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.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.
Learn about regadenoson: What is it used for, what you need to know before taking, important warnings and safety info, how to take, side effects and more...
Structure, properties, spectra, suppliers and links for: 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide.
6-Amino-1,3-dihydro-2H-purin-2-one; CAS Number: 3373-53-3; Linear Formula: C5H5N5O; find Ambeed, Inc.-AMBH46A96504 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich
You are viewing an interactive 3D depiction of the molecule 1-(7h-purin-6-yl)-n-[3-(trifluoromethyl)phenyl]-4-piperidinecarboxamide (C18H17F3N6O) from the PQR.
You are viewing an interactive 3D depiction of the molecule 8-azido-9-(5-o-phosphono-d-ribofuranosyl)-9h-purin-6-amine (C10H13N8O7P) from the PQR.
... -First A2A Adenosine Receptor Agonist Approved for Use as Pharmacolo... Stress Agent in Myocardial Perfusion Imaging- ...PALO ALTO Calif. and DEERFIELD Ill. April 10 FirstCall/...Lexiscan is the first A2A adenosine receptor agonist shown to be safe...,CV,Therapeutics,and,Astellas,Announce,FDA,Approval,for,Lexiscan(TM),(regadenoson),Injection,biological,advanced biology technology,biology laboratory technology,biology device technology,latest biology technology
This work done by an eminent group in the area raises concerns over the use of regadenoson for clinical stress testing, whether done by PET or SPECT. Invasive and pharmacologic studies had previously demonstrated peak regadenoson effect at approximately 1-2 minutes after injection, consistent with the findings of the present study. Stress labs which are not already following a 1- to 2-minute delay may wish to consider introducing one.. There are several reasons to view these results with caution, however. First, many prior studies had compared regadenoson to other vasodilators using a variety of techniques including PET, SPECT, and invasive methods. In general, no significant differences or only minimal differences, below the level of clinical relevance, were observed. The reasons for the discrepancies are unclear.. One longstanding concern with regards to regadenoson has been the use of a single fixed dose without weight adjustment, as is usually done for other vasodilators. The investigators ...
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Regadenoson produced higher stress MBF than dipyridamole and adenosine (3.58 ± 0.58 vs. 2.81 ± 0.67 vs. 2.78 ± 0.61 ml/min/g, p = 0.0009 and p = 0.0008 respectively). Regadenoson had a much higher heart rate response than adenosine and dipyridamole respectively (95 ± 11 vs. 76 ± 13 vs. 86 ± 12 beats/ minute) When stress MBF was adjusted for heart rate, there were no differences between regadenoson and adenosine (37.8 ± 6 vs. 36.6 ± 4 μl/sec/g, p = NS), but differences between regadenoson and dipyridamole persisted (37.8 ± 6 vs. 32.6 ± 5 μl/sec/g, p = 0.03). The unadjusted MPR was higher with regadenoson (3.11 ± 0.63) when compared with adenosine (2.7 ± 0.61, p = 0.02) and when compared with dipyridamole (2.61 ± 0.57, p = 0.04). Similar to stress MBF, these differences in MPR between regadenoson and adenosine were abolished when adjusted for heart rate (2.04 ± 0.34 vs. 2.12 ± 0.27, p = NS), but persisted between regadenoson and dipyridamole (2.04 ± 0.34 vs. 1.77 ± 0.33, p = ...
Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients.1-4 In addition, both adenosine and dipyridamole produce severe bronchoconstriction when given to asthmatics. Because of its ultrashort half-life, adenosine must be administered by a constant IV infusion.. Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A1, A2B, and A3.5 The discovery of highly selective and relatively short-acting adenosine receptor A2A agonists6-9 has opened the ...
Approximately 250 patients who are referred for a nuclear stress testing of the heart with regadenoson (Lexiscan®) will be recruited to participate in the study. Following regadenoson (administered as part of a stress routine test protocol) participants will receive either aminophylline (75 mg - intravenously) or a matching inactive placebo (sterile salt water) injection. Participants will be surveyed for gastrointestinal symptoms and other side effects related to regadenoson. The frequency and severity of such side effects will be compared between the two study groups (aminophylline vs. placebo ...
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Lung transplantation currently is one way to treat a variety of serious diseases and conditions such as emph ysema, pulmonary fibrosis, and cystic fibrosis. Ischemia Reperfusion Injury (IRI) is a known problem that can happen during the first few days after a lung transplant. IRI can cause swelling of the lungs and low levels of oxygen. The most serious type of IRI can cause the transplanted lung to not work properly, it can even cause death. While new treatments and practices have been put into place to lower the chances of IRI, it is still a difficult problem to overcome after a lung transplant. Medicines called Adenosine 2A receptors (A2AR) have been studied in animals with IRI for many years. Some of these studies suggest that with the use of A2AR medicines, the chance of IRI may be lowered or prevented. Regadenoson is an A2AR drug. ...
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N,N,9-Trimethyl-9H-purin-6-amine | C8H11N5 | CID 221105 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Product Number: C6621 CAS number: 390409-17-3 unlabeled Synonyms: GS-7171 fumarate // [2H6]-N-[[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-1-methylethyl ester-L-alanine fumarate-d6. ...
Product Number: C6621 CAS number: 390409-17-3 unlabeled Synonyms: GS-7171 fumarate // [2H6]-N-[[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-1-methylethyl ester-L-alanine fumarate-d6. ...
Adenoscan® (adenosine) is an approved pharmacological stress agent indicated as an adjunct to thallium-201 myocardial perfusion scintigraphy in patients unable to exercise adequately. The investigational drug, regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist, the receptor responsible for coronary vasodilation, and is being studied for potential use as a pharmacologic stress agent in myocardial perfusion imaging (MPI) studies. This study will compare the safety and efficacy of regadenoson to that of Adenoscan in detecting reversible myocardial perfusion defects ...
Adenosine might provoke bronchospasm in certain susceptible patients such as those with asthma or those on maintenance doses of bronchodilators or steroids. The selectivity of regadenoson was therefore of great interest to study for its safety and efficacy in such patients. The final answer is not yet in, and more studies are needed, but there are some preliminary data.. Prior studies have suggested that with prophylactic pre-treatment with a B-2 agonist, adenosine could be given to patients with mild asthma or chronic obstructive lung disease (COPD). It should be noted the majority of patients with COPD but no bronchospasm could be tested with adenosine without any serious problem (39). Further, tachypnea is common after adenosine infusion and is not due to changes in airway resistance or pulmonary capillary wedge pressure but rather to stimulation of carotid body receptors (40,41).. A randomized double-blind, placebo-controlled cross-over trial assessed the safety of regadenoson in 48 patients ...
In a recent prospective, double-blind, randomized multicenter phase 3 trial, ADVANCE (Adenosine versus Regadenoson Comparative Evaluation for Myocardial Perfusion Imaging), the A2A selective adenosine receptor agonist, regadenoson, was shown to be noninferior to the nonselective vasodilator, adenosine, for detecting myocardial ischemia (1). The overall visual agreement was comparably low (in the low 60% range) for the adenosine-regadenoson and for the adenosine-adenosine comparisons. Conversely, when quantitative analysis was applied, regadenoson induced virtually identical results to adenosine-regarding the size and severity of left ventricular perfusion defect size and extent of ischemia (2). What are the regulatory implications of these findings? Should the regulatory bodies rely on subjective visual interpretation of myocardial perfusion studies, on objective quantitative programs to appraise the comparability between vasodilators, or both? What is the true standard?. In order to avoid the ...
Structure, properties, spectra, suppliers and links for: (2S)-2-(8-Iodo-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-9H-purin-9-yl)propanamide.
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3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile chemical properties, What are the chemical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile 86375-28-2, What are the physical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile ect.
chemBlink provides information about CAS # 3945-69-5, 4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methyl morpholinium chloride, DMTMM, molecular formula: C10H17ClN4O3.
Methanol,[(4,6-dimethyl-1,3,5-triazin-2-yl)amino]-(9ci)/ACM84591888 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
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Are you stress now? Let me tell you about it. Stress is simply the bodys reaction the wear and tear of life. Every single activity you engage in, every emotion you feel, whether it is asking the boss for a raise, or trying to complete an assignment, set up stress. The way your body reacts to such stress agents has much to do with your health ...
II. CÍL NÁVRHU. Cílem návrhu je umožnit novým členským státům účast v projektu Evropské hlavní město kultury před skončením platnosti stávajícího rozhodnutí v roce 2019. Návrh nemění stávající pořadí pro podávání návrhů členskými státy, ale zavádí se nový systém jmenování dvou členských států oprávněných každý rok počínaje rokem 2009 podat návrhy tak, aby v členských státech mohla být vybrána dvě hlavní města.. III. ROZBOR SPOLEČNÉHO POSTOJE. 1. Obecné poznámky. Rada v návrhu Komise neprovedla žádné změny. Komise zcela přijala 1 změnu z 5 změn navrhovaných Parlamentem (změna 1).. 2. Změny učiněné Evropským parlamentem. 2.1 Změny přijaté Radou. Rada plně potvrdila změnu navrhovanou Parlamentem a přijatou Komisí (změna 1).. 2.2 Změny nezapracované Radou. Rada stejně jako Komise usoudila, že změny 2, 3, 4 a 5 šly nad rámec návrhu, a jejich zapracování nepokládala za vhodné.. III. ZÁVĚRY. Rada se ...
Buy CGS 21680 (CAS 124182-57-6), a potent, selective A2A agonist. Join researchers using high quality CGS 21680 from Abcam and achieve your mission, faster.
A review. The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain G protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various species, including rat and human, and its sequences are highly similar across species, ranging from 85% identity between human and mouse and 95% identity between rat and mouse. The A2B receptors show a ubiquitous distribution, the highest levels are present in cecum, colon and bladder, followed by blood vessels, lung, eye and mast cells. Through A2B receptors adenosine seems to cause mast cells degranulation, vasodilation, cardiac fibroblast proliferation, inhibition of Tumor Necrosis Factor (TNF-α), increased synthesis of interleukin-6 (IL-6), stimulation of Cl- secretion in intestinal epithelia and hepatic glucose prodn. Hence, A2B adenosine receptor agonists could be useful ...
ALI is one of the leading causes of morbidity and mortality of critical illness with extremely limited therapeutic options. In the present study, we pursued the hypothesis that tissue-specific adenosine signaling events through the A2B adenosine receptor contribute to lung protection and can thus be targeted for ALI treatment. To make progress on this front, we performed a head-to-head comparison of mice with genetic deletion of Adora2b in the myeloid lineage, vascular endothelial cells, or alveolar epithelial cells. Interestingly, we only observed a phenotype in mice with tissue-specific Adora2b deletion in alveolar epithelial cells, closely resembling the observed detrimental effects of global Adora2b deletion during ALI. Interestingly, the injurious effects of our two-hit model where an inflammatory event (i.t. LPS treatment) is followed by injurious mechanical ventilation seem to be supra-additive compared with the effects of injurious ventilation or LPS i.t. alone. Based on these findings ...
Particularly preferably, Z21 is 2,4-dichloro-1,3,5-triazin-6-ylf 2-chloro-4-(3-(2-suifatoethylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-chloro-4-(4-(2-su!fatoethy!sulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-chloro-4-(3-(vinylsulfonyl)-phenylarnino)-1 t3,5-triazin-6-yl, 2-chloro4-(4-(vinylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-ch!oro-4-(N-methy!-N-(2-(2-sulfatoethylsulfonyl)-ethy!)-amino)-1,3,5-triazin-6-yl, 2-ch!oro-4-(N-phenyl-N-(2-(2-sulfatoethylsulfonyl)-ethyl)-amino)-1,3,5-tria2in-6-yl, 2-fluoro-4-morpholino-1,3,5-triazin-6-yI, 2-fluoro-4-(2-sulfophenyl-amino)-1,3,5-triazin-6-yl, 2-fluoro-4-(3-sulfophenylamino)-1,3,5-triazin-6-yl, 2-fluoro-4-(4-sulfophenylamino)-1,3,5-triazin-6-yl, 2-fiuoro-4-(3-trimethylammonio-phenylamino)-1,3,5-triazin-6-ylf 2-fIuoro-4-(4-trirnethylammoniophenylamino)-1,3,5-triazin-6-yl, 2-fluoro-4-(3-(2-sulfatoethylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl( 2-fluoro-4-(4-(2-sulfatoethylsulfonyl,-phenylamino)-1 f3,5-triazin-6-yl, ...
Two main findings arise from this study: (1) the adenosine A2A receptor antagonist SCH 58261 shows neuroprotective effects in an excitotoxic rat model of HD; and (2) the inhibition of QA-evoked increase in extracellular glutamate seems to be the main mechanism of the effects elicited by SCH 58261.. The finding that SCH 58261 significantly prevented most of the effects induced by the intrastriatal injection of an excitotoxin is in line with some findings suggesting that activation of A2A receptors could participate in the generation of excitotoxicity. Adenosine A2A receptor agonists have been reported indeed to stimulate glutamate release in the rat striatum (Popoli et al., 1995; Corsi et al., 1999). Moreover, in previous experiments, we observed that the intrastriatal injection of the adenosine A2A receptor agonist CGS 21680, together with QA, potentiated QA-induced mortality in a dose-dependent way (50, 75, and 83% of mortality after 3, 6, and 12 nmol QA plus CGS 21680, respectively; P. Popoli, ...
9H-Purin-2-amine, 9-methyl- (9CI) (CAS 5752-08-9) Market Research Report 2018 aims at providing comprehensive data on 9h-purin-2-amine, 9-methyl- (9ci)
While regadenoson has become the vasodilator stress agent of choice and has streamlined and simplified stress protocols in many nuclear stress laboratories, the adverse effect of dyspnea is still experienced by many patients, and even more so by those with COPD and asthma. While patients and practitioners should anticipate this symptom, several studies have shown that the subjective experience of dyspnea is not correlated with and is not caused by bronchoconstriction. Available data from observational studies as well as controlled clinical trials, as summarized in Table 1, indicate that the use of regadenoson in patients with mild to moderate asthma and mild to moderate COPD is safe. The current data in patients with severe COPD, while limited, are reassuring and indicate that regadenoson is probably safe, particularly in those with stable lung disease. Clinical data are limited in COPD patients who require 24-hour/day home oxygen administration, have previously been intubated for respiratory ...
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BioAssay record AID 243741 submitted by ChEMBL: Inhibition of [3H]CGS-21680 binding to Adenosine A2A receptor expressed in CHO cells.
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for h
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... and vascular endothelial growth factor and are induced by IL-6 and A2 adenosine receptor agonist (A2R). Mregs can arise ... Induction of Mregs is strongly linked with the interaction of Fc receptors located on the surface of Mregs with Fc fragments of ... The first signal is stimulation by M-CSF, GM-CSF, PGE2, adenosine, glucocorticoid, or apoptotic cells. The second signal can be ... It has been shown that anti-TNF monoclonal antibodies interacting with Fcγ receptor of Mregs induce differentiation of Mregs ...
... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
... which triggers intracellular signal transduction via both adenosine A1 receptors and two sub-types of adenosine A2 receptors ( ... Moreover, minoxidil contains a nitric oxide moiety and may act as a nitric oxide agonist. This may cause follicles in the ... The expression of SUR2B in dermal papilla cells might play a role in the production of adenosine. Minoxidil induces cell growth ... Minoxidil is an adenosine 5'-triphosphate-sensitive potassium channel opener, causing hyperpolarization of cell membranes. ...
... the therapeutic potential for both agonists and antagonists of the adenosine receptors was highlighted for A2 receptors, and in ... Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. Notable adenosine ... In order to be able to characterize the function of adenosine A2 receptors, potent and selective A2-receptor antagonists were ... adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti- ...
"Stimulation of high-affinity adenosine A2 receptors decreases the affinity of dopamine D2 receptors in rat striatal membranes ... "A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers". Proc. Natl. Acad. Sci. U.S.A. ... In 1991, the phenomenon of receptor crosstalk was observed between adenosine A2A (A2A) and dopamine D2 receptor (DRD2) thus ... two adenosine A2A receptors and two dopamine D2 receptors). Maggio and co-workers showed in 1993 the ability of the muscarinic ...
Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an ... Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. Thus, it may prove ... The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... A1 receptors are also present in smooth muscle throughout the vascular system. The adenosine A1 receptor has been found to be ...
The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... Experimental evidence suggests that adenosine and adenosine agonists can activate Trk receptor phosphorylation through a ... All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... Adenosine is an endogenous agonist of the ghrelin/growth hormone secretagogue receptor. However, while it is able to increase ...
These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. Signalization in ... It has been shown that collagen, exposed after the injury to the endothelial cover of the vessel, plays as an agonist in ... cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). ... TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. Both receptors mediate phospholipase C ...
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... This is a valuable guide to design potential 5HT1D receptor agonists. When sumatriptan binds there is major conformational ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... Goadsby, P.J., Serotonin 5-HT1B/1D receptor agonists in migraine - Comparative pharmacology and its therapeutic implications. ...
... full agonist at NOP, μ-opioid and δ-opioid receptors, partial agonist at κ-opioid receptor) Etorphine MCOPPB (full agonist) MT- ... Fukuda K, Shoda T, Morikawa H, Kato S, Mima H, Mori K (1998). "Activation of phospholipase A2 by the nociceptin receptor ... 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 ...
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ...
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 ... and PGH2 is then converted to thromboxane A2 (TXA2) by thromboxane synthase. TXA2 increases platelet aggregation, promotes ... Activation of the P2Y1 receptor initiates platelet aggregation in response to ADP. The P2Y1 receptor is required for ADP- ...
PAR1 and PAR4 receptors), platelet-derived thromboxane A2 (TxA2) (TP receptor) and ADP (P2Y1 and P2Y12 receptors) that is ... Adenosine acts by binding to purinergic receptors and influencing adenylyl cyclase activity and the formation of cAMP and PKA ... In general terms, platelet activation initiated by agonist takes to a signaling cascade that leads to an increase of the ... Therefore, there are four main transmembrane receptor types: G protein coupled receptors (GPCRs), tyrosine kinase receptors ( ...
... the DP1-dependent stimulation of adenosine formation and subsequent simulation of the Adenosine A2A receptor by adenosine. In ... "Characterization of the recombinant human prostanoid DP receptor and identification of L-644,698, a novel selective DP agonist ... thromboxane A2, with PGD2 being more than 100-fold more potent than PGE2 in binding to and stimulating DP1. (http://www. ... Prostaglandin receptors Prostanoid receptors Prostaglandin DP2 receptor Eicosanoid receptor GRCh38: Ensembl release 89: ...
... its acidification of endosomes is critical in receptor endocytosis as low pH tends to drive ligand release as well as receptor ... Adenosine triphosphate (ATP) is then hydrolyzed by the V1 domain of the enzyme, enabling both the rotation of the central stalk ... Isoforms a1 and a2 target V-ATPase intracellularly, to synaptic vesicles and endosomes respectively. Subunits a3 and a4, ... The lipophilic agent xylometazoline, an alpha-adrenoreceptor agonist, displayed an increased effect when administered after ...
In vitro, D5 receptors show high constitutive activity that is independent of binding any agonists. D5 receptor is highly ... Prado C, Contreras F, González H, Díaz P, Elgueta D, Barrientos M, Herrada AA, Lladser Á, Bernales S, Pacheco R (2012). " ... Mello, F. G. (October 1978). "The Ontogeny of Dopamine-Dependent Increase of Adenosine 3',5'-Cyclic Monophosphate in the Chick ... It belongs to the D1-like receptor family along with the D1 receptor subtype. D5 receptor is a subtype of the dopamine receptor ...
... receptors are glutamate receptors particularly important in long-term potentiation in neurons. These receptors have been linked ... Funk, C.K. and Koob, G.F. (2007). A CRF2 agonist administered into the central nucleus of the amygdala decreases ethanol self- ... Katsura, M., Shibasaki, M., Hayashida, S., Torigoe, F., Tsujimura, A., Ohkuma, S. (2006) Increase in expression of a1 and a2/d1 ... Pandey, S.C., Roy, A., Zhang, H. (2003). The decreased phosphorylation of cyclic adenosine monophosphate (cAMP) response ...
... s secrete thromboxane A2, which acts on the platelet's own thromboxane receptors on the platelet surface (hence the so- ... After adding an agonist, the platelets aggregate, resulting in greater light transmission, which is detected by the photocell. ... "Differential Sensitivity of Various Markers of Platelet Activation with Adenosine Diphosphate". BioNanoScience. 9 (1): 53-58. ... These receptors trigger intraplatelet signaling, which converts GPIIb/IIIa receptors to their active form to initiate ...
The cytosolic PLA2 set (i.e. cPLA2s) of PLA2 enzymes (cPLA2; see Phospholipase A2#Cytosolic phospholipases A2) in particular ... Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... As a second drug added to corticosteroids, leukotriene inhibitors appear inferior to Beta2-adrenergic agonist drugs in the ... may serve as a mobile lid over ALOX5's substrate-binding site An Adenosine triphosphate (ATP) binding site; ATP is crucial for ...
... trienoic acid as a thromboxane A2 receptor antagonist with minimal intrinsic activity". British Journal of Haematology. 101 (1 ... Synthetic BLT2 agonists may be useful for speeding the healing of chronic ulcerative wounds, particularly in patients with, for ... to inhibit platelet aggregation responses to various agents by stimulating platelets to raise their levels of Cyclic adenosine ... BLT1 receptor) and its low affinity BLT2 receptor (Kd=23 nM); both receptors are G protein coupled receptors that, when ligand- ...
Most commonly, enzymes known as adenosine deaminases acting on RNA (ADARs) catalyze adenosine to inosine (A to I) transitions. ... miR-382 is the target for the dopamine receptor D1 (DRD1), and its overexpression results in the upregulation of DRD1 and delta ... Choi WY, Giraldez AJ, Schier AF (October 2007). "Target protectors reveal dampening and balancing of Nodal agonist and ... "High mobility group A2 protein and its derivatives bind a specific region of the promoter of DNA repair gene ERCC1 and modulate ...
Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ... A myriad of agonists have also been shown to induce the translocation of PKCε from the cytosolic to particulate fraction in ... Perjés Á, Skoumal R, Tenhunen O, Kónyi A, Simon M, Horváth IG, Kerkelä R, Ruskoaho H, Szokodi I (2014). "Apelin increases ... Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ...
Such drugs are called receptor agonists. An example of a receptor agonist is morphine, an opiate that mimics effects of the ... adenosine triphosphate (ATP), adenosine Others: acetylcholine (ACh), anandamide, etc. In addition, over 100 neuroactive ... Rinaman L (February 2011). "Hindbrain noradrenergic A2 neurons: diverse roles in autonomic, endocrine, cognitive, and ... Direct-binding agonists can be further characterized as full agonists, partial agonists, inverse agonists. Direct agonists act ...
Vilazodone is a 5-HT1A receptor partial agonist while vortioxetine is a 5-HT1A receptor agonist and 5-HT3 and 5-HT7 receptor ... One such possible mechanism is the increased levels of cyclic adenosine monophosphate (cAMP) as a result of interference with ... PMID 21701626.{{cite journal}}: CS1 maint: multiple names: authors list (link) Romero-Martínez Á, Murciano-Martí S, Moya-Albiol ... Fluvoxamine is an agonist of the σ1 receptor, while sertraline is an antagonist of the σ1 receptor, and paroxetine does not ...
... which acts as a selective agonist at these receptors. When the NMDA receptor is activated by the binding of two co-agonists, ... GLUA2, GluR2, GluRB, GluR-B, GluR-K2, HBGR2. GLUA3, GluR3, GluRC, GluR-C, GluR-K3. GLUA4, GluR4, GluRD, GluR-D ... Adenosine reuptake inhibitor (AdoRI). *Angiotensin II receptor antagonist. *Endothelin receptor antagonist. *NK1 receptor ... The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, or quisqualate receptor) is a ...
Membrane permeability to Ca++ increases, possibly due, in part, to impairment in the Ca++ pump that depends on adenosine ... Refining the value of secretory phospholipase A2 as a predictor of acute chest syndrome in sickle cell disease: results of a ... Endothelin Receptor Antagonists. *Iron Chelators. *Antiemetics. *Adrenergic Agonists. *Vaccines. *Show All. * Questions & ...
Glycoprotein IIb/IIIa receptor antagonists include abciximab, [82, 83] eptifibatide, [84] and tirofiban. [85] These drugs ... Clopidogrel (thienopyridine) inhibits adenosine 5'-diphosphate (ADP)-dependent activation of the glycoprotein IIb/IIIa complex ... Aspirin permanently impairs the cyclooxygenase pathway of thromboxane A2 production in platelets, in this way inhibiting ... Asthma or emphysema that is sensitive to beta agonists. * Peripheral vascular disease ...
It simulates adenyl cyclase to convert adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP) and causes ... Albuterol relaxes bronchial smooth muscle by acting on beta2 receptors but has little effect on cardiac muscle contractility. ... Prednisone blocks release of inflammatory mediators by inhibiting phospholipase A2. It may be useful in patients who have ... Alpha/Beta Agonists. Class Summary. Bronchodilators are among the most common therapies for bronchiolitis; studies have ...
... selective agonists at the coronary artery A2-adenosine receptor.. Ojha, T N; Singh, P; Tiwari, S; Sharma, R C. ... A theoretical structure-activity relationship study of 2-alkoxy-adenosines: ...
Acetylcholine receptor agonist (disposition) {734716009 , SNOMED-CT } Adenosine A2 receptor agonist (disposition) {734621000 , ... Farnesoid X receptor agonist (disposition) {734896001 , SNOMED-CT } Gamma-aminobutyric acid receptor agonist (disposition) { ... Serotonin receptor agonist (disposition) {783924002 , SNOMED-CT } Sigma-1 receptor agonist (disposition) {735943004 , SNOMED-CT ... Gamma-hydroxybutyrate receptor agonist (disposition) {782539002 , SNOMED-CT } Growth hormone secretagogue receptor agonist ( ...
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 ... Purinergic P1 Receptor Agonists [D27.505.696.577.725.200.100]. *Adenosine A2 Receptor Agonists [D27.505.696.577.725.200.100.200 ...
... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
... an alternative for predicting A2 A adenosine receptors agonists, Eur. J. Med. Chem., 2006, 41, 56-62. 10.1016/j.ejmech.2005.08. ...
Adenosine A2 receptor agonist Current Synonym true false 3644880010 Adenosine A2 receptor agonist product Current Synonym true ... Product containing adenosine A2 receptor agonist Current Synonym true false 3745973017 Adenosine A2 receptor agonist-containing ... Product containing adenosine A2 receptor agonist (product). Code System Preferred Concept Name. Product containing adenosine A2 ... Product containing adenosine A2 receptor agonist (product) {432062000 , SNOMED-CT } Parent/Child (Relationship Type) Product ...
Adenosine A2 receptor agonist. References:. Hutchison, A. J.; Williams, M.; de Jesus, R.; Yokoyama, R.; Oei, H. H.; Ghai, G. R ... 2-[[4-(2-Carboxyethyl)phenylethyl]amino]adenosine-5-N-ethylcarboxamide hydrochloride; 2-p-(2-Carboxyethyl)phenethylamino-5-N- ...
Relaxation of the ovine isolated iris sphincter by adenosine receptor agonists: lack of effect of adenosine A1 and A2 receptor ... Characterization of adenosine receptors mediating the vasodilator effects of adenosine receptor agonists in the ... Relaxation of mouse isolated aorta to adenosine and its analogues does not involve adenosine A1, A2 or A3 receptors European ... Differential distribution of adenosine A2 receptors in the epididymal and prostatic portions of the rat vas deferens. European ...
... the adenosine A2 receptors were down-regulated, as indicated by the fact that the ability of the A2 receptor agonist 5-N- ... Glucocorticoid receptor activation leads to up-regulation of adenosine A1 receptors and down-regulation of adenosine A2 ... Glucocorticoid receptor activation leads to up-regulation of adenosine A1 receptors and down-regulation of adenosine A2 ... Glucocorticoid receptor activation leads to up-regulation of adenosine A1 receptors and down-regulation of adenosine A2 ...
2-chloro-adenosine (2-Cl-ADO) > R-phenylisopropyl adenosine (R-PIA). 4. The known potent A2 adenosine receptor (A2AR) agonist, ... but not the A1 adenosine receptor agonist, N6-phenyl adenosine (N6-phenyl ADO, 10 microM) markedly increased 125I efflux rate ( ... 3. The P1 agonists tested (at 0.01 and 0.1 mM) revealed a rank order of potency of 5-N-ethylcarboxamine adenosine (NECA) > ... 1. P1 purinoceptor agonists like adenosine have been shown to stimulate Cl- transport in secretory epithelia. In the present ...
... selective agonists at the coronary artery A2-adenosine receptor. Indian Journal of Biochemistry & Biophysics. 1995 Feb; 32(1): ... selective agonists at the coronary artery A2-adenosine receptor. ... structure-activity relationship study of 2-alkoxy-adenosines: ... A theoretical structure-activity relationship study of 2-alkoxy-adenosines: ...
... if dogs express functional TLR4 and if LPS-induced platelet activation requires co-stimulation with ADP or thromboxane A2 (TxA2 ... Functional Toll-like receptor 4 (TLR4) has been characterized in human and murine platelets indicating that platelets play a ... Agonists of toll-like receptor (TLR)2 and TLR4 are unable to modulate platelet activation by adenosine diphosphate and platelet ... lipopolysaccharide-triggered platelet activation is dependent on adenosine diphosphate and thromboxane A2 in dogs. BMC Vet Res ...
Use of selective adenosine receptor antagonists revealed that adenosine A2(B) receptors (A2(B)R) mediate the early HAS1 ... The adenosine receptor agonist NECA (10 μM) caused a strong induction of HA synthase (HAS)1 at 6 h and a weaker induction again ... In conclusion, the current data suggest that adenosine via adenosine A2(B)R and A2(A)R/A3R induces HAS1. In turn a HA-rich ... Novel effects of adenosine receptors on pericellular hyaluronan matrix: implications for human smooth muscle cell phenotype and ...
COMBINED TREATMENT WITH HYALURONAN INHIBITOR PEP-1 AND A SELECTIVE ADENOSINE A2 RECEPTOR AGONIST REDUCES INFLAMMATION IN ... COMBINED TREATMENT WITH HYALURONAN INHIBITOR PEP-1 AND A SELECTIVE ADENOSINE A2 RECEPTOR AGONIST REDUCES INFLAMMATION IN ... Adenosine A2A receptor activation and hyaluronan fragment inhibition reduce inflammation in mouse articular chondrocytes ... Adenosine A2A receptor activation and hyaluronan fragment inhibition reduce inflammation in mouse articular chondrocytes ...
... and A2 adenosine receptor (A2R) agonists and produce higher levels of IL-10, TGF-β, and VEGF but minimal levels of IL-12, TNF-α ... used a peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist to polarize neutrophils to an N2 anti-inflammatory ... The activated profibrotic myeloid cells solely express folate receptor β. The folate-targeted TLR7 agonist (FA-TLR7-54) ... Liraglutide (Lira), a GLP-1R receptor agonist, has been reported to promote the angiogenic ability of endothelial cells [240]. ...
... , Federico S, Spalluto G, Discover ... A general description of each receptor is reported with novel agonist and antagonist structures, patented in 2008 - 2011. ... Therapeutic potential of A2 and A3 adenosine receptor: a review of novel patented ligands. Author(s): Federico S, Spalluto G ... Introduction: Adenosine exerts its effects by interacting with G-protein coupled receptors (GPCR) namely A1, A2A, A2B and A3, ...
... is an important physiological agonist that plays a vital role in normal hemostasis and thrombosis. ... In addition, the P2Y12 ... Adenosine diphosphate (ADP) released from platelet dense granules triggers the binding of fibrinogen to platelet receptor GPIIb ... Most platelet agonists, including ADP, activate platelets via cell surface receptors coupled to heterotrimeric GTP-binding ... von Willebrand and thromboxane A2. ... ADP stands for adenosine diphosphate, and its not only one of ...
TRPA1, TRPV1, TRPV2, TRPV3, PPARγ, 5-HT1A, A2 and A1 adenosine receptors, and CBD functions as an agonist, while on GPR55, ... serotonin 1A receptor (5-HT1A); and the adenosine A2A receptor [19][20][21]. The nature of interaction is not always apparent, ... receptors, such as cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2), and the metabolizing enzymes-fatty acid amide ... In addition, CBD can have inverse agonist activity on the GPR3, GPR6, and GPR12 receptors [23]. THC and CBD also can affect the ...
Indeed, administration of adenosine A2a receptor agonists decreases the affinity of dopamine for D2 receptors in striatal ... 14] Caffeine is an inhibitor of the adenosine A2 receptor and was shown to improves motor deficits in a mouse model of ... Interaction between adenosine A2a receptors and dopamine D2 receptors in the striatum might underlie some of the behavioral ... The A1 and A2a adenosine receptors are the subtypes primarily involved in the caffeine effect, with A2b and A3 receptors ...
Adenosine A2 Receptor Agonists. Adult. Anemia, Sickle Cell. Contrast Media. Female. Forearm. Humans. Image Enhancement. Male. ... No changes were found during an infusion of the adenosine A2A agonist, regadenoson. This study provides preliminary evidence ... an adenosine A2A agonist. CEUS destruction-replenishment time-intensity data were analyzed to measure microvascular blood flow ...
Adenosine A2 Receptor Agonists. *Coronary Artery Disease. *Emergency Service, Hospital. *Exercise Test ...
Adenosine-5N-ethylcarboxamide, 5-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5-N- ... NQ301 inhibits thromboxane A2 receptor (TXA2) and synthase activity in rabbit platelets.. J Extracell Vesicles, 2021, 10(5): ... Adenosine-5N-ethylcarboxamide, 5-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5-N- ... NQ301 inhibits thromboxane A2 receptor (TXA2) and synthase activity in rabbit platelets.. J Extracell Vesicles, 2021, 10(5): ...
Local injections of adenosine A1 receptor agonists in the preoptic area of the rat produced sleep, whereas an A2A agonist did ... Later studies have indicated that blockade of adenosine A1 receptors is more important than blockade of A2 receptors to produce ... Adenosine A1 agonists, but not adenosine A2A agonists, depressed the dopamine levels (Okada et al., 1997). Because the drugs ... Adenosine A1 receptors (in contrast to adenosine A2A receptors) have been shown to influence dopamine release in slices of the ...
A 1 adenosine receptor agonists, antagonists, and allosteric modulators Gao, Z. G., Tosh, D. K., Jain, S., Yu, J., Suresh, R. R ... and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ ... GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2AAdenosine Receptor. ... N6-Substituted 5′-N-Methylcarbamoyl-4′-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual ...
D2 receptors [26]. Furthermore, CBD is an agonist at the transient receptor potential A1 (TRPA1), TRPV1 and TRPV2 [27,28,29] ... CBD blunted the cognitive impairment induced by THC in an adenosine A2A receptor-dependent manner [113] and abolished the ... Luján, M.Á.; Castro-Zavala, A.; Alegre-Zurano, L.; Valverde, O. Repeated Cannabidiol treatment reduces cocaine intake and ... and exerts a negative allosteric modulation on these receptors [12,13]. On CB2 receptors, CBD acts as a partial agonist [13]. ...
... enzymes or known PDE enzyme isoforms and did not act as an antagonist at A2 or A2 receptors. The affinity for adenosine A1, A2A ... Agonist. General Function. Protein homodimerization activity. Specific Function. Beta-adrenergic receptors mediate the ... Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.. Gene Name. ... Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline 9 ...
Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 receptors. J ... Imidazoquinoline Toll-like receptor 8 agonists activate human newborn monocytes and dendritic cells through adenosine- ... Sitkovsky MV, Ohta A. The danger sensors that STOP the immune response: the A2 adenosine receptors? Trends Immunol (2005) 26( ... Adenosine acts via an A2 receptor on human neutrophils. J Immunol (1985) 135(2):1366-71. ...
Glycoprotein IIb/IIIa receptor antagonists include abciximab, [82, 83] eptifibatide, [84] and tirofiban. [85] These drugs ... Clopidogrel (thienopyridine) inhibits adenosine 5-diphosphate (ADP)-dependent activation of the glycoprotein IIb/IIIa complex ... Aspirin permanently impairs the cyclooxygenase pathway of thromboxane A2 production in platelets, in this way inhibiting ... Asthma or emphysema that is sensitive to beta agonists. * Peripheral vascular disease ...
Adenosine receptor prodrugs: synthesis and biological activity of derivatives of potent, A1-selective agonists. Maillard MC, ... Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. ... The role of adenosine receptors in the central action of caffeine. Daly JW, Shi D, Nikodijevic O, Jacobson KA. Daly JW, et al. ... 8-(3-Chlorostyryl)caffeine (CSC) is a selective A2-adenosine antagonist in vitro and in vivo. Jacobson KA, Nikodijević O, ...
Cannabinoid Receptor I+Adenosine Receptor A2a+Mu Opioid Receptor+Dopamine Receptor D1+Adenosine A3 R (1). ... Agonists, activators, antagonists and inhibitors. Cell lines and Lysates. Multiplex miRNA assays. Multiplex Assays. By research ... Cyclin A2+CDK1+Cyclin B1+Cyclin D1+Cdks+Cyclin E1+Cyclin E2+Cytochrome P450 3A4/CYP3A4+CYP2C9+HIF-1 (1). ... Glucocorticoid Receptor+Progesterone Receptor+Mineralocorticoid Receptor+Androgen Receptor (1). * Glutamate Receptor 1 (AMPA ...
  • Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused mainly on the role of adenosine receptors in the heart, and led to several randomized controlled trials using these receptor antagonists to treat bradyasystolic arrest. (wikipedia.org)
  • Use of selective adenosine receptor antagonists revealed that adenosine A2(B) receptors (A2(B)R) mediate the early HAS1 induction, whereas late HAS1 induction was mediated via A2(A)R and A3R. (nih.gov)
  • In particular, few potent and selective A2B agonists and antagonists are actually reported and a clear SAR (structure-activity relationship) profile lacks for this AR subtype. (indexindex.com)
  • Consequently, serotonin receptor antagonists have been tested for their anti-ischemic potency in atherothrombotic disease. (moviecultists.com)
  • trial has recently confirmed the early findings on patency and suggests that adjunct treatment with glycoprotein IIb/IIIa receptor antagonists may hold promise Pergolide Mesylate for the better management of myocardial infarction. (morainetownshipdems.org)
  • However studies have shown that if ?80% of glycoprotein IIb/IIIa receptors are blocked by specific antagonists platelet aggregation is almost completely inhibited.5 Glycoprotein Iib/IIIa receptor antagonists have been found to be beneficial without fibrinolytic therapy Pergolide Mesylate in clinical trials of over 30?000 patients with unstable angina or non-Q wave myocardial infarction. (morainetownshipdems.org)
  • Thus IIb/IIIa receptor antagonists have been studied in acute myocardial infarction as adjuncts to fibrinolytic therapy to see if they improved reperfusion and prevent reocclusion. (morainetownshipdems.org)
  • For example, DOR agonist [D-Ala2, D-Leu5]-enkephalin (DADLE) reduced glutamate-induced injury in neocortical neurons and this protection is usually selectively blocked by -, but not by - or -opioid receptor antagonists [9]. (bioinf.org)
  • Previous studies showed that a DOR agonist, (+) BW373U86, increased mRNA expression of brain-derived neurotrophic factor (BDNF), a member of the neurotrophin family [29,30], in the frontal cortex, and this effect was specifically blocked by Naltrindole, but not by - or k-opioid receptor antagonists [30]. (bioinf.org)
  • The encoded protein (the A2A receptor) is abundant in basal ganglia, vasculature, T lymphocytes, and platelets and it is a major target of caffeine, which is a competitive antagonist of this protein. (wikipedia.org)
  • Other steroid hormones, including aldosterone, progesterone, testosterone, and estrogen, were much less effective, and addition of the glucocorticoid receptor antagonist RU 486 or the protein synthesis inhibitor cycloheximide prevented the up-regulation, showing that the effect was mediated via a glucocorticoid receptor-specific mechanism that involves protein synthesis. (aspetjournals.org)
  • A general description of each receptor is reported with novel agonist and antagonist structures, patented in 2008 - 2011. (indexindex.com)
  • This was mimicked by the selective adenosine A1 receptor antagonist cyclopentyltheophylline. (biologyonline.com)
  • Doxofylline does not demonstrate direct inhibition of any histone deacetylase (HDAC) enzymes or known PDE enzyme isoforms and did not act as an antagonist at A2 or A2 receptors. (drugbank.com)
  • 8-(3-Chlorostyryl)caffeine (CSC) is a selective A2-adenosine antagonist in vitro and in vivo. (nih.gov)
  • In the existing research, we identified that blocking spinal a2-ARs by intrathecal pretreatment with atipamezole (a selective a2-AR antagonist) reversed the DEX pretreatment-induced down-regulation of the thermal paw withdrawal latency and mechanical paw withdrawal threshold(Fig. 2B), and the up-regulation of spinal p-ERK1/two (Fig. 2C) and the spinal c-Fos protein expression in pH five. (adenosine-receptor.com)
  • GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK 2 ) receptor antagonist. (medchemexpress.com)
  • GR 64349 is a potent and highly selective NK 2 receptor peptide antagonist, with an EC 50 of 3.7 nM in rat colon. (medchemexpress.com)
  • GR 103691 is a potent, selective dopamine D 3 receptor antagonist with a K i value of 0.4 nM. (medchemexpress.com)
  • GR 125743 is a selective 5-HT 1B/1D receptor antagonist, with pK i s of 8.85 and 8.31 for wild-type h5-HT 1B and wild-type h5-HT 1D , respectively. (medchemexpress.com)
  • GR 113808 is a potent and highly selective 5-HT 4 receptor antagonist ( pK b = 8.8). (medchemexpress.com)
  • GR 94800 is a potent and selective NK 2 receptor peptide antagonist, with pK B values of 9.6, 6.4 and 6.0 for NK 2 , NK 1 and NK 3 receptors, respectively. (medchemexpress.com)
  • GR 127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. (medchemexpress.com)
  • Intracerebroventricular treatment with the DOR agonist TAN-67 (60 nmol) significantly reduced the infarct volume and attenuated neurological deficits, while Naltrindole, a DOR antagonist, aggravated ischemic damage after forebrain ischemia in rats [12]. (bioinf.org)
  • In addition, the P2Y12 receptor is also important for potentiation of platelet activation mediated by other physiological agonists including collagen, von Willebrand and thromboxane A2. (moviecultists.com)
  • Acting through cell surface receptors , ADP activates platelets resulting in shape change, aggregation, thromboxane A 2 production, and release of granule contents. (moviecultists.com)
  • They release proaggregatory materials (eg, ADP) by the release reaction, and they synthesize thromboxane A2 from arachidonic acid. (medscape.com)
  • NQ301 inhibits thromboxane A2 receptor (TXA2) and synthase activity in rabbit platelets. (selleckchem.com)
  • In animal studies, doxofylline demonstrated to attenuate bronchoconstriction, inflammatory actions and the release of thromboxane A2 (TXA2) when challenged with platelet-activating factor 9 . (drugbank.com)
  • Aspirin functions synergistically with fibrinolytic therapy to reduce mortality3 and may reduce reocclusion.4 But aspirin is a Pergolide Mesylate relatively weak antiplatelet agent and platelet activation may still continue DEPC-1 via pathways independent of thromboxane A2. (morainetownshipdems.org)
  • An increase in the release of the vasoconstrictor thromboxane A2, suggesting the activation of platelets, occurs in patients with the primary form as well as those with the secondary form of pulmonary hypertension (PH). (dovepress.com)
  • Read Post Collagen-mediated GPVI using glycoproteins the free 22 Days in May: The Birth of the cookbook of thromboxane A2( TXA2) and is the state of moderator. (wickedchopspoker.com)
  • physiologists are thromboxane A2, which enables on the credit's academic 98° levels on the ITP factor( heavily the Jewish ' body ' platelet), and those of first alternatives. (wickedchopspoker.com)
  • Murine and human platelets also express several Toll-like receptors (TLRs), suggesting that platelets can act as sentinel cells in detecting pathogen-associated molecular patterns (PAMPs) like LPS. (biomedcentral.com)
  • Adenosine diphosphate (ADP) released from platelet dense granules triggers the binding of fibrinogen to platelet receptor GPIIb-IIIa, resulting in the formation of fibrinogen bridges that link platelets into a loose aggregate. (moviecultists.com)
  • Substances such as collagen, ristocetin, arachidonic acid, adenosine 5′-diphosphate (ADP), epinephrine, and thrombin can stimulate platelets and hence induce aggregation. (moviecultists.com)
  • ADP stands for adenosine diphosphate, and it's not only one of the most important molecules in the body, it's also one of the most numerous. (moviecultists.com)
  • This initial interaction (platelet adhesion) sets the stage for other adhesive reactions that allow the platelets to interact with other agonists in the vicinity of vessel injury, such as adenosine 5'-diphosphate (ADP), subendothelial collagen, and thrombin. (medscape.com)
  • Over 100 agonists including adenosine diphosphate thrombin and adrenaline may activate platelets. (morainetownshipdems.org)
  • Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of these hybrid receptors is still only starting to be unravelled. (wikipedia.org)
  • The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, and Parkinson's disease. (wikipedia.org)
  • As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. (wikipedia.org)
  • 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)
  • Even though the primary action of caffeine may be to block adenosine receptors this leads to very important secondary effects on many classes of neurotransmitters, including noradrenaline, dopamine, serotonin, acetylcholine, glutamate, and GABA (Daly, 1993). (biologyonline.com)
  • The interaction between adenosine A2A and dopamine D2 receptors highlighted above could provide a mechanism for several actions of caffeine and some of its metabolites on dopaminergic activity. (biologyonline.com)
  • Thus, an inhibition of A2A receptors by caffeine would be expected to increase transmission via dopamine at D2 receptors (Ferré et al. (biologyonline.com)
  • Adenosine A1 receptors (in contrast to adenosine A2A receptors) have been shown to influence dopamine release in slices of the striatum (Jin et al. (biologyonline.com)
  • Adenosine A1 agonists, but not adenosine A2A agonists, depressed the dopamine levels (Okada et al. (biologyonline.com)
  • Effects of chronic caffeine on adenosine, dopamine and acetylcholine systems in mice. (nih.gov)
  • We go on to determine that this channel inhibition by Ucn1 is mediated initially by an increase in cyclic adenosine monophosphate (cAMP) and a subsequent inactivation of phospholipase A2 (PLA2), whose metabolites are known to modulate ion channels. (westminster.ac.uk)
  • There is high interest in the development of potent and selective ligands for these adenosine receptor (AR) subtypes, primarily for their therapeutic potential but also as pharmacological tools in receptor studies. (indexindex.com)
  • It consists of three components-ligands, including 2-arachidonoylglycerol (2-AG) and arachidonoyl ethanolamide (AEA or anandamide), receptors, such as cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2), and the metabolizing enzymes-fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). (encyclopedia.pub)
  • When ligands bind to the receptor, the ion channel portion of the receptor opens, allowing ions to pass across the cell membrane . (wikipedia.org)
  • Treatment with dexamethasone caused a dose- and time-dependent increase in the number of adenosine A1 receptors but did not affect the KD or the proportions of receptors in high and low affinity states. (aspetjournals.org)
  • Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline 9 . (drugbank.com)
  • The affinity for adenosine A1, A2A and A2B receptors are reported to be all higher than 100 µM 6 . (drugbank.com)
  • GR 159897 has little or no affinity for NK 1 and NK 3 receptors. (medchemexpress.com)
  • The BDNF-mediated effect is very likely mediated through activation of TrkB, a high-affinity tyrosine kinase receptor [33,34,35]. (bioinf.org)
  • DHT is certainly 10 times stronger an androgen because of its higher affinity binding for the androgen receptor than testosterone [5]. (gpr139.info)
  • Glucocorticoid receptor activation leads to up-regulation of adenosine A1 receptors and down-regulation of adenosine A2 responses in DDT1 MF-2 smooth muscle cells. (aspetjournals.org)
  • The A2A receptor binds with the Gs protein at the intracellular site of the receptor. (wikipedia.org)
  • Isatuximab (anti-CD38) (SAR650984, hu38SB19) is an IgG1-derived monoclonal antibody that binds to a specific extracellular epitope of CD38 receptor with a kd of 0.12 nM. (selleckchem.com)
  • The neurotransmitter then binds to receptors located on the postsynaptic neuron . (wikipedia.org)
  • Substance which binds to cell receptors normally responding to naturally occurring substances and which produces a response of its own. (zfin.org)
  • This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices, as well as an extracellular N-terminus and an intracellular C-terminus. (wikipedia.org)
  • Extracellular adenosine gathers in response to cellular stress and breakdown through interactions with hypoxia induced HIF-1α. (wikipedia.org)
  • Abundant extracellular adenosine can then bind to the A2A receptor resulting in a Gs-protein coupled response, resulting in the accumulation of intracellular cAMP, which functions primarily through protein kinase A to upregulate inhibitory cytokines such as transforming growth factor-beta (TGF-β) and inhibitory receptors (i.e. (wikipedia.org)
  • Extracellular nucleotide homeostasis and P2 nucleotide receptors play important roles in regulation of the innate immune system ( 1 , 2 , 3 ). (aai.org)
  • These receptor proteins are typically composed of at least two different domains: a transmembrane domain which includes the ion pore, and an extracellular domain which includes the ligand binding location (an allosteric binding site). (wikipedia.org)
  • The cys-loop receptors are named after a characteristic loop formed by a disulfide bond between two cysteine residues in the N terminal extracellular domain. (wikipedia.org)
  • [4] [5] A binding site in the extracellular N-terminal ligand-binding domain gives them receptor specificity for (1) acetylcholine (AcCh), (2) serotonin, (3) glycine, (4) glutamate and (5) γ-aminobutyric acid (GABA) in vertebrates. (wikipedia.org)
  • Cys-loop receptors have structural elements that are well conserved, with a large extracellular domain (ECD) harboring an alpha-helix and 10 beta-strands. (wikipedia.org)
  • A crystal structure of the A2A receptor bound with the agonist NECA and a G protein-mimic has been published in 2016 (PDB code: 5g53). (wikipedia.org)
  • The adenosine receptor agonist NECA (10 μM) caused a strong induction of HA synthase (HAS)1 at 6 h and a weaker induction again after 24 h. (nih.gov)
  • 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. (selleckchem.com)
  • A1 and A2A receptors are believed to regulate myocardial oxygen demand and to increase coronary circulation by vasodilation. (wikipedia.org)
  • IMSEAR at SEARO: A theoretical structure-activity relationship study of 2-alkoxy-adenosines: selective agonists at the coronary artery A2-adenosine receptor. (who.int)
  • The aim of this study was to examine the regulation and function of HA matrix in response to adenosine in human coronary artery SMC (HCASMC). (nih.gov)
  • Most platelet agonists, including ADP, activate platelets via cell surface receptors coupled to heterotrimeric GTP-binding proteins or G proteins. (moviecultists.com)
  • The activity of the encoded protein, a G protein-coupled receptor family member, is mediated by G proteins which activate adenylyl cyclase, which induce synthesis of intracellular cAMP. (wikipedia.org)
  • G protein-coupled receptor 155 [Source:H. (gsea-msigdb.org)
  • G protein-coupled receptor 85 [Source:HG. (gsea-msigdb.org)
  • DOR is usually a type of G protein-coupled receptor and is widely distributed in the mammalian central nervous system, especially in the cortex and striatum [6,7]. (bioinf.org)
  • The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). (wikipedia.org)
  • Vilanterol (GW642444) is a potent, orally active and long-acting β2-AR (β2-adrenergic receptor) agonist with inherent 24-hour activity. (immune-system-research.com)
  • Adenosine exerts its effects by interacting with G-protein coupled receptors (GPCR) namely A1, A2A, A2B and A3, respectively. (indexindex.com)
  • Findings from several laboratories indicate that astrocytes only express IP3 receptor type 2 (IP3R2) and that a knockout of IP3R2 obliterates the GPCR-dependent astrocytic Ca 2+ responses. (frontiersin.org)
  • Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. (immune-system-research.com)
  • Experimental Design: Multiplexed barcoded RNA analysis was used to measure the expression of 141 genes from five GEPs (Oncotype Dx, MammaPrint, PAM50, EndoPredict, and Breast Cancer Index) in breast cancer tissue sections and tumor-rich cores from 71 estrogen receptor (ER) positive node-negative tumors, on which clinical Oncotype Dx testing was previously performed. (regenerativemedicine.net)
  • Adenosine A2A and beta-adrenergic calcium transient and contractile responses in rat ventricular myocytes. (umassmed.edu)
  • The gene encodes a protein which is one of several receptor subtypes for adenosine. (wikipedia.org)
  • This paper concentrates on reviewing the therapeutic potential of A2 and A3 ARs, which represent the most interesting subtypes of recent years. (indexindex.com)
  • Here, we show the expression of the endogenous peptide urocortin1 (Ucn1) and two receptor subtypes, CRF-R1 and CRF-R2, in primary human articular chondrocytes (AC) and demonstrate its role as an autocrine/paracrine pro-survival factor. (westminster.ac.uk)
  • 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)
  • GR 103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR) . (medchemexpress.com)
  • Recent studies have exhibited that this activation of the -opioid receptor (DOR) elicits a neuroprotective effect against such injuries. (bioinf.org)
  • Formation of the TLR4 receptor complex in response to LPS initiates signalling pathways leading to proinflammatory cytokine production and inflammatory response. (biomedcentral.com)
  • In addition, CBD is able to inhibit cell proliferation and to increase apoptosis in different types of cancer models.These activities seem to involve also alternative pathways, such as the interactions with TRPV and GRP55 receptor complexes. (grecc.org)
  • Targeting a multitude of specific enzymes and receptors, they either stimulate or block particular cellular signaling pathways that are implicated in various kinds of cancer. (axonmedchem.com)
  • Naturally, all products in this section can also be found by their specific biological targets as listed in the sections of enzymes , receptors , transcription factors , proteins and/or signaling pathways . (axonmedchem.com)
  • Research regarding dysregulation of neurotransmitter systems in FXS, including the metabotropic glutamate receptor (mGluR)1/5 pathway and γ aminobutyric acid (GABA) A pathways, have led to new targeted treatments for FXS. (biomedcentral.com)
  • These results suggest that under physiological conditions P2X7R are maintained in a conformationally restrained state that limits channel gating and coupling of the receptor to signaling pathways that regulate caspase-1. (aai.org)
  • This depotentiation does not require NMDA receptors, group I metabotropic glutamate receptors, or L-type calcium channels, but involves adenosine acting at A 1 receptors. (jneurosci.org)
  • cys-loop receptors , ionotropic glutamate receptors and ATP-gated channels . (wikipedia.org)
  • Tsuyoshi Goto, Scope: Peroxisome proliferator-activated receptor alpha (PPAR-α) is a ligand-activated transcription factor that regulates lipid and carbohydrate metabolism. (nara-wu.ac.jp)
  • We investigate the effects of naturally occurring PPAR-α agonists, phytol, and its metabolite phytanic acid, on obesity-induced metabolic disorders using a mouse model. (nara-wu.ac.jp)
  • Adenosine receptor prodrugs: synthesis and biological activity of derivatives of potent, A1-selective agonists. (nih.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)
  • In conclusion, the current data suggest that adenosine via adenosine A2(B)R and A2(A)R/A3R induces HAS1. (nih.gov)
  • 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)
  • Several studies have described CBD as amultitargetmolecule, acting as an adaptogen, and as amodulator, in different ways, depending on the type and location of disequilibrium both in the brain and in the body,mainly interactingwith specific receptor proteins CB1 and CB2. (grecc.org)
  • and (2) cytoplasmic/non-receptor tyrosine kinases, which act as regulatory proteins, playing key roles in cell differentiation, motility, proliferation, and survival [ 7 ] . (vpjournal.net)
  • High-dose epoprostenol has a pro-apoptotic effect on PAH-PASMCs via the IP receptor and upregulation of Fas ligand (FasL) in vitro. (dovepress.com)
  • If these receptors are ligand-gated ion channels, a resulting conformational change opens the ion channels, which leads to a flow of ions across the cell membrane. (wikipedia.org)
  • The receptors are subdivided with respect to the type of ion that they conduct (anionic or cationic) and further into families defined by the endogenous ligand. (wikipedia.org)
  • The prototypic ligand-gated ion channel is the nicotinic acetylcholine receptor . (wikipedia.org)
  • Several unique characteristics distinguish the P2X7R from other ionotropic P2X or metabotropic P2Y nucleotide receptors. (aai.org)
  • It only displays an inhibitory action against PDE2A1 and antagonism at adenosine A(2A) at high concentrations 7 . (drugbank.com)
  • To characterize the third regulatory mechanism in more detail, mice were studied that are genetically deficient in TGF due to targeted deletion of the gene coding for A1 adenosine receptors (A1AR), the major signaling pathway of TGF [ O19 ]. (uni-freiburg.de)
  • 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)
  • Description: A sandwich quantitative ELISA assay kit for detection of Rat Cholinergic Receptor, Nicotinic, Alpha 1 (CHRNa1) in samples from tissue homogenates or other biological fluids. (elisastrip.com)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Rat Cholinergic Receptor, Nicotinic, Alpha 1 (CHRNa1) in tissue homogenates, cell lysates, cell culture supernates and other biological fluids. (elisastrip.com)
  • Description: Enzyme-linked immunosorbent assay based on the Double-antibody Sandwich method for detection of Rat Cholinergic Receptor, Nicotinic, Alpha 1 (CHRNa1) in samples from tissue homogenates, cell lysates, cell culture supernates and other biological fluids with no significant corss-reactivity with analogues from other species. (elisastrip.com)
  • We performed a prospective study, CEUS perfusion imaging of resting forearm muscle was performed in adults with SCD: 1) during and after a pain episode, and 2) before, during, and after a 24-hour infusion of the investigative agent, regadenoson, an adenosine A2A agonist. (mcw.edu)
  • No changes were found during an infusion of the adenosine A2A agonist, regadenoson. (mcw.edu)
  • This, in turn, results in either a depolarization , for an excitatory receptor response, or a hyperpolarization , for an inhibitory response. (wikipedia.org)
  • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (umassmed.edu)
  • Serine/threonine kinases (STKs) transfer phosphate group from Adenosine triphosphate (ATP) to the OH (hydroxyl) group on the side chain of a serine or threonine amino acid residue in a protein, producing ADP and a phosphoprotein. (vpjournal.net)
  • Sucrose nonfermenting 1-related kinase (SNRK) is a serine/threonine kinase and a member of the adenosine monophosphate (AMP)-activated protein kinase (AMPK) family that is involved in the metabolic regulatory mechanisms in various cell types. (vpjournal.net)
  • adenosine monophosphate deaminase 3 [Sou. (gsea-msigdb.org)
  • Another Weight Loss Clinic Distinguished Ingredient Found In Slimming Capsules Is Apple Cider Vinegar John Goodman Weight Loss Rich In Acetic Acid , It Helps You To Shed Weight In Several Other Ways The Enzyme Ampk Adenosine Monophosphate Shark Tank Weight Loss Supplement Activated Protein Kinase Is Activated By The Dissolution Of Acetic Acid Into Acetate And Hydrogen This Automatically Reduces The Fat That S Being Stored Within The Stomach And Liver. (org.vn)
  • The function of such receptors located at synapses is to convert the chemical signal of presynaptically released neurotransmitter directly and very quickly into a postsynaptic electrical signal. (wikipedia.org)
  • In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors and lacks stimulating effects. (drugbank.com)
  • In the past years, by modulating A2 and A3ARs, several new possible therapeutic applications were discovered. (indexindex.com)
  • Adenine di-Phosphate (ADP) is an important physiological agonist that plays a vital role in normal hemostasis and thrombosis . (moviecultists.com)
  • Therefore, in contrast to the prevailing literature, we find that neither receptor-driven astrocyte Ca 2+ fluxes nor, by extension, gliotransmission is likely to be a major modulating force on the physiological processes underlying behavior. (frontiersin.org)
  • In dexamethasone-treated cells the A1 receptor agonist (-)-N6-phenylisopropyladenosine [(R)-PIA] was 3 times more potent as an inhibitor of cAMP formation induced by isoprenaline than in untreated cells. (aspetjournals.org)
  • GR 79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a K i s of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. (medchemexpress.com)
  • In addition, A2A receptor can suppress immune cells, thereby protecting tissue from inflammation. (wikipedia.org)
  • Functional Toll-like receptor 4 (TLR4) has been characterized in human and murine platelets indicating that platelets play a role in inflammation and hemostasis during sepsis. (biomedcentral.com)
  • One of the major components of the outer membrane of Gram negative bacteria is the endotoxin, lipopolysaccharide (LPS), whose receptor, Toll-like receptor 4 (TLR4), is present on the surface of a wide variety of immune cells such as dendritic cells, epithelial cells, polymorphonuclear cells and macrophages. (biomedcentral.com)
  • Genes up-regulated in comparison of dendritic cells (DC) stimulated with LPS (TLR4 agonist) at 2 h versus DC cells stimulated with poly(I:C) (TLR3 agonist) at 2 h. (gsea-msigdb.org)
  • The P2X7 receptor (P2X7R) is an ATP-gated cation channel that activates caspase-1 leading to the maturation and secretion of IL-1β. (aai.org)
  • Particular attention has focused on the ability of the P2X7 receptor (P2X7R) to trigger proteolytic maturation and secretion of the proinflammatory cytokines IL-1β and IL-18 from macrophages. (aai.org)
  • TU-100 activates transient receptor potential ankyrin 1 (TRPA1) expressed on intestinal epithelial cells, followed by release of the vasodilator peptide adrenomedullin (ADM). (hindawi.com)
  • Systemic administration of DOR agonist DADLE or Deltorphin-D (variant) reduces infarct volume after transient middle cerebral artery occlusion (MCAO) [24,25]. (bioinf.org)
  • In contrast to nitric oxide and similar to angiotensin II, sympathoadrenergic stimulation by phenylephrine or by baroreflex activation only slightly enhanced MR [ A2 ]. (uni-freiburg.de)
  • Conclusions DOR activation rescues TrkB signaling by reversing ischemia/reperfusion induced decrease in the full-length TrkB receptor and reduces brain injury CEP dipeptide 1 in ischemia/reperfusion Introduction Cerebral ischemia/hypoxia causes neuronal injury and prospects to severe neurological disorders with few effective therapies available. (bioinf.org)
  • 1995). In these regions of the brain there is a marked discrepancy between the distribution of the receptor and the corresponding mRNA. (biologyonline.com)
  • PLA2 (phospholipases A2) are enzymes that can hydrolyze the fatty acyl ester bond at the sn-2 position of glycerophospholipid. (immune-system-research.com)
  • 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)
  • Deletion of the adenosine A(2A) receptor in mice enhances spinal cord neurochemical responses to an inflammatory nociceptive stimulus. (neurotree.org)
  • Adenosine plays an important role in the phenotypic regulation of vascular smooth muscle cells (VSMC) and is thought to inhibit inflammatory responses during atherosclerosis. (nih.gov)
  • In: J Ethnopharmacol (1996 Jan) 50(1):1-12 ISSN: 0378-8741 The isolated rat stomach fundus preparation, a sensitive bioassay to evaluate serotonin-(5-HT) like activity, was used as a model to study the effects of parthenolide (PAR), a component to Tanacetum parthenium (feverfew), on 5-HT storage, release and stimulation of the 5-HT2B receptor. (henriettesherbal.com)
  • BMS-378806 (BMS 806) selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus. (selleckchem.com)
  • Androgen Receptor Genetic Variant Predicts COVID-19 Disease Severity: A Prospective Longitudinal Study of Hospitalized COVID-19 Male Patients. (bioq.com)
  • Prostate cancer level of resistance to castration occurs because tumors find the metabolic capacity for converting precursor steroids to 5-dihydrotestosterone (DHT), promoting signaling with the androgen receptor (AR) as well as the advancement of castration-resistant prostate tumor (CRPC)1C3. (aboutsciencenow.info)
  • Multitarget restorative strategy can be used to inhibit two or more enzymes act on an enzyme and a receptor or impact an ion channel and a transporter. (bioinf.org)
  • 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)
  • Cynarin blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells. (selleckchem.com)