and MPO. Most protection remains if ATL146e treatment is delayed for 1 h but disappears when delayed for 4 h after the start of reperfusion. In mice lacking the A(2A)AR gene, protection by ATL1465e is lost and ischemic injury of short duration is exacerbated compared with wild-type mice, suggesting a protective role for endogenous adenosine. I/R injury causes induction of hepatic transcripts for IL-1alpha, IL-1beta, IL-1Ra, IL-6, IL-10, IL-18, INF-beta, INF-gamma, regulated on activation, normal T cell expressed, and presumably secreted (RANTES), major intrinsic protein (MIP)-1alpha, MIP-2, IFN-gamma-inducible protein (IP)-10, and monocyte chemotactic protein (MCP)-1 that are suppressed by administering ATL146e to wild-type but not to A(2A)AR knockout mice. RANTES, MCP-1, and IP-10 are notable as induced chemokines that are chemotactic to T lymphocytes. The induction of cytokines may contribute to transient lymphopenia and neutrophilia that occur after liver I/R injury. We conclude that most damage after hepatic ischemia occurs during reperfusion and can be blocked by A(2A)AR activation. We speculate that inhibition of chemokine and cytokine production limits inflammation and contributes to tissue protection by the A(2A)AR agonist ATL146e.  (+info)

Input-specific modulation of neurotransmitter release in the lateral horn of the spinal cord via adenosine receptors. (4/229)

Activation of adenosine A2A receptors (A2ARs) in the CNS produces a variety of neuromodulatory actions dependent on the region and preparation examined. In autonomic regions of the spinal cord, A1R activation decreases excitatory synaptic transmission, but the effects of A2AR stimulation are unknown. We sought to determine the location and function of the A2ARs in the thoracic spinal cord, focusing on the intermediolateral cell column (IML). A2AR immunoreactivity was observed throughout the gray matter, with particularly dense immunostaining in regions containing sympathetic preganglionic neurons (SPNs), namely, the IML and intercalated nucleus. Electron microscopy revealed A2AR immunoreactivity within presynaptic terminals and in postsynaptic structures in the IML. To study the functional relevance of these A2ARs, visualized whole-cell patch-clamp recordings were made from electrophysiologically identified SPNs and interneurons within the IML. The A2AR agonist c2-[p-(carboxyethyl)phenethylamino]-5'-N-ethylcarboxyamidoadenosine (CGS 21680) had no significant effect on EPSPs but increased the amplitude of IPSPs elicited by stimulation of the lateral funiculus. These effects were attributable to activation of presynaptic A2ARs because CGS 21680 application altered the paired pulse ratio. Furthermore, neurons in the IML that have IPSPs increased via A2AR activation also receive excitatory inputs that are inhibited by A1R activation. These data show that activating A2ARs increase inhibitory but not excitatory transmission onto neurons in the IML. Simultaneous activation of A1Rs and A2ARs therefore could facilitate inhibition of the postsynaptic neuron, leading to an overall reduction of sympathetic nervous activity.  (+info)

Epoxyeicosatrienoic acids mediate adenosine-induced vasodilation in rat preglomerular microvessels (PGMV) via A2A receptors. (5/229)

Activation of rat adenosine2A receptors (A2A R) dilates preglomerular microvessels (PGMV), an effect mediated by epoxyeicosatrienoic acids (EETs). Incubation of PGMV with a selective A2A R agonist, 2-p-(2-carboxyethyl) phenethylamino-5'-N-ethylcarboxamidoadenosine (CGS 21680; 100 microM), increased isolated PGMV EET levels to 7.57+/-1.53 ng mg-1 protein from 1.06+/-0.22 ng mg-1 protein in controls (P<0.05), without affecting hydroxyeicosatetraenoic acid (HETE) levels (10.8+/-0.69 vs 11.02+/-0.74 ng mg-1 protein). CGS 21680-stimulated EETs was abolished by preincubation with an A2A R antagonist, 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phe nol (ZM241385) (100 microM). A selective epoxygenase inhibitor, methylsulfonyl-propargyloxyphenylhexanamide (MS-PPOH; 12 microM) prevented CGS 21680-induced increase in EETs, indicating inhibition of de novo synthesis of EETs. In pressurized (80 mmHg) renal arcuate arteries (110-130 microm) preconstricted with phenylephrine (20 nM), superfusion with CGS 21680 (0.01-10 microM) increased the internal diameter (i.d.) concentration-dependently; vasodilation was independent of nitric oxide and cyclooxygenase activity. CGS 21680 (10 microM) increased i.d. by 32+/-6 microm; vasodilation was prevented by inhibition of EET synthesis with MS-PPOH. Addition of 3 nM 5,6-EET, 8,9-EET and 11,12-EET increased i.d. by 53+/-9, 17+/-4 and 53+/-5 microm, respectively, whereas 14,15-EET was inactive. The responses to 5,6-EET were, however, significantly inhibited by indomethacin. We conclude that 11,12-EET is the likely mediator of A2A R-induced dilation of rat PGMV. Activation of A2A R coupled to de novo EET stimulation may represent an important mechanism in regulating preglomerular microvascular tone. British Journal of Pharmacology (2004) 141, 441-448. doi:10.1038/sj.bjp.0705640  (+info)

Randomized, controlled dose-ranging study of the selective adenosine A2A receptor agonist binodenoson for pharmacological stress as an adjunct to myocardial perfusion imaging. (6/229)

BACKGROUND: Dipyridamole and adenosine cause frequent side effects as a result of nonspecific adenosine receptor stimulation. Selective agonism of the adenosine A2A receptor should result in a similar degree of coronary vasodilation (and thus similar perfusion images) with fewer side effects. METHODS AND RESULTS: In a multicenter, randomized, single-blind, 2-arm crossover trial, 240 patients underwent 2 single photon emission computed tomographic (SPECT) imaging studies in random order, first after pharmacological stress with adenosine and a second study with the selective adenosine A2A receptor agonist binodenoson, using 1 of 4 dosing regimens. Safety, tolerability, and SPECT image concordance between the 2 agents were examined. Exact categorical agreement in the extent and severity of reversible perfusion defects ranged from 79% to 87%, with kappa values from 0.69 to 0.85, indicating very good to excellent agreement between binodenoson and adenosine. The risk of any safety event/side effect was significantly lower with any dose of binodenoson than with adenosine (P< or =0.01) because of a dose-related reduction in subjective side effects, as objective events were infrequent. There was a reduction in the severity of chest pain, dyspnea, and flushing in all binodenoson doses compared with adenosine (P<0.01), and the magnitude of severity reduction was dose-related. CONCLUSIONS: The selective adenosine A2A receptor agonist binodenoson results in an extent and severity of reversible perfusion defects on SPECT imaging similar to nonselective adenosine receptor stimulation, accompanied by a dose-related reduction in the incidence and severity of side effects.  (+info)

Role of adenosine A2A receptor in the regulation of gastric somatostatin release. (7/229)

Adenosine has been demonstrated to inhibit gastric acid secretion. In the rat stomach, this inhibitory effect may be mediated indirectly by increasing the release of somatostatin-like immunoreactivity (SLI). Results show that adenosine analogs augmented SLI release in the isolated vascularly perfused rat stomach. The rank order of potency of the analogs in stimulating SLI release was 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine (CGS 21680) approximately 5'-N-ethylcarboxamidoadenosine > 2-chloroadenosine > R-(-)-N(6)-(2-phenylisopropyl)adenosine >1-deoxy-1-[6-[[(3-iodophenyl)methyl]amino]-9H-purin-9-yl]-N-methyl-beta-d-ribofu ranuronamide > N(6)-cyclopentyladenosine approximately N(6)-cyclohexyladenosine > S-(+)-N(6)-(2-phenylisopropyl) adenosine, suggesting the involvement of the A(2A) receptor. In agreement, 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a] [1,3,5]triazin-5-ylamino]ethyl)phenol (ZM 241385), an A(2A) receptor antagonist, was shown to abolish the adenosine- and CGS 21680-stimulated SLI release. Immunohistochemical studies reveal the presence of A(2A) receptor immunoreactivity on the gastric plexi and mucosal D-cells, but not on parietal cells and G-cells, suggesting that adenosine may act directly on D-cells or indirectly on the gastric plexi to augment SLI release. The present study also demonstrates that the structure of the mucosal A(2A) receptor is identical to that in the rat brain, and that alternative splicing of this gene does not occur. A real-time reverse transcription-polymerase chain reaction assay has also been established to quantify the levels of A(2A) receptor mRNA. Results show that gastric tissues contained significantly lower levels of A(2A) receptor mRNA compared with the striatum. The lowest level was detected in the mucosa. In conclusion, adenosine may act on A(2A) receptors to augment SLI release and consequently control gastric acid secretion.  (+info)

A1 and A2A adenosine receptor modulation of alpha 1-adrenoceptor-mediated contractility in human cultured prostatic stromal cells. (8/229)

1. This study investigated the possibility that adenosine receptors modulate the alpha(1)-adrenoceptor-mediated contractility of human cultured prostatic stromal cells (HCPSC). 2. The nonselective adenosine receptor agonist, 5'-N-ethylcarboxamido-adenosine (NECA; 10 nm-10 microm), and the A(1) adenosine receptor selective agonist, cyclopentyladenosine (CPA; 10 nm-10 microm), elicited significant contractions in HCPSC, with maximum contractile responses of 18+/-3% and 17+/-2% reduction in initial cell length, respectively. 3. In the presence of a threshold concentration of phenylephrine (PE) (100 nm), CPA (1 nm-10 microm) caused contractions, with an EC(50) of 124+/-12 nm and maximum contractile response of 37+/-4%. The A(1) adenosine receptor-selective antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX 100 nm) blocked this effect. In the presence of DPCPX (100 nm), NECA (1 nm-10 microm) inhibited contractions elicited by a submaximal concentration of PE (10 microm), with an IC(50) of 48+/-2 nm. The A(2A) adenosine receptor-selective antagonist 4-(2-[7-amino-2-[furyl][1,2,4]triazolo[2,3-alpha][1,3,5,]triazin-5-yl amino]ethyl)phenol (Zm241385 100 nm) blocked this effect. 4. In BCECF-AM (10 microm)-loaded cells, both CPA (100 pM-1 microm) and NECA (100 pm-10 microm) elicited concentration-dependent decreases in intracellular pH (pH(i)), with EC(50) values of 3.1+/-0.3 and 6.0+/-0.3 nm, respectively. The response to NECA was blocked by Zm241385 (100 nm; apparent pK(B) of 9.4+/-0.4), but not by DPCPX (100 nm). The maximum response to CPA was blocked by DPCPX (100 nm), and unaffected by Zm241385 (100 nm). 5. NECA (10 nm-10 microm) alone did not increase [(3)H]-cAMP in HCPSC. In the presence of DPCPX (100 nm), NECA (10 nm-10 microm) caused a concentration dependent increase in [(3)H]-cAMP, with an EC(50) of 1.2+/-0.1 microm. This response was inhibited by Zm241385 (100 nm). CPA (10 nm-10 microm) had no effect on cAMP, in the presence or absence of forskolin (1 microm). 6. These findings are consistent with a role for adenosine receptors in the modulation of adrenoceptor-mediated contractility in human prostate-derived cells.  (+info)

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Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.
Learn about regadenoson: What is it used for, what you need to know before taking, important warnings and safety info, how to take, side effects and more...
Structure, properties, spectra, suppliers and links for: 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide.
6-Amino-1,3-dihydro-2H-purin-2-one; CAS Number: 3373-53-3; Linear Formula: C5H5N5O; find Ambeed, Inc.-AMBH46A96504 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich
You are viewing an interactive 3D depiction of the molecule 1-(7h-purin-6-yl)-n-[3-(trifluoromethyl)phenyl]-4-piperidinecarboxamide (C18H17F3N6O) from the PQR.
You are viewing an interactive 3D depiction of the molecule 8-azido-9-(5-o-phosphono-d-ribofuranosyl)-9h-purin-6-amine (C10H13N8O7P) from the PQR.
... -First A2A Adenosine Receptor Agonist Approved for Use as Pharmacolo... Stress Agent in Myocardial Perfusion Imaging- ...PALO ALTO Calif. and DEERFIELD Ill. April 10 FirstCall/...Lexiscan is the first A2A adenosine receptor agonist shown to be safe...,CV,Therapeutics,and,Astellas,Announce,FDA,Approval,for,Lexiscan(TM),(regadenoson),Injection,biological,advanced biology technology,biology laboratory technology,biology device technology,latest biology technology
This work done by an eminent group in the area raises concerns over the use of regadenoson for clinical stress testing, whether done by PET or SPECT. Invasive and pharmacologic studies had previously demonstrated peak regadenoson effect at approximately 1-2 minutes after injection, consistent with the findings of the present study. Stress labs which are not already following a 1- to 2-minute delay may wish to consider introducing one.. There are several reasons to view these results with caution, however. First, many prior studies had compared regadenoson to other vasodilators using a variety of techniques including PET, SPECT, and invasive methods. In general, no significant differences or only minimal differences, below the level of clinical relevance, were observed. The reasons for the discrepancies are unclear.. One longstanding concern with regards to regadenoson has been the use of a single fixed dose without weight adjustment, as is usually done for other vasodilators. The investigators ...
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Regadenoson produced higher stress MBF than dipyridamole and adenosine (3.58 ± 0.58 vs. 2.81 ± 0.67 vs. 2.78 ± 0.61 ml/min/g, p = 0.0009 and p = 0.0008 respectively). Regadenoson had a much higher heart rate response than adenosine and dipyridamole respectively (95 ± 11 vs. 76 ± 13 vs. 86 ± 12 beats/ minute) When stress MBF was adjusted for heart rate, there were no differences between regadenoson and adenosine (37.8 ± 6 vs. 36.6 ± 4 μl/sec/g, p = NS), but differences between regadenoson and dipyridamole persisted (37.8 ± 6 vs. 32.6 ± 5 μl/sec/g, p = 0.03). The unadjusted MPR was higher with regadenoson (3.11 ± 0.63) when compared with adenosine (2.7 ± 0.61, p = 0.02) and when compared with dipyridamole (2.61 ± 0.57, p = 0.04). Similar to stress MBF, these differences in MPR between regadenoson and adenosine were abolished when adjusted for heart rate (2.04 ± 0.34 vs. 2.12 ± 0.27, p = NS), but persisted between regadenoson and dipyridamole (2.04 ± 0.34 vs. 1.77 ± 0.33, p = ...
Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients.1-4 In addition, both adenosine and dipyridamole produce severe bronchoconstriction when given to asthmatics. Because of its ultrashort half-life, adenosine must be administered by a constant IV infusion.. Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A1, A2B, and A3.5 The discovery of highly selective and relatively short-acting adenosine receptor A2A agonists6-9 has opened the ...
Approximately 250 patients who are referred for a nuclear stress testing of the heart with regadenoson (Lexiscan®) will be recruited to participate in the study. Following regadenoson (administered as part of a stress routine test protocol) participants will receive either aminophylline (75 mg - intravenously) or a matching inactive placebo (sterile salt water) injection. Participants will be surveyed for gastrointestinal symptoms and other side effects related to regadenoson. The frequency and severity of such side effects will be compared between the two study groups (aminophylline vs. placebo ...
8-(1-hydroxyethyl)-1,3-dimethyl-7H-purine-2,6-dione,8-cyclohexyl-1,3-dimethyl-7H-purine-2,6-dione,8-(cyclohexylamino)-1,3-dimethyl-7H-purine-2,6-dione,8-[(4-aminophenyl)methyl]-1,3-dimethyl-7H-purine-2,6-dione,8-cyclohexyl-1,3,7-trimethyl-purine-2,6-dione,8-cyclohexyloxy-1,3,7-trimethyl-purine-2,6-dione,8-hexyl-1,3,7-trimethyl-purine-2,6-dione,8-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]octanoic acid,8-[1-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]ethyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[3-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]propyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[4-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]butyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[5-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]pentyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[6-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]hexyl]-1,3-dimethyl-7H-purine-2,6-dione,8-(diphenylmethyl)-1,3,7-trimethyl-purine-2,6-dione,8-[8-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]octyl]-1,3
Lung transplantation currently is one way to treat a variety of serious diseases and conditions such as emph ysema, pulmonary fibrosis, and cystic fibrosis. Ischemia Reperfusion Injury (IRI) is a known problem that can happen during the first few days after a lung transplant. IRI can cause swelling of the lungs and low levels of oxygen. The most serious type of IRI can cause the transplanted lung to not work properly, it can even cause death. While new treatments and practices have been put into place to lower the chances of IRI, it is still a difficult problem to overcome after a lung transplant. Medicines called Adenosine 2A receptors (A2AR) have been studied in animals with IRI for many years. Some of these studies suggest that with the use of A2AR medicines, the chance of IRI may be lowered or prevented. Regadenoson is an A2AR drug. ...
142130-73-2 - UZNXSBPBWFLVDK-NKWVEPMBSA-N - 3-(6-Amino-9H-purin-9-yl)-cyclopentanol - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Compound 2-CHLORO-9-[2-DEOXY-5-O-[(1,1-DIMETHYLETHYL)-DIPHENYLSILYL]-BETA-D-ERYTHRO-PENTOFURANOSYL]-9H-PURIN-6-AMINEwith free spectra: 1 NMR.
N,N,9-Trimethyl-9H-purin-6-amine | C8H11N5 | CID 221105 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Product Number: C6621 CAS number: 390409-17-3 unlabeled Synonyms: GS-7171 fumarate // [2H6]-N-[[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-1-methylethyl ester-L-alanine fumarate-d6. ...
Product Number: C6621 CAS number: 390409-17-3 unlabeled Synonyms: GS-7171 fumarate // [2H6]-N-[[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-1-methylethyl ester-L-alanine fumarate-d6. ...
Adenoscan® (adenosine) is an approved pharmacological stress agent indicated as an adjunct to thallium-201 myocardial perfusion scintigraphy in patients unable to exercise adequately. The investigational drug, regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist, the receptor responsible for coronary vasodilation, and is being studied for potential use as a pharmacologic stress agent in myocardial perfusion imaging (MPI) studies. This study will compare the safety and efficacy of regadenoson to that of Adenoscan in detecting reversible myocardial perfusion defects ...
Adenosine might provoke bronchospasm in certain susceptible patients such as those with asthma or those on maintenance doses of bronchodilators or steroids. The selectivity of regadenoson was therefore of great interest to study for its safety and efficacy in such patients. The final answer is not yet in, and more studies are needed, but there are some preliminary data.. Prior studies have suggested that with prophylactic pre-treatment with a B-2 agonist, adenosine could be given to patients with mild asthma or chronic obstructive lung disease (COPD). It should be noted the majority of patients with COPD but no bronchospasm could be tested with adenosine without any serious problem (39). Further, tachypnea is common after adenosine infusion and is not due to changes in airway resistance or pulmonary capillary wedge pressure but rather to stimulation of carotid body receptors (40,41).. A randomized double-blind, placebo-controlled cross-over trial assessed the safety of regadenoson in 48 patients ...
In a recent prospective, double-blind, randomized multicenter phase 3 trial, ADVANCE (Adenosine versus Regadenoson Comparative Evaluation for Myocardial Perfusion Imaging), the A2A selective adenosine receptor agonist, regadenoson, was shown to be noninferior to the nonselective vasodilator, adenosine, for detecting myocardial ischemia (1). The overall visual agreement was comparably low (in the low 60% range) for the adenosine-regadenoson and for the adenosine-adenosine comparisons. Conversely, when quantitative analysis was applied, regadenoson induced virtually identical results to adenosine-regarding the size and severity of left ventricular perfusion defect size and extent of ischemia (2). What are the regulatory implications of these findings? Should the regulatory bodies rely on subjective visual interpretation of myocardial perfusion studies, on objective quantitative programs to appraise the comparability between vasodilators, or both? What is the true standard?. In order to avoid the ...
Structure, properties, spectra, suppliers and links for: (2S)-2-(8-Iodo-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-9H-purin-9-yl)propanamide.
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3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile chemical properties, What are the chemical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile 86375-28-2, What are the physical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile ect.
chemBlink provides information about CAS # 3945-69-5, 4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methyl morpholinium chloride, DMTMM, molecular formula: C10H17ClN4O3.
Methanol,[(4,6-dimethyl-1,3,5-triazin-2-yl)amino]-(9ci)/ACM84591888 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
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Are you stress now? Let me tell you about it. Stress is simply the bodys reaction the wear and tear of life. Every single activity you engage in, every emotion you feel, whether it is asking the boss for a raise, or trying to complete an assignment, set up stress. The way your body reacts to such stress agents has much to do with your health ...
Buy CGS 21680 (CAS 124182-57-6), a potent, selective A2A agonist. Join researchers using high quality CGS 21680 from Abcam and achieve your mission, faster.
A review. The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain G protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various species, including rat and human, and its sequences are highly similar across species, ranging from 85% identity between human and mouse and 95% identity between rat and mouse. The A2B receptors show a ubiquitous distribution, the highest levels are present in cecum, colon and bladder, followed by blood vessels, lung, eye and mast cells. Through A2B receptors adenosine seems to cause mast cells degranulation, vasodilation, cardiac fibroblast proliferation, inhibition of Tumor Necrosis Factor (TNF-α), increased synthesis of interleukin-6 (IL-6), stimulation of Cl- secretion in intestinal epithelia and hepatic glucose prodn. Hence, A2B adenosine receptor agonists could be useful ...
ALI is one of the leading causes of morbidity and mortality of critical illness with extremely limited therapeutic options. In the present study, we pursued the hypothesis that tissue-specific adenosine signaling events through the A2B adenosine receptor contribute to lung protection and can thus be targeted for ALI treatment. To make progress on this front, we performed a head-to-head comparison of mice with genetic deletion of Adora2b in the myeloid lineage, vascular endothelial cells, or alveolar epithelial cells. Interestingly, we only observed a phenotype in mice with tissue-specific Adora2b deletion in alveolar epithelial cells, closely resembling the observed detrimental effects of global Adora2b deletion during ALI. Interestingly, the injurious effects of our two-hit model where an inflammatory event (i.t. LPS treatment) is followed by injurious mechanical ventilation seem to be supra-additive compared with the effects of injurious ventilation or LPS i.t. alone. Based on these findings ...
Particularly preferably, Z21 is 2,4-dichloro-1,3,5-triazin-6-ylf 2-chloro-4-(3-(2-suifatoethylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-chloro-4-(4-(2-su!fatoethy!sulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-chloro-4-(3-(vinylsulfonyl)-phenylarnino)-1 t3,5-triazin-6-yl, 2-chloro4-(4-(vinylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-ch!oro-4-(N-methy!-N-(2-(2-sulfatoethylsulfonyl)-ethy!)-amino)-1,3,5-triazin-6-yl, 2-ch!oro-4-(N-phenyl-N-(2-(2-sulfatoethylsulfonyl)-ethyl)-amino)-1,3,5-tria2in-6-yl, 2-fluoro-4-morpholino-1,3,5-triazin-6-yI, 2-fluoro-4-(2-sulfophenyl-amino)-1,3,5-triazin-6-yl, 2-fluoro-4-(3-sulfophenylamino)-1,3,5-triazin-6-yl, 2-fluoro-4-(4-sulfophenylamino)-1,3,5-triazin-6-yl, 2-fiuoro-4-(3-trimethylammonio-phenylamino)-1,3,5-triazin-6-ylf 2-fIuoro-4-(4-trirnethylammoniophenylamino)-1,3,5-triazin-6-yl, 2-fluoro-4-(3-(2-sulfatoethylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl( 2-fluoro-4-(4-(2-sulfatoethylsulfonyl,-phenylamino)-1 f3,5-triazin-6-yl, ...
Two main findings arise from this study: (1) the adenosine A2A receptor antagonist SCH 58261 shows neuroprotective effects in an excitotoxic rat model of HD; and (2) the inhibition of QA-evoked increase in extracellular glutamate seems to be the main mechanism of the effects elicited by SCH 58261.. The finding that SCH 58261 significantly prevented most of the effects induced by the intrastriatal injection of an excitotoxin is in line with some findings suggesting that activation of A2A receptors could participate in the generation of excitotoxicity. Adenosine A2A receptor agonists have been reported indeed to stimulate glutamate release in the rat striatum (Popoli et al., 1995; Corsi et al., 1999). Moreover, in previous experiments, we observed that the intrastriatal injection of the adenosine A2A receptor agonist CGS 21680, together with QA, potentiated QA-induced mortality in a dose-dependent way (50, 75, and 83% of mortality after 3, 6, and 12 nmol QA plus CGS 21680, respectively; P. Popoli, ...
9H-Purin-2-amine, 9-methyl- (9CI) (CAS 5752-08-9) Market Research Report 2018 aims at providing comprehensive data on 9h-purin-2-amine, 9-methyl- (9ci)
While regadenoson has become the vasodilator stress agent of choice and has streamlined and simplified stress protocols in many nuclear stress laboratories, the adverse effect of dyspnea is still experienced by many patients, and even more so by those with COPD and asthma. While patients and practitioners should anticipate this symptom, several studies have shown that the subjective experience of dyspnea is not correlated with and is not caused by bronchoconstriction. Available data from observational studies as well as controlled clinical trials, as summarized in Table 1, indicate that the use of regadenoson in patients with mild to moderate asthma and mild to moderate COPD is safe. The current data in patients with severe COPD, while limited, are reassuring and indicate that regadenoson is probably safe, particularly in those with stable lung disease. Clinical data are limited in COPD patients who require 24-hour/day home oxygen administration, have previously been intubated for respiratory ...
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BioAssay record AID 243741 submitted by ChEMBL: Inhibition of [3H]CGS-21680 binding to Adenosine A2A receptor expressed in CHO cells.
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for h
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DESCRIPTION: (Adapted from the Investigators Abstract): Adenosine administered as an aerosol to asthmatics causes bronchoconstriction, while in non-asthmatics adenosine causes bronchodilation. This occurs because the activation of A2B adenosine receptors on sensitized mast cells triggers degranulation, releasing histamine, leukotrienes, and other allergic mediators. A2B adenosine receptors are blocked by theophylline, a xanthine that is effective in treating asthma. However, theophylline is a non-selective antagonist of all four adenosine receptor subtypes and produces side effects due primarily to A1 receptor blockade, including insomnia and diuresis. The incidence of asthma is increasing and current treatment options are limited. New drugs that are potent and selective antagonists of A2B adenosine receptors have great potential for the treatment of asthma and other allergic diseases. Adenosine Therapeutics, LLC owns the first potent and selective A2B antagonists. The purpose of this phase I ...
Disclosed are processes for the synthesis of novel compounds that are A.sub.2B adenosine receptor antagonists, having the structure of Formula I or Formula II: ##STR00001## by cyclizing a compound of the formula (3): ##STR00002##
TY - JOUR. T1 - Modulating P1 Adenosine Receptors in Disease Progression of SOD1G93A Mutant Mice. AU - Armida, Monica. AU - Matteucci, Alessandra. AU - Pèzzola, Antonella. AU - Baqi, Younis. AU - Müller, Christa E. AU - Popoli, Patrizia. AU - Potenza, Rosa Luisa. PY - 2019/5. Y1 - 2019/5. N2 - Amyotrophic lateral sclerosis (ALS) is a fatal progressing neurodegenerative disease; to date, despite the intense research effort, only two therapeutic options, with very limited effects, are available. The purinergic system has been indicated as a possible new therapeutic target for ALS, but the results are often contradictory and generally confused. The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. Body weight, motor performance ...
Permanent functional deficits following spinal cord injury (SCI) arise both from mechanical injury and from secondary tissue reactions involving inflammation. Enhanced release of adenosine and glutamate soon after SCI represents a component in the sequelae that may be responsible for resulting functional deficits. The role of adenosine A2A receptor in central ischemia/trauma is still to be elucidated. In our previous studies we have demonstrated that the adenosine A2A receptor-selective agonist CGS21680, systemically administered after SCI, protects from tissue damage, locomotor dysfunction and different inflammatory readouts. In this work we studied the effect of the adenosine A2A receptor antagonist SCH58261, systemically administered after SCI, on the same parameters. We investigated the hypothesis that the main action mechanism of agonists and antagonists is at peripheral or central sites. Spinal trauma was induced by extradural compression of SC exposed via a four-level T5-T8 laminectomy in mouse.
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Recent evidence indicates that topical application of adenosine A(2A) receptor agonists, unlike growth factors, increases the rate at which wounds close in normal animals and promotes wound healing in diabetic animals as well as growth factors, yet neither the specific adenosine receptor involved no …
Adenosine A2A Receptor Agonist Polydeoxyribonucleotide Alleviates Interstitial Cystitis-Induced Voiding Dysfunction by Suppressing Inflammation and Apoptosis in Rats
View mouse Adora1 Chr1:134199225-134235431 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
View mouse Adora2a Chr10:75316877-75334784 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
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... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
1992). "Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature.". Eur. J. ... 1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics 11 (1): ... a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". Eur. J. Pharmacol. 213 ...
... which triggers intracellular signal transduction via both adenosine A1 and A2 receptors[disambiguation needed], and that the ... Moreover, minoxidil contains a nitric oxide moiety and may act as a nitric oxide agonist. This may cause follicles in the ... expression of sulfonylurea receptor 2B in dermal papilla cells might play a role in the production of adenosine. Minoxidil ... Minoxidil is an adenosine 5'-triphosphate-sensitive potassium channel opener, causing hyperpolarization of cell membranes. ...
... the therapeutic potential for both agonists and antagonists of the adenosine receptors was highlighted for A2 receptors, and in ... Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. Notable adenosine ... In order to be able to characterize the function of adenosine A2 receptors, potent and selective A2-receptor antagonists were ... adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti- ...
The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... Experimental evidence suggests that adenosine and adenosine agonists can activate Trk receptor phosphorylation through a ... All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... Adenosine is an endogenous agonist of the ghrelin/growth hormone secretagogue receptor. However, while it is able to increase ...
Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an ... Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. Thus, it may prove ... The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... A1 receptors are also present in smooth muscle throughout the vascular system. The adenosine A1 receptor has been found to be ...
These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. Signalization in ... It has been shown that collagen, exposed after the injury to the endothelial cover of the vessel, plays as an agonist in ... cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). ... TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. Both receptors mediate phospholipase C ...
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... This is a valuable guide to design potential 5HT1D receptor agonists. When sumatriptan binds there is major conformational ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... Goadsby, P.J., Serotonin 5-HT1B/1D receptor agonists in migraine - Comparative pharmacology and its therapeutic implications. ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... highly potent 5-HT1D receptor agonist.". Journal of medicinal chemistry 42 (3): 526-31. PMID 9986723. doi:10.1021/jm9805945. ... 5-HT1D receptor (5-hidroksitriptaminski (serotoninski) receptor 1D, HTR1D) je 5-HT receptor. On je kodiran istoimenim genom.[1] ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • ...
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ...
... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... 1997). „Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... Gao ZG, Jacobson KA (2007). „Emerging adenosine receptor agonists". Expert Opinion on Emerging Drugs. 12 (3): 479-92. PMID ... Adenosine Receptors: A3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...
PAR1 and PAR4 receptors), platelet-derived thromboxane A2 (TxA2) (TP receptor) and ADP (P2Y1 and P2Y12 receptors) that is ... Adenosine acts by binding to purinergic receptors and influencing adenylyl cyclase activity and the formation of cAMP and PKA ... In general terms, platelet activation initiated by agonist takes to a signaling cascade that leads to an increase of the ... Therefore, there are four main transmembrane receptor types: G protein coupled receptors (GPCRs), tyrosine kinase receptors ( ...
... the DP1-dependent stimulation of adenosine formation and subsequent simulation of the Adenosine A2A receptor by adenosine. In ... "Characterization of the recombinant human prostanoid DP receptor and identification of L-644,698, a novel selective DP agonist ... thromboxane A2, with PGD2 being more than 100-fold more potent than PGE2 in binding to and stimulating DP1. (http://www. ... Prostaglandin receptors Prostanoid receptors Prostaglandin DP2 receptor Eicosanoid receptor GRCh38: Ensembl release 89: ...
... and reduces inflammation and innate immunity nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors ... Daly JW, Jacobson KA, Ukena D (1987). "Adenosine receptors: development of selective agonists and antagonists". Prog Clin Biol ... or rather its adenosine-antagonist behavior). Mandal, Ananya. "Caffeine Pharmacology". Website Medical News. Archived from the ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
In vitro, D5 receptors show high constitutive activity that is independent of binding any agonists. D5 receptor is highly ... Prado C, Contreras F, González H, Díaz P, Elgueta D, Barrientos M, Herrada AA, Lladser Á, Bernales S, Pacheco R (2012). " ... Mello, F. G. (October 1978). "The Ontogeny of Dopamine-Dependent Increase of Adenosine 3',5'-Cyclic Monophosphate in the Chick ... It belongs to the D1-like receptor family along with the D1 receptor subtype. D5 receptor is a subtype of the dopamine receptor ...
... its acidification of endosomes is critical in receptor endocytosis as low pH tends to drive ligand release as well as receptor ... Adenosine triphosphate (ATP) is then hydrolyzed by the V1 domain of the enzyme, enabling both the rotation of the central stalk ... Isoforms a1 and a2 target V-ATPase intracellularly, to synaptic vesicles and endosomes respectively. Subunits a3 and a4, ... The lipophilic agent xylometazoline, an alpha-adrenoreceptor agonist, displayed an increased effect when administered after ...
... receptors are glutamate receptors particularly important in long-term potentiation in neurons. These receptors have been linked ... Funk, C.K. and Koob, G.F. (2007). A CRF2 agonist administered into the central nucleus of the amygdala decreases ethanol self- ... Katsura, M., Shibasaki, M., Hayashida, S., Torigoe, F., Tsujimura, A., Ohkuma, S. (2006) Increase in expression of a1 and a2/d1 ... Pandey, S.C., Roy, A., Zhang, H. (2003). The decreased phosphorylation of cyclic adenosine monophosphate (cAMP) response ...
... s secrete thromboxane A2, which acts on the platelet's own thromboxane receptors on the platelet surface (hence the so- ... After adding an agonist, the platelets aggregate, resulting in greater light transmission, which is detected by the photocell. ... "Differential Sensitivity of Various Markers of Platelet Activation with Adenosine Diphosphate". BioNanoScience. 9 (1): 53-58. ... These receptors trigger intraplatelet signaling, which converts GPIIb/IIIa receptors to their active form to initiate ...
The cytosolic PLA2 set (i.e. cPLA2s) of PLA2 enzymes (cPLA2; see Phospholipase A2#Cytosolic phospholipases A2) in particular ... Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... As a second drug added to corticosteroids, leukotriene inhibitors appear inferior to Beta2-adrenergic agonist drugs in the ... may serve as a mobile lid over ALOX5's substrate-binding site An Adenosine triphosphate (ATP) binding site; ATP is crucial for ...
Such drugs are called receptor agonists. An example of a receptor agonist is Valium, a benzodiazepine that mimics effects of ... Adenosine. Ado. Adenosine receptors. -. Small: Purine. Adenosine triphosphate. ATP. P2Y receptors. P2X receptors. ... "Hindbrain noradrenergic A2 neurons: diverse roles in autonomic, endocrine, cognitive, and behavioral functions". American ... NMDA receptors, kainate receptors, AMPARs. Small: Amino acids. Gamma-aminobutyric acid. GABA. GABAB receptors. GABAA receptors ...
... trienoic acid as a thromboxane A2 receptor antagonist with minimal intrinsic activity". British Journal of Haematology. 101 (1 ... Synthetic BLT2 agonists may be useful for speeding the healing of chronic ulcerative wounds, particularly in patients with, for ... to inhibit platelet aggregation responses to various agents by stimulating platelets to raise their levels of Cyclic adenosine ... BLT1 receptor) and its low affinity BLT2 receptor (Kd=23 nM); both receptors are G protein coupled receptors that, when ligand- ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as ... All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor ... Thromboxane A2 receptor. TP. TXA=PGH2,,PGD2=PGE2=PGF2α=PGI2[14]. contractile. Gq alpha subunit. stimulates PLC & IP3; raises Ca ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... leukotriene receptor activity. • cysteinyl leukotriene receptor activity. • galanin receptor activity. Cellular component. • ... "Leukotriene Receptors: CysLT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Cysteinyl leukotriene receptor 2, also termed CYSLTR2, is a receptor for cysteinyl leukotrienes (LT) (see leukotrienes# ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. DP2 has little or no such amino acid ... prostaglandin D receptor activity. • G-protein coupled receptor activity. • prostaglandin J receptor activity. • prostaglandin ... "Prostanoid Receptors: DP2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ...
Most commonly, enzymes known as adenosine deaminases acting on RNA (ADARs) catalyze adenosine to inosine (A to I) transitions. ... miR-382 is the target for the dopamine receptor D1 (DRD1), and its overexpression results in the upregulation of DRD1 and delta ... Choi WY, Giraldez AJ, Schier AF (October 2007). "Target protectors reveal dampening and balancing of Nodal agonist and ... "High mobility group A2 protein and its derivatives bind a specific region of the promoter of DNA repair gene ERCC1 and modulate ...
Opioid receptor agonist. *Opioid receptor antagonist. *Enkephalinase inhibitor. Other. *Adenosine reuptake inhibitor (AdoRI) ... Newton, David; Alasdair Thorpe; Chris Otter (2004). Revise A2 Chemistry. Heinemann Educational Publishers. p. 1. ISBN 0-435- ... Major receptor types studied in pharmacology include G protein coupled receptors, ligand gated ion channels and receptor ... Systems, receptors and ligands[edit]. This section needs expansion. You can help by adding to it. (July 2019) ...
ADP受體/P2Y12(英語:P2Y12)抑制劑(英語:Adenosine diphosphate receptor inhibitor)類 ... 阿司匹林低劑量服用時能阻止血小板中血栓素A2的合成,這會在受影響的血小板的生命周期(約8-9天)內抑制血小板聚集。阿司匹林的這種抗血栓作用可用於降低心臟病發生率。[122] 每天服用40 mg的阿司匹林能顯著抑制血栓
The cytosolic PLA2 set (i.e. cPLA2s) of PLA2 enzymes (cPLA2; see Phospholipase A2#Cytosolic phospholipases A2) in particular ... Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... As a second drug added to corticosteroids, leukotriene inhibitors appear inferior to Beta2-adrenergic agonist drugs in the ... An Adenosine triphosphate (ATP) binding site; ATP is crucial for ALOX5's metabolic activity ...
... a selective agonist for PGE2 receptor subtype 3". Journal of Leukocyte Biology. 68 (2): 187-93. PMID 10947062.. ... TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... "Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ...
It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor.[28] For the signal to be ... Ephrins (A1, A2, A3, A4, A5, B1, B2, B3). *Erythropoietin (see here instead) ... Agonists: des(1-3)IGF-1. *Insulin-like growth factor-1 (somatomedin C) ... It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). ...
Sunitinib, an inhibitor of the receptors for FGF, PDGF and VEGF is also based on early studies on TKIs aiming at VEGF receptors ... TKIs operate by four different mechanisms: they can compete with adenosine triphosphate (ATP), the phosphorylating entity, the ... Ephrins (A1, A2, A3, A4, A5, B1, B2, B3). *Erythropoietin (see here instead) ... Agonists: des(1-3)IGF-1. *Insulin-like growth factor-1 (somatomedin C) ...
Such drugs are called receptor agonists. An example of a receptor agonist is morphine, an opiate that mimics effects of the ... adenosine triphosphate (ATP), adenosine Others: acetylcholine (ACh), anandamide, etc. In addition, over 50 neuroactive peptides ... Rinaman L (February 2011). "Hindbrain noradrenergic A2 neurons: diverse roles in autonomic, endocrine, cognitive, and ... Direct-binding agonists can be further characterized as full agonists, partial agonists, inverse agonists. Direct agonists act ...
Vilazodone is a 5-HT1A receptor partial agonist while vortioxetine is a 5-HT1A receptor agonist and 5-HT3 and 5-HT7 receptor ... PMID 21701626.CS1 maint: multiple names: authors list (link) Romero-Martínez Á, Murciano-Martí S, Moya-Albiol L (May 2019). "Is ... One such possible mechanism is the increased levels of cyclic adenosine monophosphate (cAMP) as a result of interference with ... Fluvoxamine is an agonist of the σ1 receptor, while sertraline is an antagonist of the σ1 receptor, and paroxetine does not ...
Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ... A myriad of agonists have also been shown to induce the translocation of PKCε from the cytosolic to particulate fraction in ... Perjés Á, Skoumal R, Tenhunen O, Kónyi A, Simon M, Horváth IG, Kerkelä R, Ruskoaho H, Szokodi I (2014). "Apelin increases ... Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ...
Adenosine A2 Receptor Agonists. Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter ... It has lower affinity for non-A2A adenosine receptor subtypes thought to be associated with some of the adverse effects ... associated with non-selective adenosine receptor agonists, which increase extracellular adenosine by blocking its uptake into ... Regadenoson is an A2AR agonist that is a coronary vasodilator. It is chemically described as adenosine, 2-[4-[(methylamino) ...
Adenosine A2 Receptor Agonists. Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter ...
Adenosine. Adenosine A2 Receptor Agonists. Coronary Artery Disease. Myocardial Ischemia. Coronary Disease. Heart Diseases. ... Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
2-Alkynyl derivatives of Adenosine-5-N-ethyluronamide (NECA): selective A2 adenosine receptor agonists with potent inhibitory ... 2-Alkynyl derivatives of Adenosine-5-N-ethyluronamide (NECA): selective A2 adenosine receptor agonists with potent inhibitory ... The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to ... The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to ...
To understand the molecular mechanism of G-protein-mediated signalling, solved structures of receptors in inactive ... G-protein-coupled receptors (GPCRs) are essential components of the signalling network throughout the body. ... Adenosine A2 Receptor Agonists * Ligands * Receptor, Adenosine A2A * Receptors, Adrenergic, beta-2 ... Structure of the adenosine A(2A) receptor bound to an engineered G protein Nature. 2016 Aug 4;536(7614):104-7. doi: 10.1038/ ...
... adenosine receptor (AR) based on bovine rhodopsin predicted a protein structure that was very similar to the recently ... Adenosine A2 Receptor Agonists * Adenosine A2 Receptor Antagonists * Receptor, Adenosine A2A * Receptors, G-Protein-Coupled ... Evaluation of homology modeling of G-protein-coupled receptors in light of the A(2A) adenosine receptor crystallographic ... Automatic agonists docking to both a new homology modeled receptor and the A(2A) AR crystallographic structure produced similar ...
0 (Adenosine A2 Receptor Antagonists); 0 (Antiparkinson Agents); 0 (Dopamine Agonists); 0 (Indoles); 0 (Purines); 0 (Receptor, ... 0 (Adenosine A2 Receptor Antagonists); 0 (Antiparkinson Agents); 0 (Dopamine Agonists); 0 (Indoles); 0 (Purines); 030PYR8953 ( ... The adenosine A2A receptor antagonist, istradefylline enhances the anti-parkinsonian activity of low doses of dopamine agonists ... Antagonistas do Receptor A2 de Adenosina/uso terap utico. Antiparkinsonianos/uso terap utico. Agonistas de Dopamina/uso terap ...
Adenosine A2A Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2A Receptor Antagonists (0) see Adenosine A2 ... Adenosine A2B Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2B Receptor Antagonists (0) see Adenosine A2 ... Adenosine A2 Receptor Agonists (4) • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. MeSH ... Adenosine A2 Receptor Antagonists (8) • Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS. ...
1991) Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors. J Med Chem 34(12):3388-3390. ... 2007) New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains ... 2010) A novel highly selective adenosine A1 receptor agonist VCP28 reduces ischemia injury in a cardiac cell line and ischemia- ... Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Celine ...
Adenosine A2 Receptor Agonists. 1. 2017. 30. 0.050. Why? Purinergic P2X Receptor Antagonists. 1. 2017. 32. 0.050. Why? ... Nuclear Receptor Subfamily 1, Group F, Member 3. 1. 2012. 106. 0.130. Why? ... NK Cell Lectin-Like Receptor Subfamily B. 1. 2014. 71. 0.160. Why? ...
2007) Adenosine A1 and A2 receptor agonists reduce endotoxin-induced cellular energy depletion and oedema formation in the lung ... Plasma adenosine was decreased in females (Table 3, Females). Plasma adenosine is produced from ATP and ADP released from cell ... 2011) P2 receptors and extracellular ATP: A novel homeostatic pathway in inflammation. Front Biosci (Schol Ed) 3:1443-1456. ... 2015) Bile acid-activated receptors, intestinal microbiota, and the treatment of metabolic disorders. Trends Mol Med 21(11):702 ...
... selective A2A agonist. Join researchers using high quality CGS 21680 from Abcam and achieve your mission, faster. ... CGS 21680C, an A2 selective adenosine receptor agonist with preferential hypotensive activity.. J Pharmacol Exp Ther 251:47-55 ... Adenosine receptors and their ligands.. Naunyn Schmiedebergs Arch Pharmacol 362:382-91 (2000). Read more (PubMed: 11111832) » ... Agonists, activators, antagonists and inhibitors. Lysates. Multiplex miRNA assays. By research area. Cancer. Cardiovascular. ...
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. ... Subscribe to New Research on Adenosine-5-(N-ethylcarboxamide) A stable adenosine A1 and A2 receptor agonist. Experimentally, ... 05/01/1998 - "The effect of serotonergic agents was studied on the adenosine A2 receptor agonist NECA-induced catalepsy in mice ... 01/01/1993 - "The adenosine agonists 5-N-ethylcarboxamide-adenosine (NECA), N6-phenylisopropyladenosine (PIA) and N6- ...
1994) In vivo and ex vivo effects of adenosine A1 and A2 receptor agonists on platelet aggregation in the rabbit. Eur J ... Almost all A2A adenosine receptor agonists and antagonists also have some effects on A1 or A3 receptors (Jacobson et al., 1992 ... 1992) Molecular cloning of the rat A2 adenosine receptor: selective coexpression with D2 dopamine receptors in rat striatum. ... 1996) Adenosine A2 receptor-mediated excitatory actions on the nervous system. Prog Neurobiol 48:167-189. ...
These probes bind to A.sub.2 and A.sub.3 adenosine receptors and aid in quantifying and characterizing the receptors. The ... This application discloses probes for adenosine receptors which are functionalized congeners of the following compound: ##STR1# ... which are agonists for A-1 and A-2 adenosine receptors and the sensitivity for quantitativeanalysis of xanthine amine congeners ... Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors.. UTILITY STATEMENT. The present ...
... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
1996) Adenosine A2 receptor-induced inhibition of leukotriene B4 synthesis in whole blood ex vivo. Br J Pharmacol 117:1639-1644 ... 1D). In fact, the adenosine A2areceptor agonist CGS21680 was shown to be a very potent inhibitor (IC50 of ∼1 nM) of the AA- ... Stimulation of the adenosine A2a receptor with the agonist CGS21680 also completely blocked AA-induced translocation of 5-LO ... 1C). However, when the adenosine A2a receptor agonist CGS21680 was included in these incubations containing ADA, the enhanced ...
Phorbol ester-stimulated adherence of neutrophils to endothelial cells is reduced by adenosine A2 receptor agonists. Felsch, A ... Occupancy of adenosine receptors raises cyclic AMP alone and in synergy with occupancy of chemoattractant receptors and ... Biphasic actions of prostaglandin E(2) on the renal afferent arteriole : role of EP(3) and EP(4) receptors. Tang, L., ... Calcitonin gene-related peptide regulates phosphorylation of the nicotinic acetylcholine receptor in rat myotubes. Miles, K., ...
... an adenosine A1 receptor antagonist. Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. ... a selective adenosine A1 receptor antagonist. The selective adenosine A2 and A3 receptors antagonists did not alter the ... Right atria of adult Wistar rats were used to evaluate the effects of adenosine, ATP and CPA (an adenosine A1 receptor agonist ... Adenosine and ATP exert a negative chronotropic effect in the heart. This study aims to evaluate adenosine and P2 receptors and ...
... 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 ... Levens N, Beil M, Schulz R (1991) Intrarenal actions of the new adenosine agonist CGS 21680A, selective for the A2 receptor. J ... Kim M, Chen SW, Park SW et al (2009) Kidney-specific reconstitution of the A1 adenosine receptor in A1 adenosine receptor ...
Streptozotocin-induced diabetic rats and corresponding controls were chronically treated with the adenosine A2a AR agonist ... Adenosine A2 a receptor stimulation prevents proteinuria in diabetic rats by promoting an anti-inflammatory phenotype without ... This study investigates whether chronic stimulation of the adenosine A2a receptor (A2a AR) protects kidney function in ...
1999) Cardiovascular pharmacology of the adenosine A1/A2-receptor agonist AMP 579: coronary hemodynamic and cardioprotective ... Targeted delivery of interleukin-10, adenosine receptor agonists, or other proteins could be an effective means of limiting ... 1999) The time course of cardioprotection induced by GR79236, a selective adenosine A1-receptor agonist, in myocardial ... 2000) Targeting of rat anti-mouse transferring receptor monoclonal antibodies through blood-brain barrier in mouse. J Pharmacol ...
Adenosine A1 and A2 receptor agonists reduce endotoxin-induced cellular energy depletion and oedema formation in the lung. Eur ... Comparison of the potency of adenosine as an agonist at human adenosine receptors expressed in Chinese hamster ovary cells. ... The adenosine 2A receptor agonist GW328267C improves lung function after acute lung injury in rats. Am J Physiol Lung Cell Mol ... Adenosine protected against pulmonary edema through transporter- and receptor A2-mediated endothelial barrier enhancement. Am J ...
This study explored whether selective pharmacological antagonism of the adenosine A1 receptor subtype synergizes with ESS, ... We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in ... We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in ... We demonstrated that ESS combined with the blockage of A1 receptors increased the magnitude of the endogenous modulation and ...
Agonist activity of 2- and 5′-substituted adenosine analogs and their N6-cycloalkyl derivatives at A1- and A2-adenosine ... Evidence for an A2-subtype adenosine receptor on pancreatic glucagon secreting cells. Br J Pharmacol 1985;86:565-569pmid: ... The Adora1 receptor is activated by adenosine. In mouse islets, adenosine is released by exocytosis (28) and can act on Adora1 ... The adenosine A1 receptor (Adora1) is a G-protein coupled receptor (GPCR) that is involved in maintaining glucose homeostasis ...
1992) The effects of intravenous infusions of selective adenosine A1-receptor and A2-receptor agonists on myocardial ... Lower local concentrations of adenosine have been noted to promote neutrophil recruitment (via the A1 and A3 adenosine receptor ... Adenosine bolus did not attenuate neutrophil influx into the no-reflow area, whereas adenosine infusion demonstrated a trend (p ... Whether maximal adenosine dosages were achieved in clinical studies using intravenous adenosine is also unclear. The AMISTAD ( ...
Montesinos MC Gadangi P Longaker M . Wound healing is accelerated by agonists of adenosine A2 (G alpha S-linked) receptors. J ... Given that adenosine levels and expression of 5′ nucleotidase (an enzyme to convert adenosine monophosphate to adenosine) and A ... Extracellular adenosine acts through multiple G-protein-coupled receptors (A1, A2A, A2B, and A3) 7 to exert important control ... Day YJ Li Y Rieger JM Ramos SI Okusa MD Linden J . A2A adenosine receptors on bone marrow-derived cells protect liver from ...
Adenosine A2 Receptor Agonists Concept Receptors, Adenosine A2 Academic Article Conditional neural knockout of the adenosine A( ... Targeting adenosine A2A receptors in Parkinsons disease. Academic Article Adenosine A2A receptors and metabotropic glutamate 5 ... Adenosine A2A receptor stimulation potentiates nitric oxide release by activated microglia. Academic Article Adenosine A1 and ... Pathophysiological roles for purines: adenosine, caffeine and urate. Academic Article Forebrain adenosine A2A receptors ...
... lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. ... lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. ... The A2a specific agonist CGS21680 stimulated cAMP production but did not alter intracellular calcium concentrations in ... The A2a specific agonist CGS21680 stimulated cAMP production but did not alter intracellular calcium concentrations in ...
... increases in cAMP accumulation with potencies that were highly correlated with their potencies at A2 adenosine receptors. ... ACPD activates an mGluR subtype that potentiates responses to agonists of other receptors that are coupled to adenylate cyclase ... We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker ... Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear ...
  • The discrepancy between the experimentally observed orientation of the antagonist and those obtained by previous antagonist docking is related to the loop structure of rhodopsin being carried over to the model of the A(2A) AR and was rectified when the beta(2)-adrenergic receptor was used as a template for homology modeling. (nih.gov)
  • The encoded protein (the A2A receptor) is abundant in basal ganglia, vasculature, T lymphocytes, and platelets and it is a major target of caffeine, which is a competitive antagonist of this protein. (wikipedia.org)
  • Right atria of adult Wistar rats were used to evaluate the effects of adenosine, ATP and CPA (an adenosine A1 receptor agonist), in the presence and absence of DPCPX, an adenosine A1 receptor antagonist. (ovid.com)
  • The effects of adenosine, CPA and ATP were inhibited by DPCPX, a selective adenosine A1 receptor antagonist. (ovid.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)
  • E)-8-(3-Chlorostyryl)-1,3,7-trimethylxanthine, a caffeine derivative acting both as antagonist of adenosine A2A receptors and as inhibitor of MAO-B. (harvard.edu)
  • A2A antagonist prevents dopamine agonist-induced motor complications in animal models of Parkinson's disease. (harvard.edu)
  • 1. A method of enhancing an immune response in a host, comprising administering to the host an A.sub.2a receptor antagonist in combination or alternation with a checkpoint inhibitor. (patents.com)
  • Where indicated, DA levels were restored by bath application of exogenous DA (20 μM), or action of endogenous DA was blocked by application of a specific D1 receptor antagonist (10 μM SCH23390). (frontiersin.org)
  • Neither the change in [Ca2+]i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2-aminoethyl)carbamoylmethoxy]-phenyl}-1,3-dipropylxanthine (XAC). (rti.org)
  • NECA was chosen for the study because caffeine is a nonselective adenosine receptor antagonist, and it is not known which of the four subtypes of adenosine receptors may be involved in an effect of caffeine on fatigue. (innovations-report.com)
  • Simultaneous infusion of 10(-7) M 9-cyclopentyl-1,3-dipropylxanthine, a selective adenosine A1 receptor antagonist, markedly inhibited the diuretic and natriuretic effects of intrarenal adenosine. (aspetjournals.org)
  • Theophylline** Theophylline is an adenosine receptor antagonist. (rutgers.edu)
  • These cells possess a high density of A1 adenosine receptors (Bmax = 0.8-0.9 pmol/mg of protein), as measured by both agonist and antagonist radioligands. (aspetjournals.org)
  • Inhibition of adenylate cyclase by (R)-PIA was attenuated by the A1 receptor antagonist XAC and following inactivation of Gi with pertussis toxin (100 ng/ml). (aspetjournals.org)
  • A vasopressin antagonist that binds to the V2-receptor of LLC-PK, renal epithelial cells is highly laterally mobile but does not effect ligand-induced receptor immobilization. (springer.com)
  • Xanthine amine congener, a specific A1 receptor antagonist, failed to reverse the suppression by adenosine of tumor necrosis factor release, whereas CGS15943A, an A2 receptor antagonist, did reverse suppression by adenosine and 5-n-ethylcarboxamidadenosine. (duke.edu)
  • SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. (elsevier.com)
  • Recently, the A2A receptor antagonist 3-chlorostyrylcaffeine has been reported to be a potent inhibitor of monoamine oxidase B. An inverse relationship between non-selective adenosine receptor antagonists, the consumption of caffeine and the risk of developing Parkinson's disease has been indicated from epidemiological studies. (wikipedia.org)
  • In recent studies, the consumption of caffeine-containing beverages and a certain non-xanthine A2A receptor antagonist appear to possibly have some protective effects from Alzheimer's disease. (wikipedia.org)
  • Broad reviews from 2006 have been focusing on adenosine receptors as therapeutic targets, adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti-inflammatories and many more. (wikipedia.org)
  • Although incubation of monocytes with IB-MECA, a compound purported to act as an adenosine A 3 receptor agonist, reduced LPS-induced TNF-α production, this effect of IB-MECA was inhibited by the A 2A selective antagonist ZM241385 but not by the A 3 receptor antagonist MRS1220. (elsevier.com)
  • To address the signal transduction mechanism responsible for the anti-inflammatory effects of ATL313 in equine monocytes, production of cAMP was compared in the presence and absence of either the adenosine A 2A receptor antagonist ZM241385 or the adenosine A 2B receptor antagonist MRS1706. (elsevier.com)
  • 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)
  • Contractions to ATP and αβ-meATP were blocked by NF449, a selective P2X1 receptor antagonist. (nottingham.ac.uk)
  • MRS2578, a selective P2Y6 receptor antagonist, had no effect on contractions to UTP. (nottingham.ac.uk)
  • ADP induced endothelium-dependent vasorelaxation which was inhibited by MRS2179, a selective P2Y1 receptor antagonist, or SCH58261, a selective adenosine A2A receptor antagonist. (nottingham.ac.uk)
  • Metod: Laser-Dِoppler flowmetry technique was used to study pial vessels blood flow responses to adenosine receptors agonists and antagonist. (phypha.ir)
  • Adenosine (general agonist), NECA (A2Aand A2B receptor agonist) and CGS-21380(A2Aselective agonist), were used in absence and presence of A2A receptors- selective antagonist, ZM-243185, in naive and morphine-dependent rats. (phypha.ir)
  • DPCPX is a potent and selective A1 adenosine receptor antagonist, both in vitro and in vivo. (emmx.com)
  • 1,3-Dipropyl-8-phenylxanthine is a selective A1 adenosine antagonist. (emmx.com)
  • PSB 36 is a Potent and selective A1 adenosine receptor antagonist with binding affinities of 0.12, 187, 552, 6500 and 2300 nM for rA1, hA2B, rA2A, rA3 and hA3 receptors respectively. (emmx.com)
  • SLV 320 is a potent and selective adenosine A1 receptor antagonist (Ki values are 1, 200, 398 and 3981 nM at human A1, A3, A2A and A2B receptors respectively). (emmx.com)
  • PSB 1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. (emmx.com)
  • NMDA receptor antagonist. (emmx.com)
  • Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused mainly on the role of adenosine receptors in the heart, and led to several randomized controlled trials using these receptor antagonists to treat bradyasystolic arrest. (wikipedia.org)
  • Together with complimentary pharmacological studies, these data suggest that A 2A receptors play a prominent role in the development of ischemic injury within brain and demonstrate the potential for anatomical and functional neuroprotection against stroke by A 2A receptor antagonists. (jneurosci.org)
  • Indeed, when adenosine is eliminated from PMN suspensions by the addition of adenosine deaminase, or when cells are incubated with adenosine A 2a receptor antagonists, important quantities (40-80 pmol/10 6 cells) of 5-lipoxygenase products are synthesized by PMN incubated with 1 to 5 μM exogenous AA. (aspetjournals.org)
  • This AA-induced Ca 2+ mobilization, as well as the corresponding 5-lipoxygenase translocation and stimulation of LT synthesis, was blocked efficiently by the LT synthesis inhibitor MK0591, the LTB 4 receptor antagonists CP105696 and LY223982, and the LTA 4 hydrolase inhibitor SC57461A. (aspetjournals.org)
  • Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. (ovid.com)
  • The selective adenosine A2 and A3 receptors antagonists did not alter the chronotropic response of adenosine. (ovid.com)
  • Neuroprotection by caffeine and more specific A2A receptor antagonists in animal models of Parkinson's disease. (harvard.edu)
  • Monoamine oxidase B inhibition and neuroprotection: studies on selective adenosine A2A receptor antagonists. (harvard.edu)
  • Adenosine A2A antagonists as neurotherapeutics: crossing the bridge. (harvard.edu)
  • Therapeutic potential of adenosine A(2A) receptor antagonists in Parkinson's disease. (harvard.edu)
  • Adenosine A2A receptor antagonists for Parkinson's disease: rationale, therapeutic potential and clinical experience. (harvard.edu)
  • Described are uses of A.sub.2a adenosine receptor antagonists and agonists to provide long term modulation of immune responses. (patents.com)
  • A.sub.2a receptor antagonists in particular are provided to enhance immune responses by reducing T-cell mediated tolerance to antigenic stimuli and agonists are provided to enhance effectiveness of immunosuppressive agents. (patents.com)
  • 0004] This application relates to uses of A.sub.2a adenosine receptor agonists and antagonists to modulate T-cell mediated tolerance to antigenic stimuli. (patents.com)
  • Stably transfected cell lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. (garvan.org.au)
  • Additionally, adenosine receptor antagonists blocked mGluR-mediated increases in cAMP accumulation with potencies that were highly correlated with their potencies at A2 adenosine receptors. (jneurosci.org)
  • Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. (wikipedia.org)
  • Notable adenosine A2A receptor antagonists include caffeine, theophylline and istradefylline. (wikipedia.org)
  • Most of the therapeutic applications are connected to agonists, but the main focus with antagonists are diseases connected to motor skills, learning and memory, for example Parkinson's and Alzheimer's. (wikipedia.org)
  • Recently, selective A2A receptor antagonists are used in treatment of diseases such as Parkinson's disease, ischemia, and multiple sclerosis. (wikipedia.org)
  • Selective A2A receptor antagonists are believed to be neuroprotectors for their ability to reduce neuroinflammation. (wikipedia.org)
  • Selective A2A receptor antagonists have shown to be beneficial for enhancing the therapeutic effects of L-DOPA and reducing dyskinesia from long-term L-DOPA treatment. (wikipedia.org)
  • Trial results indicated that the viability of A2A receptor antagonists have potential advantages over the current standard treatments for Parkinson's disease. (wikipedia.org)
  • A2A receptor antagonists may prevent hepatic cirrhosis, and pentoxifylline may inhibit phosphodiesterase and provide renal protection. (wikipedia.org)
  • The A2A receptor antagonists may be used for treatment of attention deficit hyperactivity disorder (ADHD), because of the receptors ability to regulate neurotransmission in the basal ganglia and cortex, particularly dopaminergic and glutamatergic signaling. (wikipedia.org)
  • In 1992, the therapeutic potential for both agonists and antagonists of the adenosine receptors was highlighted for A2 receptors, and in 2001 the therapeutic potential for adenosine antagonists was highlighted. (wikipedia.org)
  • Several attempts have been made by using virtual screening to identify potent A2A adenosine receptor antagonists. (wikipedia.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)
  • They are differentiated by the rank order potency of adenosine agonists and the affinities for antagonists. (asahq.org)
  • [12-14] In addition to the lack of selective agonists and antagonists for those receptors, the effects of adenosine agonists on non-nociceptive transmission, such as impairment of motor function and locomotor depression, limited behavioral studies characterizing the type of adenosine receptors involved in antinociception and sometimes led to conflicting interpretations and conclusions. (asahq.org)
  • Results of experiments performed with selective adenosine receptor antagonists indicated that functional effects of ATL313 were via stimulation of A 2A receptors. (elsevier.com)
  • Results of experiments performed with one of the adenosine receptor agonists (ATL313) and selective adenosine receptor antagonists confirmed that inhibition of LPS-induced production of TNF-α occurred via stimulation of A 2A receptors. (elsevier.com)
  • Evidence for the involvement of A1 (inhibitory) and A2 (stimulatory) adenosine receptors in regulating cell growth of these tumor cells was obtained through plating efficiency studies based on the relative potency of adenosine agonists and antagonists. (nus.edu.sg)
  • By the chemical reaction of different xantine type molecules and [11C] methyl iodide we produced several A2A adenosine receptor specific antagonists for in vivo testing the receptor ligand interactions. (otka-palyazat.hu)
  • The distinction between receptor-binding sites for agonists and antagonists underpins the pharmacological differences between these two classes of ligands. (pianolarge.cf)
  • 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)
  • 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)
  • Background Despite the clear cardioprotective effects of adenosine, when administered prior to ischemia, studies on cardioprotection by adenosine when administered at reperfusion have yielded contradictory results in both pre-clinical and clinical settings. (onlinejacc.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)
  • The effects of adenosine on water and sodium excretion. (aspetjournals.org)
  • The effects of adenosine on glomerular filtration rate and renal blood flow are well documented, but its effects on water and sodium excretion are less well established. (aspetjournals.org)
  • The diuretic and natriuretic effects of adenosine during intrarenal infusion were of a similar order of magnitude in animals maintained for 3 weeks on no sodium, normal sodium or high sodium diet, and did not correlate with plasma renin activity. (aspetjournals.org)
  • These findings suggest that, in the rat, the diuretic and natriuretic effects of adenosine are 1) fully expressed only during intrarenal administration, 2) absent during intra-aortic administration, 3) not related to prior sodium intake or sodium balance, 4) mediated by the adenosine A1 receptor and 5) dissociated from its effects on glomerular filtration and renal plasma flow. (aspetjournals.org)
  • Direct effects of adenosine A2 receptor activation on renal function were examined in dogs. (umin.ac.jp)
  • 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)
  • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
  • The mechanism of AA-induced stimulation of LT synthesis observed in the absence of extracellular adenosine was investigated. (aspetjournals.org)
  • The stimulation of human leukocytes by various agents such as calcium ionophores, soluble agonists, or phagocytic stimuli results in the biosynthesis of the bioactive arachidonic acid (AA)-derived leukotrienes (LTs). (aspetjournals.org)
  • Adenosine A2 a receptor stimulation prevents proteinuria in diabetic rats by promoting an anti-inflammatory phenotype without affecting oxidative stress. (sigmaaldrich.com)
  • This study investigates whether chronic stimulation of the adenosine A2a receptor (A2a AR) protects kidney function in insulinopenic diabetic rats. (sigmaaldrich.com)
  • Adenosine A2A receptors in neuroadaptation to repeated dopaminergic stimulation: implications for the treatment of dyskinesias in Parkinson's disease. (harvard.edu)
  • Adenosine A2A receptor stimulation potentiates nitric oxide release by activated microglia. (harvard.edu)
  • Activation of nucleotide receptors with extracellular ATP and nucleotide analogues increased intracellular calcium concentration ([Ca2+]i) primarily by release of intracellular calcium stores, with relative potency of agonists similar to that seen for stimulation of Na-K-Cl cotransport. (rti.org)
  • To address possible mechanisms for stimulation of Na-K-Cl cotransport by the nucleotide receptor, I-125 efflux and patch-clamp studies were used to measure chloride secretion. (rti.org)
  • Now, a team of researchers from the University of South Carolina has hypothesized that the blockade of adenosine receptors by caffeine may be the most likely mechanism of CNS stimulation and delayed fatigue. (innovations-report.com)
  • 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)
  • Theophylline-induced respiratory recovery following cervical spinal cord hemisection is augmented by serotonin 2 receptor stimulation. (rutgers.edu)
  • The present study was designed to specifically determine if concurrent stimulation of 5-HT2 receptors may enhance motor recovery induced by theophylline alone. (rutgers.edu)
  • CGS 21680C induced renin release and tachycardia that were blocked by propranolol, indicating these effects of A2 receptor stimulation appeared to be indirect. (umin.ac.jp)
  • The results showed that neither the stimulation nor the blockade of adenosine A2A receptors modified the progressive loss of motor skills or survival of mSOD1G93A mice. (elsevier.com)
  • These results demonstrate that adenosine receptor stimulation differentially modulates the LPS-induced production of IL-10, TNF-α, and NO in vitro and in vivo. (utmb.edu)
  • Adenosine antagonises the effect of ATP by stimulation of adenosine receptors suppressing the pro-inflammatory response (14-17). (deepdyve.com)
  • Stimulation of the A1 adenosine receptor induces two distinct physiological responses. (justia.com)
  • Stimulation of the adenosine A1 receptor accordingly shortens the duration and decreases the amplitude of the action potential of AV nodal cells and subsequently prolongs the refractory period of the cells. (justia.com)
  • Extracellular adenosine gathers in response to cellular stress and breakdown through interactions with hypoxia induced HIF-1α. (wikipedia.org)
  • Abundant extracellular adenosine can then bind to the A2A receptor resulting in a Gs-protein coupled response, resulting in the accumulation of intracellular cAMP, which functions primarily through protein kinase A to upregulate inhibitory cytokines such as transforming growth factor-beta (TGF-β) and inhibitory receptors (i.e. (wikipedia.org)
  • Extracellular adenosine critically modulates ischemic brain injury, at least in part through activation of the A 1 adenosine receptor. (jneurosci.org)
  • We have recently shown that extracellular adenosine enhances human pulmonary (EC) barrier via activation of adenosine receptors (ARs) in cell cultures. (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)
  • Extracellular adenosine has been widely implicated in adaptive responses to hypoxia. (rupress.org)
  • The generation of extracellular adenosine involves phosphohydrolysis of adenine nucleotide intermediates, and is regulated by the terminal enzymatic step catalyzed by ecto-5′-nucleotidase (CD73). (rupress.org)
  • Guided by previous work indicating that hypoxia-induced vascular leakage is, at least in part, controlled by adenosine, we generated mice with a targeted disruption of the third coding exon of Cd73 to test the hypothesis that CD73-generated extracellular adenosine functions in an innate protective pathway for hypoxia-induced vascular leakage. (rupress.org)
  • ATP (Adenosine Triphosphate) is enzymatically reduced to ADP (adenosine Diphosphate) and to AMP and then to Adenosine in the extracellular space in joints normally . (seniorfitness.com)
  • In addition, platelets with the Q43P β1-tubulin variant had reduced adenosine triphosphate (ATP) secretion, thrombin receptor activating peptide (TRAP)-induced aggregation and collagen adhesion. (bloodjournal.org)
  • In particular, we focus on the interaction of the extracellular nucleotide adenosine triphosphate (ATP) with its receptors P2X1, P2X4, P2X7, P2Y1, and P2Y2 and of adenosine (Ado) with A2A and A3 receptors, as well as their roles in host immune responses. (cdc.gov)
  • The balance of these two molecules can be generated by extracellular nucleotides, such as adenosine 5'-triphosphate (ATP) and adenosine (Ado), which activate the purinergic receptors system. (biomedcentral.com)
  • Activated platelets also release various aggregation mediators including ADP, adenosine triphosphate (ATP), thromboxane A2 (TXA2), serotonin, and various proteins [ 4 ]. (hindawi.com)
  • adenosine-5′-diphosphate (ADP), uridine-5′-triphosphate (UTP) and MRS2768, a selective P2Y2 agonist, were applied cumulatively, while adenosine-5′-triphosphate (ATP) and αβ-methylene-ATP (αβ-meATP) response curves were generated from single concentrations per tissue segment. (nottingham.ac.uk)
  • Several lines of evidence have previously suggested that dopamine-induced changes in motor behavior can be modulated by adenosine analogs acting at the A2 subtype of adenosine receptor in the forebrain. (nih.gov)
  • The stimulant properties of caffeine and various analogs were correlated with the blockade of adenosine receptors. (wikipedia.org)
  • [2] Several behavioral studies have shown that intrathecal administration of adenosine analogs produces antinociception. (asahq.org)
  • Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of these hybrid receptors is still only starting to be unravelled. (wikipedia.org)
  • We report here that the apparent inability of isolated human polymorphonuclear leukocytes (PMNs) to efficiently transform arachidonic acid (AA) is the consequence of A 2a receptor engagement by endogenous adenosine accumulating in incubation media. (aspetjournals.org)
  • Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
  • 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 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)
  • We demonstrated that ESS combined with the blockage of A1 receptors increased the magnitude of the endogenous modulation and postponed the decay of responses that occur during ESS alone. (frontiersin.org)
  • Furthermore, previous studies suggest that glutamate increases cAMP accumulation by a mechanism that is dependent upon the presence of endogenous adenosine. (jneurosci.org)
  • Therefore, we tested the hypothesis that 1S,3R- ACPD-stimulated increases in cAMP accumulation in rat hippocampal slices are dependent upon the presence of endogenous adenosine and are mediated by an mGluR that potentiates cAMP responses to other agonists. (jneurosci.org)
  • Furthermore, we performed a series of studies that suggest that 1S,3R- ACPD activates an mGluR subtype that potentiates responses to agonists of other receptors that are coupled to adenylate cyclase and that 1S,3R- ACPD-stimulated increases in cAMP accumulation in hippocampal slices are mediated by potentiation of the cAMP response to low levels of endogenous adenosine that are continuously present extracellularly. (jneurosci.org)
  • Regulation of plasma membrane ion transport by endogenous purinergic receptors was assessed in a distal renal (A6) cell line. (rti.org)
  • Adenosine is an endogenous nucleoside that regulates many physiological processes by activating one or more adenosine receptor subtypes, namely A 1 , A 2A , A 2B and A 3 . (elsevier.com)
  • Previous studies indicated that extracellular nucleotide metabolites, predominantly adenosine, may trigger an endogenous protective mechanism during hypoxia and ischemia ( 12 - 15 ). (rupress.org)
  • This receptor can bind to several different endogenous ligands, such as b-endorphin, enkephalin , and exogenous opioids. (thefreedictionary.com)
  • The nucleoside adenosine, a potent endogenous anti-inflammatory agent, is deeply involved in inflammatory diseases and, by interaction with the adenosine A 2 receptor (A 2A R) it immediately promotes a mechanism of defence against the inflammatory damage. (scirp.org)
  • We validate that the interaction of VCP746 with the A 1 AR is consistent with a bitopic mode of receptor engagement (i.e., concomitant association with orthosteric and allosteric sites) and that the compound displays biased agonism relative to prototypical A 1 AR ligands. (pnas.org)
  • Thus, this study provides proof of concept that bitopic ligands can be designed as biased agonists to promote on-target efficacy without on-target side effects. (pnas.org)
  • Adenosine receptors and their ligands. (abcam.com)
  • The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. (elsevier.com)
  • It was clear that ligands of adenosine receptors and inhibitors for phosphodiesterase were targets for drug development. (wikipedia.org)
  • The aim of this work was the development and biological test of adenosine receptor ligands which are suitable for in vivo PET examinations. (otka-palyazat.hu)
  • The biological distribution of the ligands as well as their binding kinetics to the receptors was tested in vivo by dynamic PET scans and ex vivo or in vitro experiments. (otka-palyazat.hu)
  • I am interested in how activation of one of these classes of receptor leads to modification of the response to other receptor classes (cross-talk), as well as how different ligands can provoke different signalling profiles at the same receptor (agonist bias). (nottingham.ac.uk)
  • Cannabinoid receptors and their ligands: beyond CB₁ and CB₂. (nottingham.ac.uk)
  • G protein-coupled receptor list: recommendations for new pairings with cognate ligands. (nottingham.ac.uk)
  • Guanylyl cyclase C (GC-C), the receptor for diarrheagenic enterotoxins and the paracrine ligands guanylin and uroguanylin, regulates intestinal secretion. (naver.com)
  • abstract = "Adenosine released into the extracellular space by immunologic and nonimmunologic stimuli has been shown to regulate various immune functions. (utmb.edu)
  • ASP5854 ameliorated A(2A) agonist 2-[p-(2-carboxyethyl) phenethylamino]-5'-N-ethylcarboxamidoadenosine (CGS21680)- and haloperidol-induced catalepsy in mice, with the minimum effective doses of 0.32 and 0.1 mg/kg, respectively, and it also improved haloperidol-induced catalepsy in rats at doses higher than 0.1 mg/kg. (curehunter.com)
  • The selective A 2a receptor agonist CGS21680 was a very potent inhibitor of the AA-induced leukotriene (LT) synthesis, showing an IC 50 of ∼1 nM. (aspetjournals.org)
  • Streptozotocin-induced diabetic rats and corresponding controls were chronically treated with the adenosine A2a AR agonist CGS21680 throughout the four-week diabetes duration. (sigmaaldrich.com)
  • The A2a specific agonist CGS21680 stimulated cAMP production but did not alter intracellular calcium concentrations in transfected 293 cells. (garvan.org.au)
  • Receptor autoradiography with [3H]CGS21680, a specific A2 agonist, and in situ hybridization with A2 cRNA probe in guinea pig brain indicate that the receptor is expressed exclusively in the caudate nucleus. (nih.gov)
  • We show herein that in an HD transgenic mouse model (R6/2), daily administration of CGS21680 (CGS), an A 2A adenosine receptor (A 2A -R)-selective agonist, delayed the progressive deterioration of motor performance and prevented a reduction in brain weight. (elsevier.com)
  • The actions of the A2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity. (wikipedia.org)
  • Role of adenosine A2A receptors in parkinsonian motor impairment and l-DOPA-induced motor complications. (harvard.edu)
  • The role of adenosine A2 receptors in regulation of pial vessels blood flow in anesthetized morphine dependent rats. (phypha.ir)
  • Hoseini M, Hajizadeh S, Fathollahi Y, Golmohammadi M, Erfani B, Heidarian Pour A. The role of adenosine A2 receptors in regulation of pial vessels blood flow in anesthetized morphine dependent rats. (phypha.ir)
  • A series of new 2-alkynyl and 2-cycloalkynyl derivatives of adenosine-5'-N-ethyluronamid(NECA) and of N-ethyl-l'-deoxy-l'-(6-amino-2-hexynyl-9H-purin-9-yl)-b-D-ribofuranuronamid(1e, HENECA), bearing hydroxy, amino, chloro, and cyano groups in the side chain, were synthesized. (unicam.it)
  • The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to compounds endowed with sub-nanomolar affinity in binding studies. (unicam.it)
  • A crystal structure of the A2A receptor bound with the agonist NECA and a G protein-mimic has been published in 2016 (PDB code: 5g53). (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)
  • Agonist displacement profile of [3H]CGS 21680 binding was consistent with an adenosine receptor of the A2 subtype (NECA greater than (R)-PIA greater than CPA greater than (S)-PIA). (nih.gov)
  • The researchers' hypothesis is the foundation of a new study to determine the effects of intracerebroventricular injection of caffeine and the adenosine A1 and A2 receptor agonist 5'-N-ethylcarboxamidoadenosine (NECA) on treadmill run time to fatigue in rats. (innovations-report.com)
  • Adenosine receptor agonists [(R)-PIA, NECA, and (S)-PIA] inhibited isoproterenol-stimulated adenylate cyclase activity in DDT1 MF-2 cell membranes with IC50 values of 62, 538, and 750 nM, respectively. (aspetjournals.org)
  • Finally, adenosine receptor agonists stimulated adenylate cyclase activity by approximately 2-3 fold with the following potency series: PAPA-APEC greater than or equal to NECA greater than (R)-PIA, indicative of their interaction at A2 receptors. (aspetjournals.org)
  • Az A1, A2 és A3 adenozin-receptor expresszió in vivo tanulmányozásához pedig az 18F izotóppal jelölt 5'-N-etil-karboxamidadenonozint (NECA) állítottuk elő. (otka-palyazat.hu)
  • To study the A1, A2 and A3 adenosine receptor expression 18F isotope labeled 5'-N-etil-carboxamidadenosine (NECA) was produced. (otka-palyazat.hu)
  • 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)
  • Results: Adenosine, NECA and CGS-21680 increased pial vessels blood flow in naive and dependent rats dose dependently. (phypha.ir)
  • Responses of pial vessels to adenosine (10-4, 10-5, 10-6 M) and NECA (10-4, 10-5, 10-6 M) were increased significantly in morphine- dependent rats in comparison to naive rats. (phypha.ir)
  • This study explored whether selective pharmacological antagonism of the adenosine A1 receptor subtype synergizes with ESS, thereby increasing motor response. (frontiersin.org)
  • The pharmacological profile and anatomical distribution of this receptor indicate that it is of the A2a subtype. (nih.gov)
  • These results indicate that the adenosine receptor subtype responsible for regulation of LPS-induced cytokine production by equine monocytes is the A 2A receptor. (elsevier.com)
  • We recently reported the cloning of a cDNA (designated RFL9) that encodes a novel A2-adenosine receptor subtype. (pianolarge.cf)
  • Adenosine A1 receptor (ADORA1, also known as A1AR) is one of four subtypes of adenosine receptors that belong to a superfamily of protein G-coupled receptors. (ptglab.com)
  • There are at least two subtypes of adenosine receptors in the heart: A1 and A2. (justia.com)
  • Adenoscan® (adenosine) is an approved pharmacological stress agent indicated as an adjunct to thallium-201 myocardial perfusion scintigraphy in patients unable to exercise adequately. (clinicaltrials.gov)
  • To overcome these pharmacological limitations, we explored the consequences of deleting the A 2A adenosine receptor on brain damage after transient focal ischemia. (jneurosci.org)
  • We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in spinal sensorimotor networks detected as an increased amplitude of spinally-evoked motor potentials and sustained duration of ESS induced activity. (frontiersin.org)
  • Genetic and pharmacological inactivation of the adenosine A2A receptor attenuates 3-nitropropionic acid-induced striatal damage. (harvard.edu)
  • Genetic and pharmacological inactivation of adenosine A2A receptor reveals an Egr-2-mediated transcriptional regulatory network in the mouse striatum. (harvard.edu)
  • Conditional neural knockout of the adenosine A(2A) receptor and pharmacological A(2A) antagonism reduce pilocarpine-induced tremulous jaw movements: studies with a mouse model of parkinsonian tremor. (harvard.edu)
  • This work represents the first cloning of an A2a receptor in a rodent species, offers a complete pharmacological characterization of the receptor and provides an anatomical comparison between binding profile and gene expression of the receptor. (nih.gov)
  • The blockade of A2A receptors has potentially shown to be protective in several tumor models, through pharmacological inhibition or genetic deletion. (wikipedia.org)
  • Biochemical and pharmacological role of A1 adenosine receptors and their modulation as novel therapeutic strategy In: ed Protein Reviews. (eurekaselect.com)
  • We suggest that receptors of purinergic signalling could be ideal candidates for pharmacological targeting to protect against myocardial injury caused by a cytokine storm in COVID-19, in order to reduce systemic inflammatory damage to cells and tissues, preventing the progression of the disease by modulating the immune response and improving patient quality of life. (cdc.gov)
  • Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pharmacology of adenosine receptors: the state of the art. (eurekaselect.com)
  • My central area of research concerns the pharmacology and biochemistry of G protein-coupled receptors (in particular, cannabinoid, adenosine and glutamate) in the CNS and peripheral tissues. (nottingham.ac.uk)
  • 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)
  • Drugs that inhibit ADENOSINE DEAMINASE activity. (nih.gov)
  • In adenosine deaminase-treated PMN, exogenous AA induced Ca 2+ mobilization and the translocation of 5-lipoxygenase to nuclear structures. (aspetjournals.org)
  • We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker dipyridamole enhanced this response. (jneurosci.org)
  • To avoid these undesirable effects, indirect approaches, such as allosteric adenosine receptor modulation or inhibition of adenosine kinase 9,10 or adenosine deaminase, 11 have been examined and show antinociceptive effects in neuropathic rats. (asahq.org)
  • The effects profile and induction of uterine tumors share some similarity with that seen with chronic exposure to dopamine agonists. (bireme.br)
  • The current study investigated the potential for D4 and D5 to elicit dopamine agonist-like effects on estrous cyclicity. (bireme.br)
  • Separate groups of reproductively senescent female Fischer 344 rats (F344) were exposed via vapor inhalation to D4 (700ppm, 9.3mg/L) or D5 (160ppm, 2.1mg/L) or to a diet containing 0.0045, 0.045, or 4.5ppm pergolide mesylate (PM), a potent dopamine agonist used here as a reference substance, from 11 through 24 months of age. (bireme.br)
  • The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, and Parkinson's disease. (wikipedia.org)
  • As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. (wikipedia.org)
  • Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. (nih.gov)
  • In situ hybridization demonstrated that rat A2 adenosine receptor mRNA was co-expressed in the same striatal neurons as D2 dopamine receptor mRNA, and never co-expressed with striatal D1 dopamine receptor mRNA. (nih.gov)
  • The co-expression of D2 dopamine and A2 adenosine receptors in a subset of striatal cells provides an anatomical basis for dopaminergic-adenosinergic interactions on motor behavior. (nih.gov)
  • Adenosine also inhibits the release of most brain excitatory neurotransmitters, particularly dopamine (DA), and may reduce DA synthesis. (innovations-report.com)
  • Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
  • The effect of adenosine and its agonists on nitric oxide synthase (NOS) activity and the production of nitrite induced by lipopolysaccharide (LPS) in RAW 264.7 cells were investigated. (nus.edu.sg)
  • Abebe W, Hussain T, Olanrewaju H et al (1995) Role of nitric oxide in adenosine receptor-mediated relaxation of porcine coronary artery. (springer.com)
  • Experimental studies with experimental rodent models and cultures (cardiac myocytes, endothelial cells) indicate that moderate alcohol exposure can promote anti-inflammatory processes involving adenosine receptors, protein kinase C (PKC), nitric oxide synthase, heat shock proteins, and others which could underlie cardioprotection. (pubmedcentralcanada.ca)
  • As a result, adenosine decreases the phagocytic activity of macrophages by suppressing the generation of nitric oxide (18), superoxide (19, 20) and pro-inflammatory cytokines (21). (deepdyve.com)
  • The concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug discovery, particularly in the field of G protein-coupled receptors (GPCRs). (pnas.org)
  • Adenosine A2A receptors and metabotropic glutamate 5 receptors are co-localized and functionally interact in the hippocampus: a possible key mechanism in the modulation of N-methyl-D-aspartate effects. (harvard.edu)
  • Our data confirm that the modulation of adenosine receptors can elicit very different (and even opposite) effects during the progression of ALS course, thus strengthens the importance of further studies to elucidated their real therapeutic potential in this pathology. (elsevier.com)
  • Among these indirect approaches, allosteric adenosine receptor modulation represents a novel drug development direction to potentiate A1 receptor function and agonist binding via a conformation change. (asahq.org)
  • The modulation of cell growth by adenosine was found to be receptor-mediated. (nus.edu.sg)
  • Because adenosine production increases in hypoxia, the issue of a role of the nucleoside in the renal injury following ischemia reperfusion has been studied extensively. (springer.com)
  • 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)
  • 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)
  • Adenosine A1 and A2A receptor regulation of protein phosphatase 2A in the murine heart. (harvard.edu)
  • ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells. (jci.org)
  • This study demonstrates that nucleotide receptors in this model of renal epithelium initiate distinct regulation of Na-K-Cl cotransport. (rti.org)
  • In beta N22 cells the IP prostanoid receptor was expressed at similar levels to those in wild-type NG108-15 cells, and treatment with iloprost resulted in a similar down-regulation of cellular Gs alpha levels. (biochemj.org)
  • These results demonstrate that the phenomenon of agonist-induced specific G-protein down-regulation is determined by the levels of expression of the receptor. (biochemj.org)
  • an active role for receptor immobilization in down-regulation? (springer.com)
  • Although adenosine agonists were shown to attenuate pain behaviors in a variety of animal models, adenosine agonists are also implicated in the regulation of many physiologic processes, especially cardiovascular and neurologic, which either reduce the activity of excitable tissues ( e.g. , by slowing heart rate) or increase the delivery of metabolic substrates ( e.g. , inducing vasodilation). (asahq.org)
  • In addition, adenosine A1 receptor regulation after chronic oral T62 administration was examined. (asahq.org)
  • Methods and aims: Using a well-characterized animal model of binge eating, we investigated the epigenetic regulation of the A 2A Adenosine Receptor (A 2A AR) and dopaminergic D2 receptor (D2R) genes. (elsevier.com)
  • We suggest that A 2A AR activation, inducing receptor gene up-regulation, could be relevant to reduction of food consumption. (elsevier.com)
  • The adenosine receptors play crucial role in the regulation of the function of the myocardium and the central nervous system. (otka-palyazat.hu)
  • Wound healing is impaired in MyD88-deficient mice: a role for MyD88 in the regulation of wound healing by adenosine A2A receptors. (naver.com)
  • Introduction:Adenosine as a potent vasodilator has physiological role in regulation of regional cerebral blood flow (rCBF). (phypha.ir)
  • Conclusion:Based on these results it could be concluded that the role of A2B receptors in regulation of rCBF in morphine-dependent rats is more effective than A2A receptors. (phypha.ir)
  • The presence of an a-quaternary carbon such as the 3-hydroxy-3,5-dimethyl-1-hexynyl (12) and the 3-hydroxy-3-phenyl-1-butynyl(1 5) derivatives markedly reduced the antiaggregatory potency without affecting the A2 affinity. (unicam.it)
  • Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors. (patentgenius.com)
  • There is provided exceptionally stable and useful pro-drugs that are esters of N6-oxa, thia, thioxa and azacycloalkyl substituted adenosine derivatives that are selective adenosine type 1 receptor agonists, and as such, are potentially useful agents for the treatment cardiovascular diseases and central nervous system disorders. (justia.com)
  • An object of this invention are novel pro-drugs of heterocyclic substituted adenosine derivatives. (justia.com)
  • Another object of this invention are pro-drugs of heterocyclic substituted adenosine derivatives that are converted in the mammalian body to become useful A1 receptor agonists. (justia.com)
  • Still another object of this invention are pro-drugs of heterocyclic substituted adenosine derivatives that are useful for treating supraventricular tachycardias, including atrial fibrillation, atrial flutter, and AV nodal re-entrant tachycardia in mammals and especially humans. (justia.com)
  • In order to improve this selectivity, the correaponding 2-alkynyl derivatives of adenosine-5'-N-ethyluronamide 8a-d were synthesized and tested. (uni-wuerzburg.de)
  • There are no substantial differences in the extracellular half of the receptor around the ligand binding pocket. (nih.gov)
  • In the current study, we have rationally designed a novel A 1 AR ligand (VCP746)-a hybrid molecule comprising adenosine linked to a positive allosteric modulator-specifically to engender biased signaling at the A 1 AR. (pnas.org)
  • The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). (wikipedia.org)
  • A cDNA encoding a G protein-coupled receptor of unknown ligand specificity was isolated from a human hippocampal cDNA library by virtue of the high degree of structural homology between members of this receptor family. (garvan.org.au)
  • Expression of this cDNA in COS cells revealed high affinity (Kd = 38.6 nM) and saturable binding of the A2 adenosine receptor-selective ligand [3H]CGS 21680. (nih.gov)
  • Vasopressin V2-receptor mobile fraction and ligand-dependent adenylate cyclase-activity are directly correlated in LLC-PK, renal epithelial cells. (springer.com)
  • The protocols worked out provide a firm base for having been receptor/ligand research at the PET Center of the University of Debrecen. (otka-palyazat.hu)
  • The adenosine A 2A receptor (A 2A R) modulates normal vascularization and pathologic angiogenesis in many tissues and may contribute to the pathogenesis of retinopathy of prematurity (ROP) characterized by abnormal retinal vascularization in surviving premature infants. (arvojournals.org)
  • A particular focus was placed on TrkB agonist 7, 8-dihydroxyflavone, which modulates multiple functions and has demonstrated remarkable therapeutic efficacy in a variety of central nervous system disease models. (elsevier.com)
  • A1 and A2 adenosine receptor activation inversely modulates potassium currents and membrane potential in DDT1-MF2 smooth muscle cells. (otka-palyazat.hu)
  • Cerebral morphology, as well as vascular and physiological measures (before, during, and after ischemia) did not differ between A 2A receptor knock-out and wild-type littermates. (jneurosci.org)
  • However, A2b and A3 receptors are relatively less active than A1 and A2a receptors under normal physiological conditions. (innovations-report.com)
  • 9-13 Movement of the hormone-occupied receptor is not required subsequent to dimerization, and consistent with this, activated receptors appear to be aggregated and essentially immobile at physiological temperature (see section E, chapter 4). (springer.com)
  • The adenylate cyclase-coupled vasopressin V2-receptor is highly laterally mobile in membranes of LLC-PK, renal epithelial cells at physiological temperature. (springer.com)
  • Adenosine-a physiological or pathophysiological agent? (eurekaselect.com)
  • Adenosine mediates many physiological functions via activation of extracellular receptors. (nus.edu.sg)
  • Procedures - Radioligand binding experiments were performed to compare binding affinities of adenosine receptor agonists to equine adenosine A 1 , A 2A , and A 3 receptor subtypes. (elsevier.com)
  • Co-incubation of equine peripheral blood monocytes with LPS and these agonists resulted in inhibition of TNF-α production with a rank order of potency that strongly correlated with their binding affinities for equine adenosine A 2A receptors. (elsevier.com)
  • The binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to brain membrane fractions was investigated. (meta.org)
  • BAY 60-6583 is a potent adenosine A2B receptor agonist that decreases fMLP-induced superoxide production in neutrophils at low concentrations (1-10 nM). (emmx.com)
  • The dominant effect of an elevation of plasma adenosine in the renal vasculature is an A 2A AR- and A 2B AR-mediated vasodilatation that increases global as well as medullary renal blood flow and is in part endothelium-dependent. (springer.com)
  • 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)
  • 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)
  • Baranowski RL, Westenfelder C (1994) Estimation of renal interstitial adenosine and purine metabolites by microdialysis. (springer.com)
  • Beach RE, Watts BA 3rd, Good DW et al (1991) Effects of graded oxygen tension on adenosine release by renal medullary and thick ascending limb suspensions. (springer.com)
  • The aim of the current study was to investigate further the effects of intrarenal administration of adenosine on renal excretory function in the rat. (aspetjournals.org)
  • During infusion of adenosine by all three routes, there was a significant decline in glomerular filtration rate, but no change in renal plasma flow. (aspetjournals.org)
  • Ammonium chloride affects receptor number and lateral mobility of the vasopressin V2-type receptor in the plasma membrane of LLC-PK, renal epithelial cells: role of the cytoskeleton. (springer.com)
  • Renal actions of a new adenosine agonist, CGS 21680A selective for the A2 receptor. (toshan.ru)
  • The compound ATP gamma S inhibits agonist-stimulated adenylate cyclase activity in solubilized and in isobutylmethylxanthine (IBMX) and quinacrine pretreated membranes, suggesting that ATP gamma S inhibition occurs independent of AVP and A1 adenosine receptors and of phospholipase A2 activity. (jci.org)
  • Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
  • The rank order potency of inhibition by ATP analogues suggests that a P2y type of ATP receptor is involved in this inhibition. (jci.org)
  • Insulin indirectly relieves GS inhibition ( 4 , 5 ) through a signaling cascade beginning with phosphorylation of substrates, including insulin receptor substrate 1 (IRS-1), by the tyrosine kinase activity of activated insulin receptor ( 6 , 7 ). (diabetesjournals.org)
  • The DRP is a gamma-aminobutyric acid A (GABA A ) receptor-mediated depolarization of primary afferent terminals, which reflects a feedback inhibition associated with analgesia. (asahq.org)
  • In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. (nus.edu.sg)
  • [19-20] Therefore, examination of the actions of adenosine agonists on these responses and characterization of the adenosine receptors involved may provide further information on the mechanism of adenosine-induced antinociception. (asahq.org)
  • However, these analogues also possess good A1 receptor affinity resulting in low A2 selectivity. (unicam.it)
  • The brain-derived neurotrophic factor (BDNF) and its high affinity receptor tropomyosin-receptor-kinase B (TrkB) play a critical role in neuronal differentiation and survival, synapse plasticity, and memory. (elsevier.com)
  • Furthermore, it has negligible affinity to A2B and A3 adenosine receptors. (drugbank.ca)
  • 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)
  • Objective - To evaluate anti-inflammatory effects of several novel adenosine receptor agonists and to determine their specificity for various adenosine receptor subtypes on neutrophils, cells heterologously expressing equine adenosine receptors, or equine brain membranes. (elsevier.com)
  • Conclusions and Clinical Relevance - Results indicated that activation of A 2A receptors exerted anti-inflammatory effects on equine neutrophils and that stable, highly selective adenosine A 2A receptor agonists may be developed for use in management of horses and other domestic animals with septic and nonseptic inflammatory diseases. (elsevier.com)
  • The results of this study indicate that stable adenosine analogues that are selective for adenosine A 2A receptors may be suitable for development as anti-inflammatory drugs in horses. (elsevier.com)
  • The aim of this paper was to examine the link between antiplatelet and anti-inflammatory roles of quercetin in agonist-induced platelet activation. (hindawi.com)
  • In protocol B, risk zones were similar, but administration of adenosine resulted in significant reductions in infarct size from 59 ± 3% of the area-at-risk in control swine to 46 ± 4% (p = 0.02), and no-reflow from 49 ± 6% of the infarct area to 26 ± 6% (p = 0.03). (onlinejacc.org)
  • Previous studies in the rat have shown that i.v. and intra-aortic administration of adenosine decrease water and sodium excretion. (aspetjournals.org)
  • The validity of these findings was challenged recently when it was found that intrarenal administration of adenosine in the rat induced marked diuresis and natriuresis. (aspetjournals.org)
  • Schlessinger J. Signal transduction by allosteric receptor oligomerization. (springer.com)
  • Schlessinger J. The epidermal growth factor receptor as a multifunctional allosteric protein. (springer.com)
  • PD 81723 is an allosteric potentiator at the adenosine A1 receptor which acts via agonist-dependent and -independent mechanisms. (emmx.com)
  • The compounds were studied in binding and functional assays to assess their potency for the A2 compared to A1 adenosine receptor. (unicam.it)
  • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (nih.gov)
  • that the claimed compounds would have an A1-adenosine receptor antagonistic activity. (epo.org)
  • These low molecular weight compounds activated glycogen synthase at ∼100 nmol/l in cultured CHO cells transfected with the insulin receptor and in primary hepatocytes isolated from Sprague-Dawley rats, and at 500 nmol/l in isolated type 1 skeletal muscle of both lean Zucker and ZDF rats. (diabetesjournals.org)
  • 12,13 An adenosine receptor modulator, T62, belonging to a group of thiophene compounds first described a decade ago, 14 has been shown to reduce mechanical allodynia in spinal nerve-injured rats after oral, parenteral, or intrathecal application. (asahq.org)
  • Two other small molecules included in this review are adenosine A 2A receptor agonists that indirectly activate TrkB, and TrkB binding domains of BDNF, loop II-LM22A compounds that directly activate TrkB. (elsevier.com)
  • 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)
  • Their theory is based on the fact that adenosine is produced within the body and inhibits neuronal excitability and synapse transmission. (innovations-report.com)
  • Adenosine also inhibits neutrophil degranulation (22). (deepdyve.com)
  • 2'-MeCCPA is a potent and highly selective agonist at A1 adenosine receptors (Ki values are 3.3, 9580, 37600 and 1150 nM for human recombinant A1, A2A, A2B and A3 receptors respectively), which acts as a full agonist and inhibits forskolin-stimulated adenylyl cyclase activity in rat cortical membranes with an IC50 value of 13.1 nM. (emmx.com)
  • The investigational drug, regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist, the receptor responsible for coronary vasodilation, and is being studied for potential use as a pharmacologic stress agent in myocardial perfusion imaging (MPI) studies. (clinicaltrials.gov)
  • A1 and A2A receptors are believed to regulate myocardial oxygen demand and to increase coronary circulation by vasodilation. (wikipedia.org)
  • Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. (drugbank.ca)
  • CV 1808, a adenosine A2 receptor agonist, is coronary vasodilator, antihypertensive and antipsychotic following systemic administration in vivo. (emmx.com)
  • Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear to mediate slow synaptic responses in the CNS. (jneurosci.org)
  • A number of G-protein-linked receptors that are not directly coupled to adenylate cyclase increase cAMP accumulation by potentiating cAMP responses to other agonists. (jneurosci.org)
  • Nucleotide receptors may effect their responses through primary activation of membrane chloride channels. (rti.org)
  • Thus, the generation of adenosine by macrophages is an important mechanism that prevents overactive inflammatory responses. (jimmunol.org)
  • One of the major pathways by which the oxidative damage produced by free radicals promotes inflammatory responses, involves the Toll-like-receptors (TLRs). (scirp.org)
  • Adenosine receptors of the A1 and A2 subtypes were characterized in membranes from DDT1 MF-2 smooth muscle cells. (aspetjournals.org)
  • 2-Alkynyladenosines also exhibited high-affmity binding at solubilized A\(_2\) receptors from human platelet membranes. (uni-wuerzburg.de)
  • G-protein-coupled receptors (GPCRs) are essential components of the signalling network throughout the body. (nih.gov)
  • G protein-coupled receptors (GPCRs) are the largest family of cell surface proteins and tractable drug targets ( 1 , 2 ). (pnas.org)
  • These released mediators stimulate G-protein coupled receptors (GPCRs) that are necessary for phospholipase C (PLC), protein kinase C (PKC), phosphoinositide-3 kinase (PI3K) [ 4 ], and MAP kinases activations [ 5 ]. (hindawi.com)
  • This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices, as well as an extracellular N-terminus and an intracellular C-terminus. (wikipedia.org)
  • The activity of the encoded protein, a G protein-coupled receptor family member, is mediated by G proteins which activate adenylyl cyclase, which induce synthesis of intracellular cAMP. (wikipedia.org)
  • The adenosine A1 receptor (Adora1) is a G-protein coupled receptor (GPCR) that is involved in maintaining glucose homeostasis and regulating glucagon secretion ( 11 , 12 ). (diabetesjournals.org)
  • A cDNA fragment homologous to other G protein-coupled receptors was isolated from rat brain using the PCR method and demonstrated to be abundantly expressed in striatum. (nih.gov)
  • Hydrophobicity analysis of the deduced protein sequence reveals seven hydrophobic regions, characteristic of a member of the G-protein-coupled receptor superfamily. (nih.gov)
  • Similar to other G protein-coupled receptors, A2A receptors form both homo- and heterodimers. (wikipedia.org)
  • Key modulatory role of presynaptic adenosine A2A receptors in cortical neurotransmission to the striatal direct pathway. (harvard.edu)
  • Vanderhaeghen, "Striatal restricted adenosine A2 receptor (RDC8) is expressed by enkephalin but not by substance P neurons: an in situ hybridization histochemistry study," Journal of Neurochemistry, vol. (thefreedictionary.com)
  • This study aims to evaluate adenosine and P2 receptors and cellular signalling in cardiac arrest produced by purines in the heart. (ovid.com)
  • Pathophysiological roles for purines: adenosine, caffeine and urate. (harvard.edu)
  • Receptors for purines and pyrimidines are expressed throughout the cardiovascular system. (nottingham.ac.uk)
  • The increase in LPS-induced IL-10 production and suppression of LPS-induced TNF-α and NO production caused by adenosine receptor activation may explain some of the immunomodulatory actions of adenosine released in excess during inflammatory and/or ischemic insult. (utmb.edu)
  • [3-5] In the central nervous system, two main types of receptors are believed to mediate the actions of adenosine: A 1 and A 2 types of adenosine receptors. (asahq.org)
  • Suppression of lipopolysaccharide-stimulated release of tumor necrosis factor by adenosine: evidence for A2 receptors on rat Kupffer cells. (duke.edu)
  • Adenosine, nisoldipine and prostaglandin E1 each suppressed lipopolysaccharide-stimulated tumor necrosis factor release. (duke.edu)
  • The results of previous studies indicate that adenosine analogues inhibit lipopolysaccharide (LPS)-induced production of reactive oxygen species (ROS) by equine neutrophils primarily through activation of A 2A receptors. (elsevier.com)
  • IFN-γ priming of macrophages selectively prevents the induction of the A2bR in macrophages to mitigate sensitivity to adenosine and to prevent this regulatory transition. (jimmunol.org)
  • The authors explored the bone regenerative capacity of customized, three-dimensionally printed bioactive ceramic scaffolds with dipyridamole, an adenosine A 2A receptor indirect agonist known to enhance bone formation. (nyu.edu)
  • Surface-localized CD73 converts AMP into adenosine, which in turn can activate transmembrane adenosine receptors or can be internalized through dipyridamole-sensitive carriers ( 14 ). (rupress.org)
  • Radioligand binding assay and functional (GTPase and cAMP) assays of the receptor, transiently expressed in mammalian cells, demonstrate typical characteristics of the A2 type adenosine receptor. (nih.gov)
  • Using a recently developed A2 adenosine receptor agonist radioligand 2-[4-(2-[( 4-aminophenyl]methylcarbonyl)ethyl) phenyl]ethylamino-5'-N-ethylcarboxamido adenosine (125I-PAPA-APEC), we have demonstrated the presence of A2 adenosine receptors in this cell line. (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)
  • Inactivation of neuronal forebrain A receptors protects dopaminergic neurons in a mouse model of Parkinson's disease. (harvard.edu)
  • The presence of heterodimeric complexes has progressed in suggesting new ways to regulate neuronal activity by targeting the A2A receptor. (wikipedia.org)
  • In this study we report that i.p. pretreatment of mice with CGS-21680 HCl (CGS), a selective agonist of A 2 adenosine receptors, at 0.2 to 2 mg/kg caused an augmentation of plasma IL-10 levels induced by i.p. injection of LPS, but decreased plasma levels of LPS-induced TNF-α. (utmb.edu)
  • In addition, A2A receptor can suppress immune cells, thereby protecting tissue from inflammation. (wikipedia.org)
  • Awad AS, Huang L, Ye H et al (2006) Adenosine A2A receptor activation attenuates inflammation and injury in diabetic nephropathy. (springer.com)
  • These findings suggest that during pathological conditions such as inflammation or trauma, the significant amounts of cellular adenosine which are released may increase the production of NO by macrophage. (nus.edu.sg)
  • Our study suggested that PDRN, by binding the A 2A receptor, contributed to a great extent towards reducing inflammation. (scirp.org)
  • Effects of these agonists on endotoxin-induced production of reactive oxygen species (ROS) by equine neutrophils and roles of specific adenosine receptor subtypes and cAMP production in mediating these effects were determined. (elsevier.com)
  • The volume of cerebral infarction, as well as the associated neurological deficit induced by transient filament occlusion of the middle cerebral artery, were significantly attenuated in A 2A receptor knock-out mice. (jneurosci.org)
  • This neuroprotective phenotype of A 2A receptor-deficient mice was observed in different genetic backgrounds, confirming A 2A receptor disruption as its cause. (jneurosci.org)
  • Cell counts, EBDA extravasation, as well as levels of proteins and inflammatory cytokines were decreased in adenosine-treated mice. (physiology.org)
  • Mice heterozygous for both A1 and A(2A) adenosine receptor genes show similarities to mice given long-term caffeine. (harvard.edu)
  • Forebrain adenosine A2A receptors contribute to L-3,4-dihydroxyphenylalanine-induced dyskinesia in hemiparkinsonian mice. (harvard.edu)
  • Here, we show that the expression of a potential glucagon inhibitor, the adenosine A1 receptor (Adora1), is gradually diminished in α-cells of NOD mice, autoantibody-positive (AA + ) and overtly type 1 diabetic (T1D) patients during the progression of disease. (diabetesjournals.org)
  • Finally, when stimulated with cholinergic or cAMP agonists, cells from mice that lacked CFTR, as well as wild-type cells treated with a CFTR inhibitor, exhibited identical rates and magnitudes of shrinkage and Cl − efflux compared with control cells. (wiley.com)
  • between 50% and 35% regrowth in mice injected with a liposomal formulation of Adenosine. (seniorfitness.com)
  • In studies where Adenosine is removed from the joint synovial fluid (the slippery fluid in a joint capsule that lubricates and nourishes the cartilage), or in knock-out mice who can't make the stuff, the joints rapidly degrade (in youth for the KO mice). (seniorfitness.com)
  • Conversely, blockade of adenosine A1 receptors from the presymptomatic stage significantly attenuated motor disease progression and induced a non-significant increase of median survival in ALS mice. (elsevier.com)