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
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
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
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.
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.

Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic myocardial injury. (1/77)

We recently reported the identification of a novel human adenosine A3 receptor-selective agonist, (2S,3S,4R,5R)-3-amino-5-[6-[5-chloro-2-(3-methylisoxazol-5-ylmethoxy)benzylamino] purin-9-yl]-4-hydroxytetrahydrofuran-2-carboxylic acid methylamide (CP-608,039), with 1,260-fold selectivity for the human A3 versus human A1 receptor (DeNinno et al., J Med Chem 46: 353-355, 2003). However, because the modest (20-fold) rabbit A3 receptor selectivity of CP-608,039 precludes demonstration of A3-mediated cardioprotection in rabbit models, we identified another member of this class, (2S,3S,4R,5R)-3-amino-5-[6-(2,5-dichlorobenzylamino)purin-9-yl]-4-hydroxytetrahyd rofuran-2-carboxylic acid methylamide (CP-532,903), which both retained human A3 receptor selectivity (210-fold; human A3/human A1 Ki: 23/4,800 nM) and had improved rabbit A3 receptor selectivity (90-fold; rabbit A3/rabbit A1 Ki: 23/2,000 nM). Infarct size was measured in Langendorff hearts or in vivo after 30 min of regional ischemia and 120 min of reperfusion. Five-minute perfusion with CP-532,903 before ischemia-reperfusion elicited a concentration-dependent reduction in infarct size in isolated hearts (EC50: 0.97 nM; maximum reduction in infarct size: 77%, P < 0.05 vs. control). Furthermore, administration of CP-532,903 (150 nM) at reperfusion also significantly reduced infarct size by 64% (P < 0.05 vs. control), which was not different (P > or = 0.05) from the cardioprotection provided by the same concentration of drug given before ischemia. The selective rabbit A1 receptor antagonist BWA1433 did not affect CP-532,903-dependent cardioprotection. In vivo, CP-532,903 (1 mg/kg) reduced infarct size by 50% in the absence of significant hemodynamic effects (mean arterial pressure, heart rate, rate-pressure product). CP-532,903 and CP-608,039 represent a novel class of human A3 receptor-selective agonists that may prove suitable for investigation of the clinical cardioprotective efficacy of A3 receptor activation.  (+info)

An adenosine analogue, IB-MECA, down-regulates estrogen receptor alpha and suppresses human breast cancer cell proliferation. (2/77)

Adenosine, a natural metabolite, plays important roles in several physiological and pathological processes, including modulation of cellular proliferation. Here, we report that among different adenosine analogues tested, micromolar concentrations of the A(3) adenosine receptor (A(3)AR)-selective agonist N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) completely inhibited the growth of the human breast cancer cell lines MCF-7 and ZR-75 while inducing apoptosis in T47D and Hs578T cells, which do not express A(3)AR mRNA. In MCF-7 cells, A(3)AR overexpression did not increase the sensitivity to drug treatment and an A(3)AR antagonist did not abolish IB-MECA effect. In search for mechanisms of the effect of this ligand, we found that in estrogen receptor alpha (ERalpha)-positive cells, IB-MECA rapidly down-regulated ERalpha at mRNA and protein levels and consequently at the transcriptional activity level. Moreover, overexpression of ERalpha in MCF-7 cells alleviated the proliferation inhibition induced by IB-MECA. The inhibitory effects on cell growth and to some extent on ERalpha were mimicked by 2-chloro-adenosine >3'-deoxyadenosine> adenosine but not by a variety of other ligands. Our studies indicate that IB-MECA can down-regulate ERalpha and inhibit proliferation or induce apoptosis in different breast cancer cell types and raise the possibility of using this and related compounds in breast cancer treatment.  (+info)

Role of direct RhoA-phospholipase D1 interaction in mediating adenosine-induced protection from cardiac ischemia. (3/77)

Activation of adenosine A1 or A3 receptors protects heart cells from ischemia-induced injury. The A3 receptor signals via RhoA and phospholipase D (PLD) to induce cardioprotection. The objective of the study was to investigate how RhoA activates PLD to achieve the anti-ischemic effect of adenosine A3 receptors. In an established cardiac myocyte model of preconditioning using the cultured chick embryo heart cells, overexpression of the RhoA-noninteracting PLD1 mutant I870R selectively blocked the A3 agonist (Cl-IBMECA, 10 nM)-induced cardioprotection. I870R caused a significantly higher percentage of cardiac cells killed in A3 agonist-treated than in A1 agonist (CCPA, 10 nM)-treated myocytes (ANOVA and posttest comparison, P<0.01). Consistent with its inhibitory effect on the PLD activity, I870R attenuated the Cl-IBMECA-mediated PLD activation. Cl-IBMECA caused a 41 +/- 15% increase in PLD activity in mock-transfected myocytes (P<0.01, paired t test) while having only a slight stimulatory effect on the PLD activity in I870R-transfected cells. To further test the anti-ischemic role of a direct RhoA-PLD1 interaction, atrial cardiac myocytes were rendered null for native adenosine receptors by treatment with irreversible A1 antagonist m-DITC-XAC and were selectively transfected with the human adenosine A1 or A3 receptor cDNA individually or they were cotransfected with cDNAs encoding either receptor plus I870R. I870R preferentially inhibited the human A3 receptor-mediated protection from ischemia. The RhoA-noninteracting PLD1 mutant caused a significantly higher percentage of cardiac cells killed in myocytes cotransfected with the human A3 receptor than in those cells expressing the human A1 receptor (ANOVA and posttest comparison, P<0.01). The present data provided the first demonstration of a novel physiological role for the direct RhoA-PLD1 interaction, that of potent protection from cardiac ischemia. The study further supported the concept that a divergent signaling mechanism mediates the anti-ischemic effect of adenosine A1 and A3 receptors.  (+info)

Partial agonists for A(3) adenosine receptors. (4/77)

Selective agonists for A(3) adenosine receptors (ARs) could potentially be therapeutic agents for a variety of disorders, including brain and heart ischemic conditions, while partial agonists may have advantages over full agonists as a result of an increased selectivity of action. A number of structural determinants for A(3)AR activation have recently been identified, including the N(6)-benzyl group, methanocarba substitution of ribose, 2-chloro and 2-fluoro substituents, various 2'- and 3'-substitutions and 4'-thio substitution of oxygen. The 2-chloro substitution of CPA and R-PIA led to A(3) antagonism (CCPA) and partial agonism (Cl-R-PIA). 2-Chloroadenosine was a full agonist, while 2-fluoroadenosine was a partial agonist. Both 2'- and 3'- substitutions have a pronounced effect on its efficacy, although the effect of 2'-substitution was more dramatic. The 4-thio substitution of oxygen may also diminish efficacy, depending on other substitutions. Both N(6)-methyl and N(6)-benzyl groups may contribute to the A(3) affinity and selectivity; however, an N(6)-benzyl group but not an N(6)-methyl group diminishes A(3)AR efficacy. N(6)-benzyl substituted adenosine derivatives have similar potency for human and rat A(3)ARs while N(6)-methyl substitution was preferable for the human A(3)AR. The combination of 2-chloro and N(6)-benzyl substitutions appeared to reduce efficacy further than either modification alone. The A(2A)AR agonist DPMA was shown to be an antagonist for the human A(3)AR. Thus, the efficacy of adenosine derivatives at the A(3)AR appears to be more sensitive to small structural changes than at other subtypes. Potent and selective partial agonists for the A(3)AR could be identified by screening known adenosine derivatives and by modifying adenosine and the adenosine derivatives.  (+info)

Inhibition of phenylephrine-induced cardiomyocyte hypertrophy by activation of multiple adenosine receptor subtypes. (5/77)

Plasma adenosine levels are elevated in cardiovascular disease including hypertension and heart failure, and the nucleoside has been proposed to serve as an endogenous antimyocardial remodeling factor. We studied the modulation of phenylephrine-induced hypertrophy by adenosine receptor activation in isolated neonatal cultured ventricular myocytes. Phenylephrine (10 muM) increased cell size by 35% and significantly increased expression of atrial natriuretic peptide. These effects were reduced by the stable adenosine analog 2-chloroadenosine and were completely blocked by the adenosine A(1) receptor agonist N(6)-cyclopentyladenosine (1 microM), the A(2A) receptor agonist 2-p-(2-carboxyethyl)-phenethylamino-5'-N-ethylcarboxamidoadenosine (100 nM), and the A(3) receptor agonist N(6)-(3-iodobenzyl)adenosine-5'-methyluronamide (100 nM). The antihypertrophic effects of all three agonists were completely reversed by their respective antagonists. Phenylephrine significantly up-regulated expression of the immediate early gene c-fos especially within the first 30 min of phenylephrine treatment. These effects were almost completely inhibited by all adenosine receptor agonists. Although phenylephrine also induced early stimulation of both p38 mitogen-activated protein kinase and extracellular signal-regulated kinase, these responses were unaffected by adenosine agonists. The expression of the G-protein regulatory factors RGS2 and RGS4 were increased by nearly 3-fold by phenylephrine treatment although this was completely prevented by adenosine receptor agonists. These agents also blocked the ability of phenylephrine to up-regulate Na/H exchange isoform 1 (NHE1) expression in hypertrophied myocytes. Thus, our results demonstrate an antihypertrophic effect of adenosine acting via multiple receptor subtypes through a mechanism involving down-regulation of NHE1 expression. The ability to prevent regulators of G-protein signaling (RGS) up-regulation further suggests that adenosine receptor activation minimizes signaling which leads to hypertrophic responses.  (+info)

Activation of A3 adenosine receptors attenuates lung injury after in vivo reperfusion. (6/77)

BACKGROUND: A3 adenosine receptor (AR) activation worsens or protects against renal and cardiac ischemia-reperfusion (IR) injury, respectively. The aims of the current study were to examine in an in vivo model the effect of A3AR activation on IR lung injury and investigate the mechanism by which it exerts its effect. METHODS: The arterial branch of the left lower lung lobe in intact-chest, spontaneously breathing cats was occluded for 2 h and reperfused for 3 h (IR group). Animals were treated with the selective A3 receptor agonist IB-MECA (300 microg/kg intravenously) given 15 min before ischemia or with IB-MECA as described, with pretreatment 15 min earlier with the selective A3AR antagonist MRS-1191, the nonsulfonylurea adenosine triphosphate-sensitive potassium channel-blocking agent U-37883A, or the nitric oxide synthase inhibitor N-nitro-l-arginine benzyl ester. RESULTS: IB-MECA markedly (P < 0.01) reduced the percentage of injured alveoli (IR, 48 +/- 4%; IB-MECA, 18 +/- 2%), wet:dry weight ratio (IR, 8.2 +/- 0.4; IB-MECA, 4 +/- 2), and myeloperoxidase activity (IR, 0.52 +/- 0.06 U/g; IB-MECA, 0.17 +/- 0.04 U/g). This protective effect was completely blocked by pretreatment with the selective A3AR antagonist MRS-1191 and the adenosine triphosphate-sensitive potassium channel blocking agent U-37883A but not the nitric oxide synthase inhibitor N-nitro-l-arginine benzyl ester. CONCLUSIONS: In the feline lung, the A3AR agonist IB-MECA confers a powerful protection against IR lung injury. This effect is mediated by a nitric oxide synthase-independent pathway and involves opening of adenosine triphosphate-sensitive potassium channels. Therefore, selective activation of A3AR may be an effective means of protecting the reperfused lung.  (+info)

Role of adenosine A1 and A3 receptors in regulation of cardiomyocyte homeostasis after mitochondrial respiratory chain injury. (7/77)

Activation of either the A(1) or the A(3) adenosine receptor (A(1)R or A(3)R, respectively) elicits delayed cardioprotection against infarction, ischemia, and hypoxia. Mitochondrial contribution to the progression of cardiomyocyte injury is well known; however, the protective effects of adenosine receptor activation in cardiac cells with a respiratory chain deficiency are poorly elucidated. The aim of our study was to further define the role of A(1)R and A(3)R activation on functional tolerance after inhibition of the terminal link of the mitochondrial respiratory chain with sodium azide, in a state of normoxia or hypoxia, compared with the effects of the mitochondrial ATP-sensitive K(+) channel opener diazoxide. Treatment with 10 mM sodium azide for 2 h in normoxia caused a considerable decrease in the total ATP level; however, activation of adenosine receptors significantly attenuated this decrease. Diazoxide (100 muM) was less effective in protection. During treatment of cultured cardiomyocytes with hypoxia in the presence of 1 mM sodium azide, the A(1)R agonist 2-chloro-N(6)-cyclopentyladenosine was ineffective, whereas the A(3)R agonist 2-chloro-N(6)-iodobenzyl-5'-N-methylcarboxamidoadenosine (Cl-IB-MECA) attenuated the decrease in ATP level and prevented cell injury. Cl-IB-MECA delayed the dissipation in the mitochondrial membrane potential during hypoxia in cells impaired in the mitochondrial respiratory chain. In cells with elevated intracellular Ca(2+) concentration after hypoxia and treatment with NaN(3) or after application of high doses of NaN(3), Cl-IB-MECA immediately decreased the elevated intracellular Ca(2+) concentration toward the diastolic control level. The A(1)R agonist was ineffective. This may be especially important for the development of effective pharmacological agents, because mitochondrial dysfunction is a leading factor in the pathophysiological cascade of heart disease.  (+info)

CF101, an agonist to the A3 adenosine receptor, enhances the chemotherapeutic effect of 5-fluorouracil in a colon carcinoma murine model. (8/77)

NF-kappaB and the upstream kinase PKB/Akt are highly expressed in chemoresistance tumor cells and may hamper the apoptotic pathway. CF101, a specific agonist to the A3 adenosine receptor (A3AR), inhibits the development of colon carcinoma growth in cell cultures and xenograft murine models. Because CF101 has been shown to downregulate PKB/Akt and NF-kappaB protein expression level, we presumed that its combination with chemotherapy will enhance the antitumor effect of the cytotoxic drug. In this study, we utilized 3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and colony formation assays and a colon carcinoma xenograft model. It has been shown that a combined treatment of CF101 and 5-fluorouracil (5-FU) enhanced the cytotoxic effect of the latter on HCT-116 human colon carcinoma cell proliferation and tumor growth. Downregulation of PKB/Akt, NF-kappaB, and cyclin D1, and upregulation of caspase-3 protein expression level were observed in cells and tumor lesions on treatment with a combination of CF101 and 5-FU. Moreover, in mice treated with the combined therapy, myelotoxicity was prevented as was evidenced by normal white blood cell and neutrophil counts. These results show that CF101 potentiates the cytotoxic effect of 5-FU, thus preventing drug resistance. The myeloprotective effect of CF101 suggests its development as an add-on treatment to 5-FU.  (+info)

294964902 - EP 1019427 A1 2000-07-19 - N?6 -SUBSTITUTED-ADENOSINE-5 -URONAMIDES AS ADENOSINE RECEPTOR MODULATORS - [origin: WO9906053A1] A series of adenosine-5 -uronamide derivatives bearing N 6 -arylurea, alkarylurea, heteroarylurea, arylcarbonyl, alkarylcarbonyl or heteroarylcarbonyl groups which have affinity and, in some cases, selectivity for the adenosine A1 or A3 receptors are disclosed. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A1 or A3 receptors, or can be used in a diagnostic application to determine the relative binding of other compounds to the A1 or A3 receptors.[origin: WO9906053A1] A series of adenosine-5 -uronamide derivatives bearing N 6 -arylurea, alkarylurea, heteroarylurea, arylcarbonyl, alkarylcarbonyl or heteroarylcarbonyl groups which have affinity and, in some cases, selectivity for the adenosine A1 or A3 receptors are disclosed. These compounds can be used in a pharmaceutical composition to treat
Accumulating evidence supports a therapeutic role of purinergic signaling in cardiac diseases. Previously, efficacy of systemically infused MRS2339, a char
Long Term Causes continued Militarism- national policy based on military strength and glorification of war Examples - Build up of arms by countries all around the world - Build up of naval power by all major countries (Notable countries include Great Britain, France, Germany, United States, Russia, Japan, Italy)
364168652 - EP 2081946 B1 20120530 - ADENOSINE DERIVATIVES FOR THE TREATMENT OF PAIN - [origin: WO2008000745A2] Compounds of formula (I) below are disclosed. Their use as medicaments is described, in particular for the treatment of pain or inflammation. In said Fomula, when X=Y=Z=OH, R SUB 1 /SUB is OCH SUB 2 /SUB CF SUB 2 /SUB CF SUB 3 /SUB , phenoxy (substituted with 3-(4- trifluoromethylphenyl), 3,4-dichloro, (3-trifluoromethyl,4-fluoro), (3-trifluoromethyl,4- chloro), (3-chloro, 4-cyano), or 3,5-bis(trifluoromethyl)), l-piperazinyl(4-(3,4- dichlorophenyl)), phenyl (substituted with 3,4-dichloro, 3,5-difluoro, 3,5- bis(trifluoromethyl) or 3,4,5-trifluoro) or 2-benzofuranyl; or when X=Y=OH and Z=OMe, R SUB 1 /SUB is OCH SUB 3 /SUB , OCH SUB 2 /SUB CHF SUB 2 /SUB , OCH SUB 2 /SUB cyclopentyl, O-(2,5- difluorophenyl) or (S)-sec-butylamino; or when X=H and Y=Z=OH, R SUB 1 /SUB is n-hexylamino or cyclopentylamino; or when (IV) X=Z=OH and Y=H, R SUB 1 /SUB is cyclopentylamino;or a pharmaceutically
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Effects of adenosine receptor agonists of the A1, A2A and A3 subtypes on the proinflammatory activity of human neutrophils in ...
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f.vtHYTHlNG HER PLAIN AMD CLEAK Consljoljockcn ticcoroer ALL THATS TttJ« WgLL GIVE TO YO0. No. 2057 PUBLISHED; EVERY TUESDAY AND FRIDAY NOTES OF OUR TOWN i i BMS OF INTEREST GONOBBNINa THE PEOPLE OF OUB BOROOQH CONDENSED FOB RECORDER READERS. William Plank is ill u his boms on Sprint Mill gvenue. Mr. .IM.I Mrs. Harvey field won! to Oettyaburg oa Saturday. •Miss,, Uargare, Wright and i.i n Jones ipral Sunday in WarneravUla. Rev. .111.1 Mrs. .1. F. Shearer an i Itini friends in this borough over Sun-day. \n Intaraatlnc letter from William Henry is published on the third page of this leane. The Penn BoelaJ Club is holdlni - » the P 0. B or .\. Hall every Saturday evening. Rev. Mr. Balnea, of Hanayunk, oon- l1 : ■ In the BaptIM Church on Sunday morning and evening John Devlin and brothers have loft this place for good to take up their ,,si1 Mount Washington, Pitta-burg, South Bide. The ladles of Calvary Church will i sals 11 Bread and Cakea on Sat-nrday afternoon, November tad ...
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مقدمه: گلوتامیک‌اسید یکی از مهم‌ترین آمینواسیدها از نظر کاربردهای صنعتی و تجاری است و تولید میکروبی آن از برخی باکتری‌ها گزارش شده است. با توجه به نقش باکتری‌های پروبیوتیک در ارتقای سلامتی انسان و تقاضای روزافزون کاربرد آنها در صنایع غذایی، در پژوهش حاضر تولید آمینواسیدهای گلوتامیک‌اسید و فولیک‌اسید با استفاده از باکتری‌های پروبیوتیک (بیفیدوباکتریوم، بیفیدوباکتریوم بیفیدوم و اسپرولاکتوباسیلوس) بررسی شد. مواد و روش‏‏ها: چند محیط اختصاصی و محیط MRS آگار برای کشت سویه‌های پروبیوتیک مدنظر استفاده شدند. گلوتامیک‌اسید موجود در ریزموجودات با
SMC announces that Can-Fite BioPharma has published the results of a study using STAM™ model in International Journal of Molecular Medicine.. Title: The A3 adenosine receptor agonist, namodenoson, ameliorates non-alcoholic steatohepatitis in mice. The A3 adenosine receptor agonist, namodenoson, ameliorates non‑alcoholic steatohepatitis in mice (spandidos-publications.com). ...
Diamond I, Mochly-Rosen D, Gordon AS. In Alcohol and seizures: basic mechanisms and clinical concepts. Porter R, Mattson R, Kramer J and Diamond I (eds). FA Davis, Philadelphia, pp 79-86, (1990). ...
... is a selective adenosine A3 subtype receptor agonist. It has antiinflammatory effects and has been shown to reduce ... The A3 adenosine receptor agonist CP-532,903 [N6-(2,5-dichlorobenzyl)-3'-aminoadenosine-5'-N-methylcarboxamide] protects ... Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic ... Adenosine receptor agonists, All stub articles, Nervous system drug stubs). ...
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. In a mouse model of ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ...
... structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors ... PSB-10 is a drug which acts as a selective antagonist for the adenosine A3 receptor (ki value at human A3 receptor is 0.44 nM ... Müller CE (2003). "Medicinal chemistry of adenosine A3 receptor ligands". Current Topics in Medicinal Chemistry. 3 (4): 445-62 ... with high selectivity over the other three adenosine receptor subtypes (ki values at human A1, A2A and A2B receptors are 4.1, ...
Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in ... There are four known types of adenosine receptors in humans: A1, A2A, A2B and A3; each is encoded by a different gene. The ... The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the ... "Entrez Gene: ADORA2A adenosine A2A receptor". Jacobson KA, Gao ZG (2006). "Adenosine receptors as therapeutic targets". Nature ...
"The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia". The Journal ... October 2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system". ... The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human ... alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting ...
There are four well-known adenosine receptors found in the body, A1, A2A, A2B, and A3. The endogenous agonist for these ... Adenosine is a normal neuromodulator that activates adenosine g-protein coupled receptors. The actions of A1 and A2A receptors ... A2A receptors are not found in neurons that express the dopamine receptor D1 receptors and Substance P. Within the striatum, ... and signal transduction in the form of cyclic adenosine monophosphate (cAMP). A2B and A3 receptors require concentrations of ...
... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... January 2002). "7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This ...
All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... Experimental evidence suggests that adenosine and adenosine agonists can activate Trk receptor phosphorylation through a ... Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). Extracellular ... Adenosine is an endogenous agonist of the ghrelin/growth hormone secretagogue receptor. However, while it is able to increase ...
Adenosine diphosphate (ADP) is a platelet agonist. When it is added to saline-diluted whole blood in the test cuvette, it ... Thrombin receptor activating peptide-6 (TRAP-6) activates platelets through the thrombin receptor protease activated receptor-1 ... Prostaglandin E1 (PGE1) is a platelet inhibitor that causes an increase in cyclic adenosine monophosphate (cAMP) in platelets ... Activation of the P2Y1 receptor initiates platelet aggregation in response to ADP. The P2Y1 receptor is required for ADP- ...
... adenosine receptor binding affinity (21 μM for A1, 32 μM for A2A, 4.5 μM for A2B, and >100 for μM for A3) is ... "Adenosine receptors: development of selective agonists and antagonists". Progress in Clinical and Biological Research. 230 (1 ... Müller, Christa E.; Jacobson, Kenneth A. (2011), Fredholm, Bertil B. (ed.), "Xanthines as Adenosine Receptor Antagonists", ... Studies indicate that, similar to caffeine, simultaneous antagonism of adenosine receptors is responsible for paraxanthine's ...
Subtype-selective agonists for α3 produce anxiolytic effects without sedative, amnesia, or ataxia. selective a3 agonists also ... The unedited receptor is activated faster and deactivates slower than the edited receptor. GABAA receptor GRCh38: Ensembl ... Also, alpha subunits 1 and 6 have a uridine instead of an adenosine at the site corresponding to the editing site in alpha ... Adipiplon PWZ-029 (partial agonist at α3, partial inverse agonist at α5) TP003 (Selective full agonist at α3) α3IA The GABRA3 ...
... agonists, which are used to treat high blood pressure and asthma, for example. Many cells have these receptors, and the binding ... 81 (1): 211.e1-7. doi:10.1016/j.urology.2012.09.011. PMID 23200975. Fitzpatrick D, Purves D, Augustine G (2004). "Table 20:2". ... "Convergence of major physiological stimuli for renin release on the Gs-alpha/cyclic adenosine monophosphate signaling pathway ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 There is no α1C receptor. There was a subtype known as C, but ...
On the other hand, nanomolar concentrations of adenosine activate A1 and A3 receptors, resulting in neutrophilic chemotaxis ... Cerqueira MD (July 2004). "The future of pharmacologic stress: selective A2A adenosine receptor agonists". The American Journal ... In the airways of patients with asthma, the expression of adenosine receptors is upregulated. Adenosine receptors affect ... the expression of adenosine receptors on the neutrophil, and the affinity of these receptors for adenosine. Micromolar ...
... β2 and β3 and the five dopamine receptors D1, D2, D3, D4 and D5. Their fine structure, without agonist or agonist-activated, is ... A. Vulpian (1856). "Note sur quelques réactions propres à la substance des capsules surrénales". Comptes Rendus de l'Académie ... In addition the vesicles contained adenosine triphosphate (ATP), with a molar noradrenaline:ATP ratio in sympathetic nerve ... he called alpha adrenotropic receptor (now α-adrenoceptor or α-adrenergic receptor), while the receptor with the second rank ...
... which has been shown to be an inverse agonist for adenosine A1 receptor sites. Hydrophilic extractions of the herb commonly ... doi:10.1213/01.ANE.0000096189.70405.A5. PMID 14742369. S2CID 14526474. Wills, R.B.H. & Shohet, D. (July 2009). "Changes in ... Valerenic acid in valerian stimulates GABA(A) and serotonin receptors as a positive allosteric modulator and partial agonist, ... Holzl J, Godau P (1989). "Receptor binding studies with Valeriana officinalis on the benzodiazepine receptor". Planta Medica. ...
... such as nicotinic ACh receptors -at micromolar concentrations- or adenosine A3. The exact effects of methoctramine still remain ... and other agonists, such as bethanechol or berberine). At higher concentrations, allosteric properties of methoctramine have ... Gallamine triethiodide M2 receptor Muscarinic receptor Acetylcholine Jakubík J, Zimčík P, Randáková A, Fuksová K, El-Fakahany ... As shown in the chart above, methoctramine binds preferently to M2 receptors, found mostly in the parasympathetic nerves and ...
Link, K.H.; Cruz, F.G.; Ye, H.F.; O'reilly, K.E.; Dowdell, S.; Koh, J.T. (2004). "Photo-caged agonists of the nuclear receptors ... Tsutsui, H; Shimizu, H; Mizuno, H; Nukina, N; Furuta, T; Miyawaki, A (Nov 2009). "The E1 mechanism in photo-induced beta- ... Kaplan, J. H.; Forbush, B.; Hoffman, J. F. (1978). "Rapid photolytic release of adenosine 5'-triphosphate from a protected ... Other caged hormones were used to study receptor-ligand interactions. Lipids were shown to be involved in signaling. To dissect ...
157 (1): 148.e1-148.e5. doi:10.1016/j.ahj.2008.09.017. PMID 19081411. Drepper, Michael D; Spahr, L; Frossard, JL (2012). " ... is suggested to bind covalently to CYS17 or CYS270 of the P2Y12 receptor and therefore blocking the binding of the agonist. ... P2Y12 receptor is a G-coupled receptor and is activated by adenosine diphosphate. ADP binds to the P2Y12 receptor that leads to ... Adenosine diphosphate (ADP) receptor inhibitors are a drug class of antiplatelet agents, used in the treatment of acute ...
Leukotriene-A4 hydrolase), or are the cellular receptors responsible for mediating the cellular responses to the down-stream ... 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 ... Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ...
EP3 receptor-deficient mice and/or wild type mice treated with an EP3 receptor agonist are similarly protected from allergic ... Prostaglandin E1 (PGE1), which has one less double bond than PGE2, has the same binding affinity and potency for EP3 as PGE2. ... and pathways that inhibit adenylyl cyclase which thereby lowers cellular levels of cyclic adenosine monophosphate (cAMP) to ... Eicosanoid receptor Prostaglandin E2 receptor 1 (EP1) Prostaglandin E2 receptor 2 (EP2) Prostaglandin E2 receptor 4 (EP4) ...
It has been reported that, after prolonged receptor exposure to the agonist, the agonist itself causes an agonist-induced ... Improgo MR, Scofield MD, Tapper AR, Gardner PD (October 2010). "The nicotinic acetylcholine receptor CHRNA5/A3/B4 gene cluster ... "Nicotinic acetylcholine receptor desensitization is regulated by activation-induced extracellular adenosine accumulation". The ... Nicotinic acetylcholine receptors are the best-studied of the ionotropic receptors. Since nicotinic receptors help transmit ...
CB2 receptor agonists cause a reduction in the intracellular levels of cyclic adenosine monophosphate (cAMP). CB2 also signals ... 11: e3. doi:10.1017/S1462399409000957. PMC 2768535. PMID 19152719. Galiègue S, Mary S, Marchand J, Dussossoy D, Carrière D, ... The prevalence of this trend suggests that modulating CB2 receptor activity by either selective CB2 receptor agonists or ... Unlike the CB1 receptor, in the brain, CB2 receptors are found primarily on microglia. The CB2 receptor is expressed in some ...
Subunits a3 and a4, however, mediate V-ATPase localization to the plasma membrane in osteoclasts (a3) and renal intercalated ... 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 ... The lipophilic agent xylometazoline, an alpha-adrenoreceptor agonist, displayed an increased effect when administered after ...
"Direct mapping of an agonist-binding domain within the parathyroid hormone/parathyroid hormone-related protein receptor by ... "Nuclear localization of the type 1 parathyroid hormone/parathyroid hormone-related peptide receptor in MC3T3-E1 cells: ... "Constitutive activation of the cyclic adenosine 3',5'-monophosphate signaling pathway by parathyroid hormone (PTH)/PTH-related ... It is a member of the secretin family of G protein-coupled receptors. The activity of this receptor is mediated by Gs G ...
... subsequent studies showed that it was a high affinity receptor for the arachidonic acid metabolite, lipoxin A4, but also bound ... 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- ...
In mice, CD206 or the mannose receptor marker can be used to differentiate the M2 from M1. Moreover, the in vivo translation of ... Some authors mention the M2d subtype activation as a response to IL-6 and adenosines, and these macrophages are also referred ... 74 (Supplement 1): A5-6. doi:10.1136/annrheumdis-2015-207259.13. S2CID 76272907. Mackaness GB (September 1962). "Cellular ... August 2018). "TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer ...
2002). "The adenosine 2b receptor is recruited to the plasma membrane and associates with E3KARP and Ezrin upon agonist ... solute carrier family 9 isoform A3 regulatory factor 2) gene. NHERF-2 is a scaffold protein that connects plasma membrane ... "The adenosine 2b receptor is recruited to the plasma membrane and associates with E3KARP and Ezrin upon agonist stimulation". J ... "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance ...
Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic receptor Discovery and development of beta2 agonists ... 81 (1): 211.e1-7. doi:10.1016/j.urology.2012.09.011. PMID 23200975. Rang HP (2003). Pharmacology. Edinburgh: Churchill ... catalysing the formation of cyclic adenosine monophosphate (cAMP) which then activates protein kinase A, and counterbalancing ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation". The Journal of Biological ...
"Allosteric interactions between agonists and antagonists within the adenosine A2A receptor-dopamine D2 receptor heterotetramer ... Caffeine is an antagonist of all four adenosine receptor subtypes (A1, A2A, A2B, and A3), although with varying potencies. The ... this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor) and the A2A-D2 receptor heterotetramer ( ... this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A-D2 receptor heterotetramer has ...
... estrogen receptor - estrogen receptor negative - estrogen receptor positive - estrogen receptor test - estrogen replacement ... combretastatin A4 phosphate - comedo carcinoma - common bile duct - comorbidity - compassionate use trial - complementary and ... gonadotropin-releasing hormone agonist - Gonzalez regimen - Gorlin syndrome - goserelin - gossypol - gp100 - gp209-2M - GPX-100 ... adenosine triphosphate - adenovirus - adjunct agent - adjunctive therapy - adjuvant therapy - adrenocortical - Adriamycin - ...
... but differ by the site of binding to the intended receptor and the drugs' affinities to the receptor. As a result, they have a ... In long GnRH-agonist protocols there was uncertainty in the evidence of improved live birth rates but there could be increases ... 32 (1): 43.e1-7. doi:10.1016/j.urolonc.2013.05.005. PMC 4006350. PMID 23810664. Metformin use at time of RP was extracted from ... 2018). "HL156A, a novel pharmacological agent with potent adenosine-monophosphate-activated protein kinase (AMPK) activator ...
It is one of two primary endogenous agonists of human hydroxycarboxylic acid receptor 2 (HCA2, aka GPR109A), a Gi/o-coupled G ... E3. doi:10.1016/j.jaci.2019.06.029. PMID 31279007. Vatanen, T.; Franzosa, E.A.; Schwager, R.; et al. (2018). "The human gut ... The metabolite produced by this reaction is butyryl-CoA, and is produced as follows: Adenosine triphosphate + butyric acid + ... In humans, butyric acid is one of two primary endogenous agonists of human hydroxycarboxylic acid receptor 2 (HCA2), a Gi/o- ...
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... 29 (1): 185.e1-185.e7. doi:10.1016/j.jcrc.2013.09.031. PMID 24262273. Patel A, Laffan MA, Waheed U, Brett SJ (July 2014). " ... and low production of adenosine triphosphate (ATP), can cause myocardial depression, reducing cardiac contractility and causing ... There are four families of PRRs: the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I- ...
They are small molecules erythropoietin receptor agonists designed to activate the tissue-protective erythropoietin receptor. ... February 2017). "E3 Ligase RNF126 Directly Ubiquitinates Frataxin, Promoting Its Degradation: Identification of a Potential ... Frataxin assists iron-sulfur protein synthesis in the electron transport chain to generate adenosine triphosphate, the energy ... "Erythropoietin and small molecule agonists of the tissue-protective erythropoietin receptor increase FXN expression in neuronal ...
... by pattern recognition receptors such as Toll-like receptors ((TLRs)). MIR155HG (i.e. miR-155-5p) expression is greatly ... 202 (5): 466.e1-7. doi:10.1016/j.ajog.2010.01.057. PMID 20452491. Hu YL, Fong S, Largman C, Shen WF (Sep 2010). "HOXA9 ... Since microbial lipopolysaccharide (an agonist of TLR4) activates a chain of events that lead to the stimulation of the NF-κB ... Lewis BP, Burge CB, Bartel DP (Jan 2005). "Conserved seed pairing, often flanked by adenosines, indicates that thousands of ...
... full agonist at NOP, μ-opioid and δ-opioid receptors, partial agonist at κ-opioid receptor) Etorphine MCOPPB (full agonist) MT- ... inhibition by aspirin-triggered-15-epi-lipoxin A4". Journal of Immunology. 166 (6): 3650-4. doi:10.4049/jimmunol.166.6.3650. ... causing an intracellular decrease in cyclic adenosine monophosphate(cAMP) levels, an important second messenger for many signal ... receptor agonists in acute versus chronic pain: studies with bifunctional NOP/μ receptor agonists in the sciatic nerve ligation ...
A3 adenosine receptor agonist IB-MECA reverses chronic cerebral ischemia-induced inhibitory avoidance memory deficit.. *Pengfei ... Effect of Selective 5-HT6R Agonist on Expression of 5-HT Receptor and Neurotransmitter in Vascular Dementia Rats. *Haining Yu, ... Selective 5-HT6R agonist can alleviate learning deficit of VD rats, possibly via improving neurotransmitter levels in brain ...
The adenosine A3 receptor agonist, N6-(3-iodobenzyl)-adenosine-5′-N-methyluronamide, is protective in two murine models of ... The 67 kDa laminin receptor: Structure, function and role in disease. Nelson, J., Mcferran, N. V., Pivato, ǴE., Chambers, E., ...
Cordyceps sinensis acts as an adenosine A3 receptor agonist on mouse melanoma and lung carcinoma cells, and human fibrosarcoma ... and vascular endothelial growth factor receptor (VEGF) expression levels [31]. Here VEGF is a central molecule involved in the ...
A2B and A3 adenosine receptor ligands containing boron clusters as phenylisosteres and selective A3 agonists. European journal ... Synthesis and evaluation of adenosine derivatives as A1, A2A, ...
TDI decreased the stimulation of lymphocyte c-Adenosine-monophosphate (cAMP) concentrations by the receptor agonists ... isoproterenol and prostaglandin-E1. TDI by itself stimulated cAMP production. Personal monitoring identified average exposures ...
Adenosine A3 Receptor Agonists - Preferred Concept UI. M0545337. Scope note. Drugs that selectively bind to and activate ... Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.. Allowable Qualifiers:. AD administration & dosage. AE ... Adenosine A3 Receptor Agonists [D27.505.519.625.725.200.100.300] Adenosine A3 Receptor Agonists ... Adenosine A3 Receptor Agonists [D27.505.696.577.725.200.100.300] Adenosine A3 Receptor Agonists ...
Adenosine A3 Receptor Agonists 100% * Adenosine A3 Receptors 54% * Unmyelinated Nerve Fibers 50% ... Activation of Adenosine A3 Receptors Suppresses Airway Hypersensitivity: Role of Pulmonary C-Fiber Afferents. Lin, Y. ... Melatoninergic Agonists and Omega-3 Fatty Acids in Circadian Rhythm and Neuroprotection: from Cellular, Animal, to Clinical ...
Adenosine A3 Receptor Agonists 25% * Adenine 24% * N(6)-(3-iodobenzyl)-5-N-methylcarboxamidoadenosine 24% ...
A3 adenosine receptor agonist reduces brain ischemic injury and inhibits inflammatory cell migration in rats. Am J Pathol 2011; ... Functional separation of pseudopod extension and particle internalization during Fc gamma receptor-mediated phagocytosis. J Exp ... while antagonizing the endogenous actions of TGF-β with an injection of a soluble TGF-β type II receptor resulted in a drastic ...
... visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist. ... toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor ... A non-imaging high throughput approach to chemical library screening at the unmodified adenosine-A3 receptor in living cells. ... Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide- ...
... of receptor internalization and recycling by the carboxyl-terminal domains of the human A1 and rat A3 adenosine receptors: ... consequences for agonist-stimulated translocation of arrestin3. Ferguson, G., Watterson, K. R. & Palmer, T. M., 17 Dec 2002, In ...
Adenosine Family A3 receptor. View product information for catalog number - Cr1430. Downloadable pdf data sheet available. ... A3 receptor agonists and/or agonists may have important clinical value in the treatment of asthma and inflammation. ... Background: Adenosine A3 receptors are involved in a variety of intracellular signaling pathways and physiological functions. ... 1993) Molecular cloning and characterization of the human A3 adenosine receptor. Proc Natl Acad Sci USA 90:10365-10369. ...
The adenosine A3 receptor agonist, N6-(3-iodobenzyl)-adenosine-5′-N-methyluronamide, is protective in two murine models of ... Potential role of poly (adenosine 5′-diphosphate-ribose) polymerase activation in the pathogenesis of myocardial contractile ... Novel phenanthridinone inhibitors of poly (adenosine 5′-diphosphate-ribose) synthetase: potent cytoprotective and antishock ...
cAMPNOMAD Adenosine A3 Receptor Cell Line 9.995,00€. cAMPNOMAD Cells are cell lines stably co-expressing tag-free GPCRs and ... When an agonist binds to M5 Receptor, the Gq/G11 protein is activated which, in turn, triggers a cellular response mediated by ... Each vial of cAMPNOMAD Adenosine A3 Receptor Cell Line contains HEK293 cells stably expressing the following constructs:. * ... cAMPNOMAD Adenosine A1 Receptor Cell Line 9.995,00€. cAMPNOMAD Cells are cell lines stably co-expressing tag-free GPCRs and ...
The A3 adenosine receptor (A3AR) is over-expressed in human hepatocellular carcinoma (HCC) cells. Namodenoson, an A3AR agonist ... Targeting the A3 adenosine receptor to treat hepatocellular carcinoma: anti-cancer and hepatoprotective effects. ...
Adenosine A3 agonists reverse neuropathic pain via T cell-mediated production of IL-10. The A3 adenosine receptor (A3AR) has ... A Novel Combined Selective 5-HT Reuptake Inhibitor/5-HT 1A Receptor Partial Agonist/5-HT 6 Receptor Full Agonist ... A Novel Combined Selective 5-HT Reuptake Inhibitor/5-HT 1A Receptor Partial Agonist/5-HT 6 Receptor Full Agonist ... Adenosine A3 agonists reverse neuropathic pain via T cell-mediated production of IL-10 ...
Piclidenoson is a novel, first-in-class, A3 adenosine receptor agonist (A3AR) small molecule, orally bioavailable drug with an ...
Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate … ...
Adenosine/*analogs & derivatives Receptor, Adenosine A3/agonists. J Med Chem 2007 Mar 22;50(6):1222-30 2-. chloro-. N(6)-. (3- ... Other names Receptors, Adenosine A3; A3 Receptors, Adenosine; A3 Receptor, Adenosine; Adenosine A3 Receptor; Adenosine A3 ... Adenosine/*analogs & derivatives Receptor, Adenosine A3/agonists. Biochem Pharmacol 2008 Aug 15;76(4):482-94 ABEA-. X-. BY630 0 ... Boron Compounds Adenosine/*analogs & derivatives Receptor, Adenosine A3/agonists. FASEB J 2008 Mar;22(3):850-60 9-. chloro-. 5- ...
Indeed, administration of adenosine A2a receptor agonists decreases the affinity of dopamine for D2 receptors in striatal ... The A1 and A2a adenosine receptors are the subtypes primarily involved in the caffeine effect, with A2b and A3 receptors ... Interaction between adenosine A2a receptors and dopamine D2 receptors in the striatum might underlie some of the behavioral ... By antagonizing the negative modulatory effects of adenosine receptors on dopamine receptors, caffeine leads to inhibition and ...
Adenosine receptor prodrugs: synthesis and biological activity of derivatives of potent, A1-selective agonists. Maillard MC, ... A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. Jacobson KA, Nikodijević O, Shi D, Gallo ... The role of adenosine receptors in the central action of caffeine. Daly JW, Shi D, Nikodijevic O, Jacobson KA. Daly JW, et al. ... Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. ...
Interactions Between Adenosine Receptors and Cordycepin (3- Deoxyadenosine) from Cordyceps Militaris: Possible Pharmacological ... A3 receptors activated anti-inflammatory pathways in lung ischemia-reperfusion injury [161], while A3 receptor agonists ... The family of adenosine receptors includes four members: adenosine receptors A1, A2A, A2B, and A3 [7]. Adenosine is a ... Here, we summarized the pharmacological basis of adenosine, adenosine receptors, adenosine agonist cordycepin (3- ...
Adenosine A1 Receptor Agonists. *Adenosine A2 Receptor Agonists. *Adenosine A3 Receptor Agonists ... Adenosine A2 Receptor Agonists*Adenosine A2 Receptor Agonists. Adenosine A2B Receptor Agonists*Adenosine A2B Receptor Agonists ... "Adenosine A2 Receptor Agonists" by people in this website by year, and whether "Adenosine A2 Receptor Agonists" was a major or ... Purinergic P1 Receptor Agonists [D27.505.519.625.725.200.100]. *Adenosine A2 Receptor Agonists [D27.505.519.625.725.200.100.200 ...
5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine 15% ... Adenosine Deaminase Inhibitors 14% * N(6)-cyclopentyladenosine 14% * Adenosine A1 Receptor Agonists 13% ... Determination of adenosine effects and adenosine receptors in murine corpus cavernosum. Rita C. Tostes, Fernanda R.C. Giachini ... Dive into the research topics of Determination of adenosine effects and adenosine receptors in murine corpus cavernosum. ...
Functional expression of adenosine A2A and A3 receptors in the mouse dendritic cell line XS-106 European Journal of ... Vanilloid receptor agonists and antagonists are mitochondrial inhibitors: how vanilloids cause non-vanilloid receptor mediated ... Inhibitory effects of CB1 and CB2 receptor agonists on responses of DRG neurons and dorsal horn neurons in neuropathic rats. ... Oleamide is a selective endogenous agonist of rat and human CB1 cannabinoid receptors. British Journal of Pharmacology. 141(2 ...
The A3 agonist IB-MECA moderately decreased fMLP-induced MMP-9 secretion. Agonists and antagonists of the other types of ... The effect of adenosine was mimicked by the adenosine A2a receptor agonist CGS21680 and was inhibited by both the A2a ... The effect of adenosine was mimicked by the adenosine A2a receptor agonist CGS21680 and was inhibited by both the A2a ... The effect of adenosine was mimicked by the adenosine A2a receptor agonist CGS21680 and was inhibited by both the A2a ...
An adenosine receptor agonist does not mimic and an adenosine receptor antagonist does not prevent the effects of ADA ... Inhibition of adenosine kinase prevents the accumulation of dATP in ADA-inhibited FTOC. The ability of 5′A5′dAdo to correct ... The general adenosine receptor agonist 5′-N-ethylcarboxamidoadenosine (NECA), the general adenosine receptor antagonist 8-[4 ... Adenosine receptor expression. Adenosine receptor expression was analyzed by RT-PCR with RNA prepared from day-15 fetal ...
... methylamides as A3 adenosine receptor (AR) agonists, we discovered μM binding hits at the δ-opioid receptor (DOR) and ... methylamides as A3 adenosine receptor (AR) agonists, we discovered μM binding hits at the δ-opioid receptor (DOR) and ... methylamides as A3 adenosine receptor (AR) agonists, we discovered μM binding hits at the δ-opioid receptor (DOR) and ... Repurposing of a nucleoside scaffold from adenosine receptor agonists to opioid receptor antagonists. ACS Omega. 2018 Oct 31;3( ...
Adenosine receptor A2b. MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLA.... unknown. agonist. Adenosine receptor A3. ... Adenosine receptor A1. MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVS.... unknown. agonist. Adenosine receptor A2a. ... Adenosine is also indicated in the treatment of supraventricular tachycardia.[L31998] Adenosine was granted FDA approval on 30 ... The structure of adenosine was first described in 1931,[A229823] though the vasodilating effects were not described in ...
  • 8-(3-Chlorostyryl)caffeine (CSC) is a selective A2-adenosine antagonist in vitro and in vivo. (nih.gov)
  • The effect of adenosine was mimicked by the adenosine A2a receptor agonist CGS21680 and was inhibited by both the A2a antagonist SCH5826 and A2a RNA silencing. (lih.lu)
  • Functionalized congeners, when a chemically functionalized string is usually integrated at an insensitive site on the pharmacophore, have already been designed from your agonist and antagonist ligands of varied G proteinCcoupled receptors (GPCRs). (thetechnoant.info)
  • In the first trial, various doses of adenosine (an endogenous P1 receptor agonist), and its synthetic antagonist CGS-15943, were injected intracerebroventricularly (ICV) to the chicks and the cumulative food intake was measured at definite time intervals. (ac.ir)
  • The A3 adenosine receptor (A3AR) is over-expressed in human hepatocellular carcinoma (HCC) cells. (bvsalud.org)
  • Namodenoson, an A3AR agonist, induces de-regulation of the Wnt and NF-kB signaling pathways resulting in apoptosis of HCC cells. (bvsalud.org)
  • Piclidenoson is a novel, first-in-class, A3 adenosine receptor agonist (A3AR) small molecule, orally bioavailable drug with an excellent safety profile demonstrating evidence of efficacy in Phase II clinical studies. (canfite.com)
  • 2000) A (3) adenosine receptor ligands: history and perspectives. (multispaninc.com)
  • A2A, and A3 receptor functionalized congeners possess yielded macromolecular conjugates, irreversibly binding AR ligands for receptor inactivation and crosslinking, radioactive probes that make use of prosthetic organizations, immobilized ligands for affinity chromatography, and dual-acting ligands that work as binary medicines. (thetechnoant.info)
  • To explore the relationship between both of these cardioprotective ARs as well as the question which receptor may be the even more essential anti-ischemic receptor, we designed specific binary ligands by tethering functionalized congeners. (thetechnoant.info)
  • Therapeutic Potential of Highly Selective A3 Adenosine Receptor Ligands in the Central and Peripheral Nervous System. (unifi.it)
  • cAMP NOMAD ADORA1 Cell Line allows to assay compounds analyzing the G-Protein signalling pathway by Go involving receptor activation. (innoprot.com)
  • When an agonist binds to ADORA1, Go protein is activated which, in turn, triggers a cellular response mediated by cAMP. (innoprot.com)
  • When an agonist binds to [Arg8]‐AVP, the Gs protein is activated which, in turn, triggers a cellular response mediated by cAMP via adenylate cyclase stimulation. (innoprot.com)
  • The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP. (reference.md)
  • Adenosine A1 and A2A receptor regulation of protein phosphatase 2A in the murine heart. (umassmed.edu)
  • Adenosine A2A receptor stimulation increases angiogenesis by down-regulating production of the antiangiogenic matrix protein thrombospondin 1. (umassmed.edu)
  • In vitro pharmacological approaches to the study of G protein-coupled receptors: radioligand binding, autoradiography, 2nd messenger assays (cAMP, cGMP, inositol phosphates) intracellular Ca2+ measurements, immunohistochemistry, reporter gene assays, Western blotting, primary cell culture. (nottingham.edu.my)
  • The inhibition of MMP-9 secretion by adenosine, as well as the calcium effect, was prevented by the protein kinase A inhibitor H-89. (lih.lu)
  • While screening off-target effects of rigid (N)methanocarba-adenosine 5′-methylamides as A 3 adenosine receptor (AR) agonists, we discovered μM binding hits at the δ-opioid receptor (DOR) and translocator protein (TSPO). (elsevier.com)
  • This group, which initial reported "type":"entrez-protein","attrs":"text message":"CGS21680″,"term_id":"878113053″,"term_text message":"CGS21680″CGS21680 37 PF-04217903 as an A2A AR agonist, partnered with this lab to find out if the functionalized congener strategy could be prolonged towards the A2A AR. (thetechnoant.info)
  • It is well known that there is complementarity in shape and electrostatics between a ligand molecule and its receptor protein. (biomedcentral.com)
  • P-selectin, soluble endothelial protein C receptor, soluble thrombomodulin, plasminogen activator inhibitor 1, ADAMTS-13, von Willebrand factor, tissue factor, soluble intercellular adhesion molecule 1, and vascular cell adhesion molecule 1 were more elevated in LF patients than in controls. (cdc.gov)
  • Endothelial protein C receptor, thrombomodulin, intercellular adhesion molecule 1, plasminogen activator inhibitor 1, D-dimer, and hepatocyte growth factor were higher in fatal than nonfatal LF cases. (cdc.gov)
  • Osteoclasts] express this receptor called RANK and [RANKL], which is a protein that's expressed on the surface of osteoblasts, and there's also a soluble form," Dr. Cronstein said. (the-rheumatologist.org)
  • Adenosine receptor prodrugs: synthesis and biological activity of derivatives of potent, A1-selective agonists. (nih.gov)
  • Initial clinical experience with regadenoson, a novel selective A2A agonist for pharmacologic stress single-photon emission computed tomography myocardial perfusion imaging. (umassmed.edu)
  • Binary medicines with combined selectivity for both A1 and A3 ARs had been produced through the covalent linking of functionalized congeners of adenosine agonists, each which is usually selective for either the A1 or the A3 AR subtype. (thetechnoant.info)
  • MRS 1740 65 and MRS 1741 66, thiourea-linked regioisomers of the binary conjugate, had been highly powerful and selective in radioligand-binding assays for the A1 and A3 ARs (Ki ideals of 0.7C3.5 nM) weighed against the A2A AR. (thetechnoant.info)
  • Regadenoson is a newer, selective adenosine 2A receptor agonist initially studied in myocardial perfusion imaging with nuclear scintigraphy techniques [ 3 , 4 ]. (cdc.gov)
  • A catecholamine non-selective beta-adrenergic agonist typically used to treat bradycardia and heart block. (drugbank.com)
  • For instance, the ADAC conjugate 64 bound to the rat A1 receptor using a Ki worth of PF-04217903 31 nM also to the rat -opioid receptor using a Ki worth of 150 nM. (thetechnoant.info)
  • Georgiou P , Zanos P , Garcia-Carmona JA, Hourani S , Kitchen I , Laorden ML, Bailey A. Methamphetamine abstinence induces changes in μ-opioid receptor, oxytocin and CRF systems: Association with an anxiogenic phenotype. (neurotree.org)
  • adiponectin receptor 2 [Source:HGNC. (gsea-msigdb.org)
  • Lower levels of complement proteins and anti-microbial proteins and peptides contribute to neonatal susceptibility to infection, while elevated levels of adenosine, adiponectin, and adrenomedullin in neonatal blood may influence immune cell polarization. (frontiersin.org)
  • Adenosine A2A and beta-adrenergic calcium transient and contractile responses in rat ventricular myocytes. (umassmed.edu)
  • In midrange doses, it acts on beta-adrenergic receptors to increase heart rate and contractility, improve cardiac output, and enhance conduction (increasing sinoatrial rate) in the heart. (medscape.com)
  • Strong alpha-receptor stimulant with little beta-adrenergic activity that produces vasoconstriction of arterioles in the body, helping increase systemic vascular resistance. (medscape.com)
  • Neutrophils were activated by N-formylmethionyl- leucyl-phenylalanine (fMLP) in the presence or absence of adenosine or adenosine analogs. (lih.lu)
  • Al-Hasani R , Foster JD, Metaxas A, Ledent C, Hourani SM , Kitchen I , Chen Y. Increased desensitization of dopamine Dâ‚‚ receptor-mediated response in the ventral tegmental area in the absence of adenosine A(2A) receptors. (neurotree.org)
  • In contrast, dipyridamole induces vasodilation indirectly, by blocking adenosine reuptake and increasing endogenous adenosine. (cdc.gov)
  • Georgiou P , Zanos P , Hourani S , Kitchen I , Bailey A. Cocaine abstinence induces emotional impairment and brain region-specific upregulation of the oxytocin receptor binding. (neurotree.org)
  • Zanos P , Wright SR, Georgiou P , Yoo JH , Ledent C, Hourani SM , Kitchen I , Winsky-Sommerer R , Bailey A. Chronic methamphetamine treatment induces oxytocin receptor up-regulation in the amygdala and hypothalamus via an adenosine A2A receptor-independent mechanism. (neurotree.org)
  • Either the RANKL on the surface of osteoblasts or the soluble form binds to the receptor on the osteoclast precursors, and that induces differentiation to form osteoclasts. (the-rheumatologist.org)
  • Its beta2-agonist effects include bronchodilation, chronotropic cardiac activity, and positive inotropic effects. (medscape.com)
  • Recent animal model studies have shown that A3 receptors play important roles in brain ischemia, immunosuppresion, and bronchospasm. (multispaninc.com)
  • It also causes bronchospasm and mast cell degranulation via A3 receptors. (cdc.gov)
  • A long acting beta2-adrenoceptor agonist for the management of lung diseases associated with bronchospasm. (drugbank.com)
  • A beta-2 adrenergic agonist used to treat bronchospasm, asthma, and COPD. (drugbank.com)
  • Cordycepin (3-deoxyadenosine) is an activator of adenosine receptors. (fortunejournals.com)
  • Adenosine acts as an activator (agonist) on (purinergic) adenosine receptors throughout the body. (selfdecode.com)
  • During osteoclast differentiation, one receptor that is particularly noteworthy is receptor activator of nuclear factor-κB (RANK) and RANK-ligand (RANKL). (the-rheumatologist.org)
  • Through the activation of adenosine receptors A1, A2A, A2B and A3, adenosine plays an important role in protecting against acute lung injury and brain injury. (fortunejournals.com)
  • Cannabidiol enhances microglial phagocytosis via transient receptor potential (TRP) channel activation. (nottingham.edu.my)
  • Adenosine released during cardiac ischemia exerts a powerful, protective impact in the center via activation of A1 and A3 receptors [42,45,74], which activate different defensive signaling cascades. (thetechnoant.info)
  • One objective was to utilize this ligand device to check the hypothesis that activation of both receptors exerts a cardioprotective impact significantly higher than activation of either receptor independently. (thetechnoant.info)
  • In the present study, we investigated the effects of adenosine A 2A receptor (A 2A AR) activation on resident lung cells after IR injury using an isolated, bufferperfused murine lung model. (typeset.io)
  • Methods: To assess the protective effects of A2AAR activation, three groups of C57BL/6J mice were studied: a sham group (perfused for 2 hr with no ischemia), an IR group (1 hr ischemia + 1 hr reperfusion) and an IR+ATL313 group where ATL313, a specific A 2A AR agonist, was included in the reperfusion buffer after ischemia. (typeset.io)
  • Activation of the A2A adenosine receptor by regadenoson produces coronary vasodilation and increases coronary blood flow (CBF). (drugcentral.org)
  • Regadenoson is a more potent vasodilator than adenosine and exhibits selectivity for the coronary circulation relative to the renal, peripheral and mesenteric circulation in animals [ 5 ]. (cdc.gov)
  • Adenosine (Adenocard) is an FDA-approved drug, primarily used to treat irregular heartbeat (arrhythmias), in addition to pain and high blood pressure in the lungs (pulmonary hypertension). (selfdecode.com)
  • What Is Adenosine (Adenocard)? (selfdecode.com)
  • Adenocard is one of the brand names adenosine is available under. (selfdecode.com)
  • In conclusion, we show here that adenosine inhibits MMP-9 secretion by neutrophils. (lih.lu)
  • Stimulation of adenosine A2A receptors inhibits expression of netrin-1 and its receptor Unc5b during osteoclastogenesis, and blocking netrin-1 or Unc5b diminishes inflammatory bone destruction. (the-rheumatologist.org)
  • Milrinone inhibits PDE III, producing an increase in intracellular cyclic adenosine monophosphate (cAMP), which raises intracellular calcium levels and thereby improving cardiac inotropy and peripheral vasodilation. (medscape.com)
  • Regadenoson is low affinity agonist (Ki 1.3 uM) for the A2A adenosine receptor, with at least 10-fold lower affinity for the A1 adenosine receptor (Ki 16.5 uM), and weak, if any, affinity for the A2B and A3 adenosine receptors. (drugcentral.org)
  • Regadenoson, dipyridamole and adenosine are commonly used vasodilators in myocardial perfusion imaging for the detection of obstructive coronary artery disease. (cdc.gov)
  • There are few comparative studies of the vasodilator properties of regadenoson, adenosine and dipyridamole in humans. (cdc.gov)
  • Fifteen healthy normal volunteers, with Framingham score less than 1% underwent vasodilator stress testing with regadenoson (400 μg bolus), dipyridamole (0.56 mg/kg) and adenosine (140 μg /kg/min) on separate days. (cdc.gov)
  • Twenty minutes later, stress imaging was performed at peak vasodilation, i.e. 70 seconds after regadenoson, 4 minutes after dipyridamole infusion and between 3-4 minutes of the adenosine infusion. (cdc.gov)
  • 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). (cdc.gov)
  • 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). (cdc.gov)
  • 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). (cdc.gov)
  • 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 = 0.07) and between adenosine and dipyridamole (2.12 ± 0.27 vs. 1.77 ± 0.33, p = 0.01). (cdc.gov)
  • Based on fully quantitative perfusion using CMR, regadenoson and adenosine have similar vasodilator efficacy and are superior to dipyridamole. (cdc.gov)
  • Adenosine, a naturally produced nucleoside, has been shown to have cardioprotective effects and to inhibit secretion of various cytokines. (lih.lu)
  • Ex Vivo Perfusion With Adenosine A2A Receptor Agonist Enhances Rehabilitation of Murine Donor Lungs After Circulatory Death. (umassmed.edu)
  • Thymocyte development past the CD4 - CD8 - stage is markedly inhibited in adenosine deaminase-deficient (ADA-deficient) murine fetal thymic organ cultures (FTOCs) due to the accumulation of ADA substrates derived from thymocytes failing developmental checkpoints. (jci.org)
  • Adenosine A3 receptors are involved in a variety of intracellular signaling pathways and physiological functions. (multispaninc.com)
  • Adenosine increased intracellular cAMP concentration and accelerated the return to baseline of the intracytoplasmic calcium peak. (lih.lu)
  • A potential role for cannabinoid receptors in the therapeutic action of fenofibrate. (nottingham.edu.my)
  • Four adenosine receptors have been identified (A1, A2a, A2B, and A3), but as a drug, it mainly activates receptors in the so-called cardiac atrioventricular (AV) nodal tissue and those within the blood vessels to achieve its therapeutic effects [ 8 ]. (selfdecode.com)
  • TDI decreased the stimulation of lymphocyte c-Adenosine-monophosphate (cAMP) concentrations by the receptor agonists isoproterenol and prostaglandin-E1. (cdc.gov)
  • However, prolactin also binds to specific receptors in the gonads, lymphoid cells, and liver. (medscape.com)
  • A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. (reference.md)
  • Therefore, adenosine may represent a new approach to prevent matrix degradation and remodeling after myocardial injury. (lih.lu)
  • The myocyte versions utilized cultured myocardial muscle mass cells from chick embryo, either Rabbit Polyclonal to Chk2 (phospho-Thr387) ventricular cells expressing indigenous adenosine A1 and A3 ARs or designed atrial cells, expressing either human being A3 receptors only or both human being A1 and A3 receptors. (thetechnoant.info)
  • Ex vivo lung perfusion with adenosine A2A receptor agonist allows prolonged cold preservation of lungs donated after cardiac death. (umassmed.edu)
  • 2008) Bench-to-bedside review: adenosine receptors - promising targets in acute lung injury? (multispaninc.com)
  • Adenosine, a mediator of innate immunity, is abundantly secreted by the injured lung tissues during inflammation. (fortunejournals.com)
  • Adenosine is approved by the FDA and widely used for treating surgical pain, nerve pain, lung hypertension, and certain types of irregular heartbeat (arrhythmias) [ 1 , 2 , 3 , 4 ]. (selfdecode.com)
  • The long-term (trophic) actions of purine and pyrimidine nucleosides and nucleotides in promoting migration and proliferation of both vascular smooth muscle and endothelial cells via P1 and P2Y receptors during angiogenesis and vessel remodeling during restenosis after angioplasty are described. (typeset.io)
  • There is dual control of vascular tone by ATP released as a cotransmitter with noradrenaline from perivascular sympathetic nerves to cause vasoconstriction via P2X1 receptors, whereas ATP released from endothelial cells in response to changes in blood flow (producing shear stress) or hypoxia acts on P2X and P2Y receptors on endothelial cells to produce nitric oxide and endothelium-derived hyperpolarizing factor, which dilates vessels. (typeset.io)
  • Production of anti-inflammatory adenosine by ecto-5′-nucleotidase (CD73) helps maintain endothelial barrier function. (thelancet.com)
  • We utilized a book style in which brand-new binary conjugates of adenosine functionalized congeners which were pharmacologically complementary had been synthesized and examined in a book cardiac myocyte style of adenosine-elicited cardioprotection. (thetechnoant.info)
  • This agent stimulates beta1- and alpha-adrenergic receptors, thereby increasing cardiac muscle contractility and heart rate, as well as vasoconstriction. (medscape.com)
  • The caffeine in guarana might block the affects of adenosine, which is often used by doctors to do a test called a cardiac stress test. (medlineplus.gov)
  • Adenosine is nonselective and causes negative chronotropic, dromotropic and inotropic effects via A1 receptors. (cdc.gov)
  • Compuestos que se unen selectivamente a los RECEPTORES DE ADENOSINA A3, activándolos. (bvsalud.org)
  • Jing Du, Weijing Kan, Hongkun Bao, Yue Jia, Jian Yang, Hongxiao Jia, Interactions Between Adenosine Receptors and Cordycepin (3-Deoxyadenosine) from Cordyceps Militaris: Possible Pharmacological Mechanisms for Protection of the Brain and the Amelioration of Covid-19 Pneumonia. (fortunejournals.com)
  • Here, we summarized the pharmacological basis of adenosine, adenosine receptors, adenosine agonist cordycepin (3'-deoxyadenosine), and Cordyceps product in the brain protection and amelioration of pneumonia to provide useful information to cope with the global pandemic of novel coronavirus (COVID-19). (fortunejournals.com)
  • This review discusses the adenosine receptor-mediated pharmacological effects of Cordyceps and cordycepin on acute and chronic pneumonia and the subsequent organ damage. (fortunejournals.com)
  • Cordyceps and cordycepin products could be used as a potential medicinal adenosine receptor agonist that can play a beneficial role in the amelioration of Covid-19 pneumonia and protection of brain. (fortunejournals.com)
  • Adenosine has many physiological roles in the brain, and in rodents, it changes food intake when applied centrally. (ac.ir)
  • Metaxas A, Al-Hasani R , Farshim P, Tubby K, Berwick A, Ledent C, Hourani S , Kitchen I , Bailey A. Genetic deletion of the adenosine A(2A) receptor prevents nicotine-induced upregulation of α7, but not α4β2* nicotinic acetylcholine receptor binding in the brain. (neurotree.org)
  • A2A receptors also inhibit osteoclast differentiation and stimulate osteoblast expression of axonal guidance proteins, which further regulate osteoclast differentiation. (the-rheumatologist.org)
  • Wells L, Opacka-Juffry J, Fisher D, Ledent C, Hourani S , Kitchen I . In vivo dopaminergic and behavioral responses to acute cocaine are altered in adenosine A(2A) receptor knockout mice. (neurotree.org)
  • While scrutinizing and modeling the chemistry of linkage from the catecholamines to peptides through small-molecule derivatives with elongated stores, Goodman and co-workers discovered 2-adrenergic agonists which were superpotent. (thetechnoant.info)
  • We investigated the effect of central injection of the purine molecule adenosine on both food and fat intakes in neonatal chicks. (ac.ir)
  • Effects of chronic caffeine on adenosine, dopamine and acetylcholine systems in mice. (nih.gov)
  • The structure of adenosine was first described in 1931,[A229823] though the vasodilating effects were not described in literature until the 1940s. (rcsb.org)
  • Sympathomimetic agent with primarily beta1-agonist effects, increasing heart rate and blood pressure. (medscape.com)
  • Its alpha-agonist effects include increased peripheral vascular resistance, reversed peripheral vasodilatation, systemic hypotension, and vascular permeability. (medscape.com)
  • Adenosine A2 Receptor Agonists" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)
  • A3 adenosine receptor agonist IB-MECA reverses chronic cerebral ischemia-induced inhibitory avoidance memory deficit. (semanticscholar.org)
  • A beta-2 adrenergic receptor agonist and bronchodilator used for the treatment of asthma and chronic obstructive pulmonary disease (COPD). (drugbank.com)
  • Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS. (bvsalud.org)
  • Unlike adenosine, other drugs for treating arrhythmias are categorized under classes I to IV of antiarrhythmic agents (Vaughan-Williams classification scheme) [ 8 ]. (selfdecode.com)
  • The present study suggests that in the avian central nervous system, P1 receptors are entailed in the regulation of food and fat intake in an antagonistic manner. (ac.ir)
  • Zanos P , Georgiou P , Rojo Gonzalez L, Hourani S , Chen Y, Kitchen I , Kieffer BL , Winsky-Sommerer R, Bailey A. Emotional impairment and persistent up-regulation of mGlu5 receptor following morphine abstinence: implications of an mGlu5-MOPr interaction. (neurotree.org)
  • In low doses, dopamine acts on dopaminergic receptors in renal and splanchnic vascular beds, causing vasodilatation in these beds. (medscape.com)
  • In high doses, it acts on alpha-adrenergic receptors to increase systemic vascular resistance and raise blood pressure. (medscape.com)