Exercise Test: Controlled physical activity which is performed in order to allow assessment of physiological functions, particularly cardiovascular and pulmonary, but also aerobic capacity. Maximal (most intense) exercise is usually required but submaximal exercise is also used.Tomography, Emission-Computed, Single-Photon: A method of computed tomography that uses radionuclides which emit a single photon of a given energy. The camera is rotated 180 or 360 degrees around the patient to capture images at multiple positions along the arc. The computer is then used to reconstruct the transaxial, sagittal, and coronal images from the 3-dimensional distribution of radionuclides in the organ. The advantages of SPECT are that it can be used to observe biochemical and physiological processes as well as size and volume of the organ. The disadvantage is that, unlike positron-emission tomography where the positron-electron annihilation results in the emission of 2 photons at 180 degrees from each other, SPECT requires physical collimation to line up the photons, which results in the loss of many available photons and hence degrades the image.Myocardial Perfusion Imaging: The creation and display of functional images showing where the blood is flowing into the MYOCARDIUM by following over time the distribution of tracers injected into the blood stream.Thallium Radioisotopes: Unstable isotopes of thallium that decay or disintegrate emitting radiation. Tl atoms with atomic weights 198-202, 204, and 206-210 are thallium radioisotopes.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)Radiopharmaceuticals: Compounds that are used in medicine as sources of radiation for radiotherapy and for diagnostic purposes. They have numerous uses in research and industry. (Martindale, The Extra Pharmacopoeia, 30th ed, p1161)Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Alkynes: Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Receptor, Adenosine A3: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Siloxanes: Silicon polymers that contain alternate silicon and oxygen atoms in linear or cyclic molecular structures.Silicon: A trace element that constitutes about 27.6% of the earth's crust in the form of SILICON DIOXIDE. It does not occur free in nature. Silicon has the atomic symbol Si, atomic number 14, and atomic weight [28.084; 28.086].Polymers: Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).Uterine Neoplasms: Tumors or cancer of the UTERUS.Sex Cord-Gonadal Stromal Tumors: Neoplasms derived from the primitive sex cord or gonadal stromal cells of the embryonic GONADS. They are classified by their presumed histogenesis and differentiation. From the sex cord, there are SERTOLI CELL TUMOR and GRANULOSA CELL TUMOR; from the gonadal stroma, LEYDIG CELL TUMOR and THECOMA. These tumors may be identified in either the OVARY or the TESTIS.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Consumer Product SafetyApiaceae: A large plant family in the order Apiales, also known as Umbelliferae. Most are aromatic herbs with alternate, feather-divided leaves that are sheathed at the base. The flowers often form a conspicuous flat-topped umbel. Each small individual flower is usually bisexual, with five sepals, five petals, and an enlarged disk at the base of the style. The fruits are ridged and are composed of two parts that split open at maturity.Acorus: A plant genus of the family ACORACEAE, order Arales, subclass Arecidae most notable for Acorus calamus L. root which contains asarone and has been used in TRADITIONAL MEDICINE.Pimenta: A plant genus in the family MYRTACEAE, order Myrtales, subclass Rosidae. It is best known for allspice from the dried berry of Pimenta diocia.Piper nigrum: A plant species in the PIPERACEAE plant family. It is a common spice on foods and is used medicinally to increase gastrointestinal assimilation of other supplements and drugs. Piperine is a key component. Black pepper is picked unripe and heaped for a few days to ferment. White Pepper is the ripe fruit dehulled by maceration in water.Myrtaceae: The myrtle plant family of the order Myrtales. It includes several aromatic medicinal plants such as EUCALYPTUS.Acoraceae: A plant family of the order Arales, subclass Arecidae, class Liliopsida (monocot).Black Pepper: A common spice from fruit of PIPER NIGRUM. Black pepper is picked unripe and heaped for a few days to ferment. White Pepper is the ripe fruit dehulled by maceration in water. Piperine is a key component used medicinally to increase gastrointestinal assimilation of other supplements and drugs.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Receptor, Adenosine A1: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Receptor, Adenosine A2B: A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Adenosine Deaminase: An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Medical Missions, Official: Travel by a group of physicians for the purpose of making a special study or undertaking a special project of short-term duration.Missions and Missionaries: To be used for articles pertaining to medical activities carried out by personnel in institutions which are administered by a religious organization.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Arachidonate 5-Lipoxygenase: An enzyme that catalyzes the oxidation of arachidonic acid to yield 5-hydroperoxyarachidonate (5-HPETE) which is rapidly converted by a peroxidase to 5-hydroxy-6,8,11,14-eicosatetraenoate (5-HETE). The 5-hydroperoxides are preferentially formed in leukocytes.Arachidonic Acid: An unsaturated, essential fatty acid. It is found in animal and human fat as well as in the liver, brain, and glandular organs, and is a constituent of animal phosphatides. It is formed by the synthesis from dietary linoleic acid and is a precursor in the biosynthesis of prostaglandins, thromboxanes, and leukotrienes.Neutrophils: Granular leukocytes having a nucleus with three to five lobes connected by slender threads of chromatin, and cytoplasm containing fine inconspicuous granules and stainable by neutral dyes.Leukotrienes: A family of biologically active compounds derived from arachidonic acid by oxidative metabolism through the 5-lipoxygenase pathway. They participate in host defense reactions and pathophysiological conditions such as immediate hypersensitivity and inflammation. They have potent actions on many essential organs and systems, including the cardiovascular, pulmonary, and central nervous system as well as the gastrointestinal tract and the immune system.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Acute Lung Injury: A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).Lipopolysaccharides: Lipid-containing polysaccharides which are endotoxins and important group-specific antigens. They are often derived from the cell wall of gram-negative bacteria and induce immunoglobulin secretion. The lipopolysaccharide molecule consists of three parts: LIPID A, core polysaccharide, and O-specific chains (O ANTIGENS). When derived from Escherichia coli, lipopolysaccharides serve as polyclonal B-cell mitogens commonly used in laboratory immunology. (From Dorland, 28th ed)Lung: Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood.Inflammation: A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.Capillary Permeability: The property of blood capillary ENDOTHELIUM that allows for the selective exchange of substances between the blood and surrounding tissues and through membranous barriers such as the BLOOD-AIR BARRIER; BLOOD-AQUEOUS BARRIER; BLOOD-BRAIN BARRIER; BLOOD-NERVE BARRIER; BLOOD-RETINAL BARRIER; and BLOOD-TESTIS BARRIER. Small lipid-soluble molecules such as carbon dioxide and oxygen move freely by diffusion. Water and water-soluble molecules cannot pass through the endothelial walls and are dependent on microscopic pores. These pores show narrow areas (TIGHT JUNCTIONS) which may limit large molecule movement.Lung Injury: Damage to any compartment of the lung caused by physical, chemical, or biological agents which characteristically elicit inflammatory reaction. These inflammatory reactions can either be acute and dominated by NEUTROPHILS, or chronic and dominated by LYMPHOCYTES and MACROPHAGES.Respiratory Distress Syndrome, Adult: A syndrome characterized by progressive life-threatening RESPIRATORY INSUFFICIENCY in the absence of known LUNG DISEASES, usually following a systemic insult such as surgery or major TRAUMA.Proteinuria: The presence of proteins in the urine, an indicator of KIDNEY DISEASES.Macrophages: The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)Phenotype: The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.Abstracting and Indexing as Topic: Activities performed to identify concepts and aspects of published information and research reports.Diabetes Mellitus, Experimental: Diabetes mellitus induced experimentally by administration of various diabetogenic agents or by PANCREATECTOMY.
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)... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
1992). "Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature.". Eur. J. ... 1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics 11 (1): ... a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". Eur. J. Pharmacol. 213 ...
"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 ...
The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... and adenosine agonists can activate Trk receptor phosphorylation through a mechanism that requires the adenosine A2A receptor. ... In the US, Adenosine is marketed as Adenocard. In India Adenosine is sold as Adenoscan (Cipla) All adenosine receptor subtypes ... Adenosine is an endogenous agonist of the ghrelin/growth hormone secretagogue receptor. However, while it is able to increase ...
Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an ... Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. Thus, it may prove ... The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... A1 receptors are also present in smooth muscle throughout the vascular system. The adenosine A1 receptor has been found to be ...
These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. Signalization in ... It has been shown that collagen, exposed after the injury to the endothelial cover of the vessel, plays as an agonist in ... cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). ... TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. Both receptors mediate phospholipase C ...
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... This is a valuable guide to design potential 5HT1D receptor agonists. When sumatriptan binds there is major conformational ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... Goadsby, P.J., Serotonin 5-HT1B/1D receptor agonists in migraine - Comparative pharmacology and its therapeutic implications. ...
... 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 ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... highly potent 5-HT1D receptor agonist.". Journal of medicinal chemistry 42 (3): 526-31. PMID 9986723. doi:10.1021/jm9805945. ... 5-HT1D receptor (5-hidroksitriptaminski (serotoninski) receptor 1D, HTR1D) je 5-HT receptor. On je kodiran istoimenim genom.[1] ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • ...
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ...
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- ...
... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... 1997). „Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... Gao ZG, Jacobson KA (2007). „Emerging adenosine receptor agonists". Expert Opinion on Emerging Drugs. 12 (3): 479-92. PMID ... Adenosine Receptors: A3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...
... and reduces inflammation and innate immunity nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors ... Daly JW, Jacobson KA, Ukena D (1987). "Adenosine receptors: development of selective agonists and antagonists". Prog Clin Biol ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
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 adenilyl 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: ...
... 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 ...
The cytosolic PLA2 set (i.e. cPLA2s) of PLA2 enzymes (cPLA2; see Phospholipase A2#Cytosolic phospholipases A2) in particular ... Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... As a second drug added to corticosteroids, leukotriene inhibitors appear inferior to Beta2-adrenergic agonist drugs in the ... may serve as a mobile lid over ALOX5's substrate-binding site An Adenosine triphosphate (ATP) binding site; ATP is crucial for ...
Such drugs are called receptor agonists. An example of a receptor agonist is Valium, a benzodiazepine that mimics effects of ... Adenosine. Ado. Adenosine receptors. -. Small: Purine. Adenosine triphosphate. ATP. P2Y receptors. P2X receptors. ... "Hindbrain noradrenergic A2 neurons: diverse roles in autonomic, endocrine, cognitive, and behavioral functions". American ... NMDA receptors, kainate receptors, AMPARs. Small: Amino acids. Gamma-aminobutyric acid. GABA. GABAB receptors. GABAA receptors ...
... trienoic acid as a thromboxane A2 receptor antagonist with minimal intrinsic activity". British Journal of Haematology. 101 (1 ... Syntheic BLT2 agonists may be useful for speeding the healing of chronic ulcerative wounds, particularly in patients with, for ... to inhibit platelet aggregation responses to various agents by stimulating platelets to raise their levels of Cyclic adenosine ... BLT1 receptor) and its low affinity BLT2 receptor (Kd=23 nM); both receptors are G protein coupled receptors that, when ligand- ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as ... All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor ... Thromboxane A2 receptor. TP. TXA=PGH2,,PGD2=PGE2=PGF2α=PGI2[14]. contractile. Gq alpha subunit. stimulates PLC & IP3; raises Ca ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... leukotriene receptor activity. • cysteinyl leukotriene receptor activity. • galanin receptor activity. Cellular component. • ... "Leukotriene Receptors: CysLT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Cysteinyl leukotriene receptor 2, also termed CYSLTR2, is a receptor for cysteinyl leukotrienes (LT) (see leukotrienes# ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. DP2 has little or no such amino acid ... prostaglandin D receptor activity. • G-protein coupled receptor activity. • prostaglandin J receptor activity. • prostaglandin ... "Prostanoid Receptors: DP2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ...
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 ...
Opioid receptor agonist. *Opioid receptor antagonist. *Enkephalinase inhibitor. Other. *Adenosine reuptake inhibitor (AdoRI) ... Newton, David; Alasdair Thorpe; Chris Otter (2004). Revise A2 Chemistry. Heinemann Educational Publishers. p. 1. ISBN 0-435- ... Major receptor types studied in pharmacology include G protein coupled receptors, ligand gated ion channels and receptor ... Systems, receptors and ligands[edit]. This section needs expansion. You can help by adding to it. (July 2019) ...
ADP受體/P2Y12(英語:P2Y12)抑制劑(英語:Adenosine diphosphate receptor inhibitor)類 ... 阿司匹林低劑量服用時能阻止血小板中血栓素A2的合成,這會在受影響的血小板的生命周期(約8-9天)內抑制血小板聚集。阿司匹林的這種抗血栓作用可用於降低心臟病發生率。[122] 每天服用40 mg的阿司匹林能顯著抑制血栓
The cytosolic PLA2 set (i.e. cPLA2s) of PLA2 enzymes (cPLA2; see Phospholipase A2#Cytosolic phospholipases A2) in particular ... Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... As a second drug added to corticosteroids, leukotriene inhibitors appear inferior to Beta2-adrenergic agonist drugs in the ... An Adenosine triphosphate (ATP) binding site; ATP is crucial for ALOX5's metabolic activity ...
Adenosine. Adenosine A2 Receptor Agonists. Coronary Artery Disease. Myocardial Ischemia. Coronary Disease. Heart Diseases. ... Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Adenosine A2 Receptor Agonists. Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter ...
2-Alkynyl derivatives of Adenosine-5-N-ethyluronamide (NECA): selective A2 adenosine receptor agonists with potent inhibitory ... 2-Alkynyl derivatives of Adenosine-5-N-ethyluronamide (NECA): selective A2 adenosine receptor agonists with potent inhibitory ... The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to ... The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to ...
0 (Adenosine A2 Receptor Antagonists); 0 (Antiparkinson Agents); 0 (Dopamine Agonists); 0 (Indoles); 0 (Purines); 0 (Receptor, ... 0 (Adenosine A2 Receptor Antagonists); 0 (Antiparkinson Agents); 0 (Dopamine Agonists); 0 (Indoles); 0 (Purines); 030PYR8953 ( ... The adenosine A2A receptor antagonist, istradefylline enhances the anti-parkinsonian activity of low doses of dopamine agonists ... Antagonistas do Receptor A2 de Adenosina/uso terap utico. Antiparkinsonianos/uso terap utico. Agonistas de Dopamina/uso terap ...
1991) Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors. J Med Chem 34(12):3388-3390. ... 2007) New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains ... 2010) A novel highly selective adenosine A1 receptor agonist VCP28 reduces ischemia injury in a cardiac cell line and ischemia- ... Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Celine ...
Adenosine A2A Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2A Receptor Antagonists (0) see Adenosine A2 ... Adenosine A2B Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2B Receptor Antagonists (0) see Adenosine A2 ... Adenosine A2 Receptor Agonists (4) • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. MeSH ... Adenosine A2 Receptor Antagonists (8) • Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS. ...
Adenosine A2 Receptor Agonists. 1. 2017. 30. 0.050. Why? Purinergic P2X Receptor Antagonists. 1. 2017. 32. 0.050. Why? ... Nuclear Receptor Subfamily 1, Group F, Member 3. 1. 2012. 106. 0.130. Why? ... NK Cell Lectin-Like Receptor Subfamily B. 1. 2014. 71. 0.160. Why? ...
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. ... Subscribe to New Research on Adenosine-5-(N-ethylcarboxamide) A stable adenosine A1 and A2 receptor agonist. Experimentally, ... 05/01/1998 - "The effect of serotonergic agents was studied on the adenosine A2 receptor agonist NECA-induced catalepsy in mice ... 01/01/1993 - "The adenosine agonists 5-N-ethylcarboxamide-adenosine (NECA), N6-phenylisopropyladenosine (PIA) and N6- ...
... selective A2A agonist. Join researchers using high quality CGS 21680 from Abcam and achieve your mission, faster. ... CGS 21680C, an A2 selective adenosine receptor agonist with preferential hypotensive activity.. J Pharmacol Exp Ther 251:47-55 ... Adenosine receptors and their ligands.. Naunyn Schmiedebergs Arch Pharmacol 362:382-91 (2000). Read more (PubMed: 11111832) » ... Agonists, activators, antagonists and inhibitors. Lysates. Multiplex miRNA assays. By research area. Cancer. Cardiovascular. ...
2007) Adenosine A1 and A2 receptor agonists reduce endotoxin-induced cellular energy depletion and oedema formation in the lung ... Plasma adenosine was decreased in females (Table 3, Females). Plasma adenosine is produced from ATP and ADP released from cell ... 2011) P2 receptors and extracellular ATP: A novel homeostatic pathway in inflammation. Front Biosci (Schol Ed) 3:1443-1456. ... 2015) Bile acid-activated receptors, intestinal microbiota, and the treatment of metabolic disorders. Trends Mol Med 21(11):702 ...
... 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 ...
1994) In vivo and ex vivo effects of adenosine A1 and A2 receptor agonists on platelet aggregation in the rabbit. Eur J ... Almost all A2A adenosine receptor agonists and antagonists also have some effects on A1 or A3 receptors (Jacobson et al., 1992 ... 1992) Molecular cloning of the rat A2 adenosine receptor: selective coexpression with D2 dopamine receptors in rat striatum. ... 1996) Adenosine A2 receptor-mediated excitatory actions on the nervous system. Prog Neurobiol 48:167-189. ...
These probes bind to A.sub.2 and A.sub.3 adenosine receptors and aid in quantifying and characterizing the receptors. The ... This application discloses probes for adenosine receptors which are functionalized congeners of the following compound: ##STR1# ... which are agonists for A-1 and A-2 adenosine receptors and the sensitivity for quantitativeanalysis of xanthine amine congeners ... Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors.. UTILITY STATEMENT. The present ...
Streptozotocin-induced diabetic rats and corresponding controls were chronically treated with the adenosine A2a AR agonist ... Adenosine A2 a receptor stimulation prevents proteinuria in diabetic rats by promoting an anti-inflammatory phenotype without ... This study investigates whether chronic stimulation of the adenosine A2a receptor (A2a AR) protects kidney function in ...
1996) Adenosine A2 receptor-induced inhibition of leukotriene B4 synthesis in whole blood ex vivo. Br J Pharmacol 117:1639-1644 ... 1D). In fact, the adenosine A2areceptor agonist CGS21680 was shown to be a very potent inhibitor (IC50 of ∼1 nM) of the AA- ... Stimulation of the adenosine A2a receptor with the agonist CGS21680 also completely blocked AA-induced translocation of 5-LO ... 1C). However, when the adenosine A2a receptor agonist CGS21680 was included in these incubations containing ADA, the enhanced ...
... an adenosine A1 receptor antagonist. Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. ... a selective adenosine A1 receptor antagonist. The selective adenosine A2 and A3 receptors antagonists did not alter the ... Right atria of adult Wistar rats were used to evaluate the effects of adenosine, ATP and CPA (an adenosine A1 receptor agonist ... Adenosine and ATP exert a negative chronotropic effect in the heart. This study aims to evaluate adenosine and P2 receptors and ...
Agonist activity of 2- and 5′-substituted adenosine analogs and their N6-cycloalkyl derivatives at A1- and A2-adenosine ... Evidence for an A2-subtype adenosine receptor on pancreatic glucagon secreting cells. Br J Pharmacol 1985;86:565-569pmid: ... The Adora1 receptor is activated by adenosine. In mouse islets, adenosine is released by exocytosis (28) and can act on Adora1 ... The adenosine A1 receptor (Adora1) is a G-protein coupled receptor (GPCR) that is involved in maintaining glucose homeostasis ...
... lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. ... lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. ... The A2a specific agonist CGS21680 stimulated cAMP production but did not alter intracellular calcium concentrations in ... The A2a specific agonist CGS21680 stimulated cAMP production but did not alter intracellular calcium concentrations in ...
... increases in cAMP accumulation with potencies that were highly correlated with their potencies at A2 adenosine receptors. ... ACPD activates an mGluR subtype that potentiates responses to agonists of other receptors that are coupled to adenylate cyclase ... We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker ... Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear ...
... renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors ... Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. Am J ... Levens N, Beil M, Schulz R (1991) Intrarenal actions of the new adenosine agonist CGS 21680A, selective for the A2 receptor. J ... Kim M, Chen SW, Park SW et al (2009) Kidney-specific reconstitution of the A1 adenosine receptor in A1 adenosine receptor ...
Agonist displacement profile of [3H]CGS 21680 binding was consistent with an adenosine receptor of the A2 subtype (NECA greater ... Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum.. Fink ... Expression of this cDNA in COS cells revealed high affinity (Kd = 38.6 nM) and saturable binding of the A2 adenosine receptor- ... The co-expression of D2 dopamine and A2 adenosine receptors in a subset of striatal cells provides an anatomical basis for ...
Adenosine A1 and A2 receptor agonists reduce endotoxin-induced cellular energy depletion and oedema formation in the lung. Eur ... Comparison of the potency of adenosine as an agonist at human adenosine receptors expressed in Chinese hamster ovary cells. ... The adenosine 2A receptor agonist GW328267C improves lung function after acute lung injury in rats. Am J Physiol Lung Cell Mol ... Adenosine protected against pulmonary edema through transporter- and receptor A2-mediated endothelial barrier enhancement. Am J ...
Receptor autoradiography with [3H]CGS21680, a specific A2 agonist, and in situ hybridization with A2 cRNA probe in guinea pig ... demonstrate typical characteristics of the A2 type adenosine receptor. The messenger RNA (mRNA) of this A2 receptor is found in ... A full-length complementary DNA (cDNA) clone encoding the guinea pig brain A2 adenosine receptor has been isolated by ... Cloning and expression of the A2a adenosine receptor from guinea pig brain.. Meng F1, Xie GX, Chalmers D, Morgan C, Watson SJ ...
1992) The effects of intravenous infusions of selective adenosine A1-receptor and A2-receptor agonists on myocardial ... Lower local concentrations of adenosine have been noted to promote neutrophil recruitment (via the A1 and A3 adenosine receptor ... Adenosine bolus did not attenuate neutrophil influx into the no-reflow area, whereas adenosine infusion demonstrated a trend (p ... Whether maximal adenosine dosages were achieved in clinical studies using intravenous adenosine is also unclear. The AMISTAD ( ...
Stimulation of reactive astrogliosis in vivo by extracellular adenosine diphosphate or an adenosine A2 receptor agonist ... Adenosine and its nucleotides adenosine triphosphate (ATP) and adenosine diphosphate (ADP) stimulate the proliferation of brain ... N-cyclopropyl adenosine-5-carboxamide. Known as: 1-(6-amino-9H-purin-9-yl)-N-cyclopropyl-1-deoxy-beta-D-ribofuranuronamide, 5 ...
AntagonistsEffects of adenosineAntagonistCGS21680NECAExtracellular adenosineAbstractTriphosphateAnalogsStimulationEndogenousThromboxaneDiphosphatePotentDEAMINASERole of adenosineModulatesEffect of adenosineAdenylate cyclasePharmacologyDopamineGPCRsAffinityPurinergicPharmacologicalNucleosideLigandsPotency1993Subtypes of adenosine receptorsSubtypeDerivativesPlateletMyocardialPhysiologicalAllostericRegulation1994ModulationAnaloguesRenalHypoxiaActivateProteinBlockade of adenosineInhibitionActions of adenosineCompoundsMacrophagesResponsesMiceInhibitsAffinitiesInhibitorsPorcine
- 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)
- While several A2A receptor antagonists have progressed to clinical trials for the treatment of Parkinson's disease, A2AR blockade in the context of cancer is less characterized. (wikipedia.org)
- Indeed, when adenosine is eliminated from PMN suspensions by the addition of adenosine deaminase, or when cells are incubated with adenosine A 2a receptor antagonists, important quantities (40-80 pmol/10 6 cells) of 5-lipoxygenase products are synthesized by PMN incubated with 1 to 5 μM exogenous AA. (aspetjournals.org)
- This AA-induced Ca 2+ mobilization, as well as the corresponding 5-lipoxygenase translocation and stimulation of LT synthesis, was blocked efficiently by the LT synthesis inhibitor MK0591, the LTB 4 receptor antagonists CP105696 and LY223982, and the LTA 4 hydrolase inhibitor SC57461A. (aspetjournals.org)
- Together with complimentary pharmacological studies, these data suggest that A 2A receptors play a prominent role in the development of ischemic injury within brain and demonstrate the potential for anatomical and functional neuroprotection against stroke by A 2A receptor antagonists. (jneurosci.org)
- Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. (ovid.com)
- The selective adenosine A2 and A3 receptors antagonists did not alter the chronotropic response of adenosine. (ovid.com)
- Described are uses of A.sub.2a adenosine receptor antagonists and agonists to provide long term modulation of immune responses. (patents.com)
- A.sub.2a receptor antagonists in particular are provided to enhance immune responses by reducing T-cell mediated tolerance to antigenic stimuli and agonists are provided to enhance effectiveness of immunosuppressive agents. (patents.com)
- This application relates to uses of A.sub.2a adenosine receptor agonists and antagonists to modulate T-cell mediated tolerance to antigenic stimuli. (patents.com)
- Stably transfected cell lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. (garvan.org.au)
- Additionally, adenosine receptor antagonists blocked mGluR-mediated increases in cAMP accumulation with potencies that were highly correlated with their potencies at A2 adenosine receptors. (jneurosci.org)
- Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. (nih.gov)
- This review provides an overview of the medicinal chemistry and therapeutic potential of various agonists/partial agonists, antagonists and allosteric modulators of A1 AR, with a particular emphasis on their current status and future perspectives in clinical settings. (eurekaselect.com)
- A1 adenosine receptors, A1 AR agonists, partial agonists, antagonists and allosteric modulators, pharmacology of A1 AR, structure- activity relationships of A1 AR. (eurekaselect.com)
- A1 adenosine receptor agonists, antagonists, and allosteric modulators. (eurekaselect.com)
- They are differentiated by the rank order potency of adenosine agonists and the affinities for antagonists. (asahq.org)
- [12-In addition to the lack of selective agonists and antagonists for those receptors, the effects of adenosine agonists on non-nociceptive transmission, such as impairment of motor function and locomotor depression, limited behavioral studies characterizing the type of adenosine receptors involved in antinociception and sometimes led to conflicting interpretations and conclusions. (asahq.org)
- Evidence for the involvement of A1 (inhibitory) and A2 (stimulatory) adenosine receptors in regulating cell growth of these tumor cells was obtained through plating efficiency studies based on the relative potency of adenosine agonists and antagonists. (nus.edu.sg)
- By the chemical reaction of different xantine type molecules and [11C] methyl iodide we produced several A2A adenosine receptor specific antagonists for in vivo testing the receptor ligand interactions. (otka-palyazat.hu)
- Anti-platelet agents (such as aspirin, ADP receptor antagonists, and GPIIb/IIIa antagonists), phosphodiesterase inhibitors and anti-coagulants are major part of the current treatment towards treating ischemic diseases. (eurekaselect.com)
- The distinction between receptor-binding sites for agonists and antagonists underpins the pharmacological differences between these two classes of ligands. (pianolarge.cf)
- Antagonists of ERK1/2 and PI3K were perfused in hearts treated with the KOP agonist U50488H (U50). (bvsalud.org)
- To investigate the mechanisms involved in cannabidiol (CBD)-induced neuroprotection in hypoxic-ischemic (HI) immature brain, forebrain slices from newborn mice underwent oxygen and glucose deprivation in the presence of vehicle, or CBD alone or with selective antagonists of cannabinoid CB(1) and CB(2), and adenosine A(1) and A(2) receptors. (unboundmedicine.com)
- Right atria of adult Wistar rats were used to evaluate the effects of adenosine, ATP and CPA (an adenosine A1 receptor agonist), in the presence and absence of DPCPX, an adenosine A1 receptor antagonist. (ovid.com)
- The effects of adenosine, CPA and ATP were inhibited by DPCPX, a selective adenosine A1 receptor antagonist. (ovid.com)
- Effects of adenosine on tubular transport are most pronounced in the proximal tubule where the nucleoside stimulates NaCl reabsorption in the subnormal concentration range while inhibiting transport at elevated levels. (springer.com)
- Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. (springer.com)
- Beach RE, Good DW (1992) Effects of adenosine on ion transport in rat medullary thick ascending limb. (springer.com)
- Several studies have also suggested that the beneficial effects of adenosine occur through the effects of the A2AR and A2BR ( 7 , 22 , 27 , 43 ). (physiology.org)
- Background Despite the clear cardioprotective effects of adenosine, when administered prior to ischemia, studies on cardioprotection by adenosine when administered at reperfusion have yielded contradictory results in both pre-clinical and clinical settings. (onlinejacc.org)
- The effects of adenosine on water and sodium excretion. (aspetjournals.org)
- The effects of adenosine on glomerular filtration rate and renal blood flow are well documented, but its effects on water and sodium excretion are less well established. (aspetjournals.org)
- The diuretic and natriuretic effects of adenosine during intrarenal infusion were of a similar order of magnitude in animals maintained for 3 weeks on no sodium, normal sodium or high sodium diet, and did not correlate with plasma renin activity. (aspetjournals.org)
- These findings suggest that, in the rat, the diuretic and natriuretic effects of adenosine are 1) fully expressed only during intrarenal administration, 2) absent during intra-aortic administration, 3) not related to prior sodium intake or sodium balance, 4) mediated by the adenosine A1 receptor and 5) dissociated from its effects on glomerular filtration and renal plasma flow. (aspetjournals.org)
- Thus, we propose a novel mechanism whereby IFN-γ contributes to host defense by desensitizing macrophages to the immunoregulatory effects of adenosine. (jimmunol.org)
- Direct effects of adenosine A2 receptor activation on renal function were examined in dogs. (umin.ac.jp)
- Regadenoson is an selective low-affinity (Ki= 1.3 µM) A2A receptor agonist that mimics the effects of adenosine in causing coronary vasodilatation and increasing myocardial blood flow. (drugbank.ca)
- 1 This study aimed to determine the role of the vascular endothelium on recovery of contractile function following global low-flow ischaemia of guinea-pig isolated working hearts and the effects of adenosine analogues on this recovery. (cf.ac.uk)
- 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)
- 1. A method of enhancing an immune response in a host, comprising administering to the host an A.sub.2a receptor antagonist in combination or alternation with a checkpoint inhibitor. (patents.com)
- Aki Y, Tomohiro A, Nishiyama A et al (1997) Effects of KW-3902, a selective and potent adenosine A1 receptor antagonist, on renal hemodynamics and urine formation in anesthetized dogs. (springer.com)
- Where indicated, DA levels were restored by bath application of exogenous DA (20 μM), or action of endogenous DA was blocked by application of a specific D1 receptor antagonist (10 μM SCH23390). (frontiersin.org)
- Simultaneous infusion of 10(-7) M 9-cyclopentyl-1,3-dipropylxanthine, a selective adenosine A1 receptor antagonist, markedly inhibited the diuretic and natriuretic effects of intrarenal adenosine. (aspetjournals.org)
- Neither the change in [Ca2+]i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2-aminoethyl)carbamoylmethoxy]-phenyl}-1,3-dipropylxanthine (XAC). (rti.org)
- NECA was chosen for the study because caffeine is a nonselective adenosine receptor antagonist, and it is not known which of the four subtypes of adenosine receptors may be involved in an effect of caffeine on fatigue. (innovations-report.com)
- Theophylline** Theophylline is an adenosine receptor antagonist. (rutgers.edu)
- The dose-related increase in lobar arterial pressure in response to adenosine was blocked by an adenosine (P1) receptor antagonist, BWA1433U, the cyclooxygenase inhibitor, meclofenamate, and the thromboxane A2 receptor antagonist, SQ29548. (aspetjournals.org)
- A vasopressin antagonist that binds to the V2-receptor of LLC-PK, renal epithelial cells is highly laterally mobile but does not effect ligand-induced receptor immobilization. (springer.com)
- SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. (elsevier.com)
- Contractions to ATP and αβ-meATP were blocked by NF449, a selective P2X1 receptor antagonist. (nottingham.ac.uk)
- MRS2578, a selective P2Y6 receptor antagonist, had no effect on contractions to UTP. (nottingham.ac.uk)
- ADP induced endothelium-dependent vasorelaxation which was inhibited by MRS2179, a selective P2Y1 receptor antagonist, or SCH58261, a selective adenosine A2A receptor antagonist. (nottingham.ac.uk)
- Tbe 2',3'-dideoxy analogue of the potent A\(_1\) receptor agonist, N\(^6\)-cyclohexyladenosine (CHA), was synthesized as a potential antagonist for the A\(_1\) adenosine receptor. (uni-wuerzburg.de)
- Competition of 2-alkynyladenosines 2a-d for the antagonist radioligand [\(^3\)H]DPCPX and for the agonist [\(^3\)H]CCPA gave K\(_i\) values in the nanomolar range, and the compounds showed moderate A\(_2\) selectivity. (uni-wuerzburg.de)
- Metod: Laser-Dِoppler flowmetry technique was used to study pial vessels blood flow responses to adenosine receptors agonists and antagonist. (phypha.ir)
- Adenosine (general agonist), NECA (A2Aand A2B receptor agonist) and CGS-21380(A2Aselective agonist), were used in absence and presence of A2A receptors- selective antagonist, ZM-243185, in naive and morphine-dependent rats. (phypha.ir)
- The selective A 2a receptor agonist CGS21680 was a very potent inhibitor of the AA-induced leukotriene (LT) synthesis, showing an IC 50 of ∼1 nM. (aspetjournals.org)
- ASP5854 ameliorated A(2A) agonist 2-[p-(2-carboxyethyl) phenethylamino]-5'-N-ethylcarboxamidoadenosine (CGS21680)- and haloperidol-induced catalepsy in mice, with the minimum effective doses of 0.32 and 0.1 mg/kg, respectively, and it also improved haloperidol-induced catalepsy in rats at doses higher than 0.1 mg/kg. (curehunter.com)
- Streptozotocin-induced diabetic rats and corresponding controls were chronically treated with the adenosine A2a AR agonist CGS21680 throughout the four-week diabetes duration. (sigmaaldrich.com)
- The A2a specific agonist CGS21680 stimulated cAMP production but did not alter intracellular calcium concentrations in transfected 293 cells. (garvan.org.au)
- Receptor autoradiography with [3H]CGS21680, a specific A2 agonist, and in situ hybridization with A2 cRNA probe in guinea pig brain indicate that the receptor is expressed exclusively in the caudate nucleus. (nih.gov)
- We show herein that in an HD transgenic mouse model (R6/2), daily administration of CGS21680 (CGS), an A 2A adenosine receptor (A 2A -R)-selective agonist, delayed the progressive deterioration of motor performance and prevented a reduction in brain weight. (elsevier.com)
- 4 The adenosine analogues, N6-cyclopentyladenosine (CPA, A1 selective), 5'-N-ethylcarboxamidoadenosine (NECA, two-fold A2 selective over A1) and 2-p-((carboxyethyl)-phenethylamino)-5'carboxamidoadenosine (CGS21680, A2A selective) were infused (3 × 10−7 M) from 10 min into the 30-min low-flow ischaemia of denuded hearts and during reperfusion. (cf.ac.uk)
- A series of new 2-alkynyl and 2-cycloalkynyl derivatives of adenosine-5'-N-ethyluronamid(NECA) and of N-ethyl-l'-deoxy-l'-(6-amino-2-hexynyl-9H-purin-9-yl)-b-D-ribofuranuronamid(1e, HENECA), bearing hydroxy, amino, chloro, and cyano groups in the side chain, were synthesized. (unicam.it)
- The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to compounds endowed with sub-nanomolar affinity in binding studies. (unicam.it)
- To test this hypothesis, we examined the effects of pre- and posttreatment of adenosine and 5′- N -ethylcarboxamidoadenosine (NECA), a nonselective stable AR agonist, on LPS-induced lung injury. (physiology.org)
- Mice were given vehicle or LPS intratracheally followed by adenosine, NECA, or vehicle instilled via the internal jugular vein. (physiology.org)
- Importantly, posttreatment with adenosine or NECA recovers lung vascular barrier and reduces inflammation induced by LPS challenge. (physiology.org)
- Agonist displacement profile of [3H]CGS 21680 binding was consistent with an adenosine receptor of the A2 subtype (NECA greater than (R)-PIA greater than CPA greater than (S)-PIA). (nih.gov)
- The researchers' hypothesis is the foundation of a new study to determine the effects of intracerebroventricular injection of caffeine and the adenosine A1 and A2 receptor agonist 5'-N-ethylcarboxamidoadenosine (NECA) on treadmill run time to fatigue in rats. (innovations-report.com)
- The drugs chosen were, R-phenylisopropyl-adenosine (R-PIA) with high affinity for the A1 receptor, N-ethylcarboxamide-adenosine (NECA) with almost equal affinity for the A1 and A2 receptor and 2-(2-aminoethylamino)-carbonylethylphenylethylamino-adenosin e (APEC) with high affinity for the A2 receptor. (nih.gov)
- Az A1, A2 és A3 adenozin-receptor expresszió in vivo tanulmányozásához pedig az 18F izotóppal jelölt 5'-N-etil-karboxamidadenonozint (NECA) állítottuk elő. (otka-palyazat.hu)
- To study the A1, A2 and A3 adenosine receptor expression 18F isotope labeled 5'-N-etil-carboxamidadenosine (NECA) was produced. (otka-palyazat.hu)
- Binding of [\(^3\)H]NECA to A\(_2\) receptors of rat striatal membranes was inhibited by compounds 2a-d with K\(_i\) values ranging from 2.8 to 16.4 nM. (uni-wuerzburg.de)
- Results: Adenosine, NECA and CGS-21680 increased pial vessels blood flow in naive and dependent rats dose dependently. (phypha.ir)
- Responses of pial vessels to adenosine (10-4, 10-5, 10-6 M) and NECA (10-4, 10-5, 10-6 M) were increased significantly in morphine- dependent rats in comparison to naive rats. (phypha.ir)
- The A2A adenosine receptor-selective agonist but not the non-selective A2 receptor agonist, NECA, attenuated ischaemia- and reperfusion-induced stunning. (cf.ac.uk)
- EGF also potentiates the forskolin-induced stimulation of C-AMP but has no effect on the elevation of C-AMP caused by NECA (5′-[N-ethyl]-carboxamido adenosine), an adenosine A2-receptor agonist. (ulster.ac.uk)
- 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)
- The mechanism of AA-induced stimulation of LT synthesis observed in the absence of extracellular adenosine was investigated. (aspetjournals.org)
- Extracellular adenosine critically modulates ischemic brain injury, at least in part through activation of the A 1 adenosine receptor. (jneurosci.org)
- We have recently shown that extracellular adenosine enhances human pulmonary (EC) barrier via activation of adenosine receptors (ARs) in cell cultures. (physiology.org)
- In this study, we demonstrate that, following TLR stimulation, macrophages upregulate the adenosine 2b receptor (A2bR) to enhance their sensitivity to immunosuppressive extracellular adenosine. (jimmunol.org)
- In this study, we investigated the effect of IFN-γ on TLR-activated macrophages, and we reveal that IFN-γ sustains inflammatory macrophage activation by attenuating their sensitivity to extracellular adenosine. (jimmunol.org)
- Extracellular adenosine has been widely implicated in adaptive responses to hypoxia. (rupress.org)
- The generation of extracellular adenosine involves phosphohydrolysis of adenine nucleotide intermediates, and is regulated by the terminal enzymatic step catalyzed by ecto-5′-nucleotidase (CD73). (rupress.org)
- Guided by previous work indicating that hypoxia-induced vascular leakage is, at least in part, controlled by adenosine, we generated mice with a targeted disruption of the third coding exon of Cd73 to test the hypothesis that CD73-generated extracellular adenosine functions in an innate protective pathway for hypoxia-induced vascular leakage. (rupress.org)
- abstract = "Adenosine released into the extracellular space by immunologic and nonimmunologic stimuli has been shown to regulate various immune functions. (utmb.edu)
- In addition, platelets with the Q43P β1-tubulin variant had reduced adenosine triphosphate (ATP) secretion, thrombin receptor activating peptide (TRAP)-induced aggregation and collagen adhesion. (bloodjournal.org)
- The balance of these two molecules can be generated by extracellular nucleotides, such as adenosine 5'-triphosphate (ATP) and adenosine (Ado), which activate the purinergic receptors system. (biomedcentral.com)
- Activated platelets also release various aggregation mediators including ADP, adenosine triphosphate (ATP), thromboxane A2 (TXA2), serotonin, and various proteins [ 4 ]. (hindawi.com)
- adenosine-5′-diphosphate (ADP), uridine-5′-triphosphate (UTP) and MRS2768, a selective P2Y2 agonist, were applied cumulatively, while adenosine-5′-triphosphate (ATP) and αβ-methylene-ATP (αβ-meATP) response curves were generated from single concentrations per tissue segment. (nottingham.ac.uk)
- Several lines of evidence have previously suggested that dopamine-induced changes in motor behavior can be modulated by adenosine analogs acting at the A2 subtype of adenosine receptor in the forebrain. (nih.gov)
- Several behavioral studies have shown that intrathecal administration of adenosine analogs produces antinociception. (asahq.org)
- Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
- The stimulation of human leukocytes by various agents such as calcium ionophores, soluble agonists, or phagocytic stimuli results in the biosynthesis of the bioactive arachidonic acid (AA)-derived leukotrienes (LTs). (aspetjournals.org)
- Adenosine A2 a receptor stimulation prevents proteinuria in diabetic rats by promoting an anti-inflammatory phenotype without affecting oxidative stress. (sigmaaldrich.com)
- This study investigates whether chronic stimulation of the adenosine A2a receptor (A2a AR) protects kidney function in insulinopenic diabetic rats. (sigmaaldrich.com)
- Activation of nucleotide receptors with extracellular ATP and nucleotide analogues increased intracellular calcium concentration ([Ca2+]i) primarily by release of intracellular calcium stores, with relative potency of agonists similar to that seen for stimulation of Na-K-Cl cotransport. (rti.org)
- To address possible mechanisms for stimulation of Na-K-Cl cotransport by the nucleotide receptor, I-125 efflux and patch-clamp studies were used to measure chloride secretion. (rti.org)
- Now, a team of researchers from the University of South Carolina has hypothesized that the blockade of adenosine receptors by caffeine may be the most likely mechanism of CNS stimulation and delayed fatigue. (innovations-report.com)
- After TLR stimulation, macrophages alter their metabolism and release low levels of ATP, which is rapidly converted into immunosuppressive adenosine via CD39-mediated hydrolysis. (jimmunol.org)
- Theophylline-induced respiratory recovery following cervical spinal cord hemisection is augmented by serotonin 2 receptor stimulation. (rutgers.edu)
- The present study was designed to specifically determine if concurrent stimulation of 5-HT2 receptors may enhance motor recovery induced by theophylline alone. (rutgers.edu)
- CGS 21680C induced renin release and tachycardia that were blocked by propranolol, indicating these effects of A2 receptor stimulation appeared to be indirect. (umin.ac.jp)
- The results showed that neither the stimulation nor the blockade of adenosine A2A receptors modified the progressive loss of motor skills or survival of mSOD1G93A mice. (elsevier.com)
- These results demonstrate that adenosine receptor stimulation differentially modulates the LPS-induced production of IL-10, TNF-α, and NO in vitro and in vivo. (utmb.edu)
- Adenosine antagonises the effect of ATP by stimulation of adenosine receptors suppressing the pro-inflammatory response (14-17). (deepdyve.com)
- Dibutyryl C-AMP has a negative effect on RPE cell proliferation while isoproterenol is ineffective.The data presented here suggest that after stimulation of EGF receptors, tyrosine-kinase-activated products can influence secondary messenger products produced from activation of β2-type (linked with C-AMP formation) and muscarinic (linked with InsPs production) receptors in RPE cells. (ulster.ac.uk)
- Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of these hybrid receptors is still only starting to be unravelled. (wikipedia.org)
- We report here that the apparent inability of isolated human polymorphonuclear leukocytes (PMNs) to efficiently transform arachidonic acid (AA) is the consequence of A 2a receptor engagement by endogenous adenosine accumulating in incubation media. (aspetjournals.org)
- Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
- As a breakdown product of ATP, adenosine is an endogenous purine nucleoside that modulates many physiological processes in all cells of the body. (physiology.org)
- The A2AR is expressed in lung tissues, where it is activated by endogenous/exogenous adenosine or A2AR agonists and where it exerts anti-inflammatory effects ( 24 , 39 , 45 ). (physiology.org)
- Furthermore, previous studies suggest that glutamate increases cAMP accumulation by a mechanism that is dependent upon the presence of endogenous adenosine. (jneurosci.org)
- Therefore, we tested the hypothesis that 1S,3R- ACPD-stimulated increases in cAMP accumulation in rat hippocampal slices are dependent upon the presence of endogenous adenosine and are mediated by an mGluR that potentiates cAMP responses to other agonists. (jneurosci.org)
- Furthermore, we performed a series of studies that suggest that 1S,3R- ACPD activates an mGluR subtype that potentiates responses to agonists of other receptors that are coupled to adenylate cyclase and that 1S,3R- ACPD-stimulated increases in cAMP accumulation in hippocampal slices are mediated by potentiation of the cAMP response to low levels of endogenous adenosine that are continuously present extracellularly. (jneurosci.org)
- Regulation of plasma membrane ion transport by endogenous purinergic receptors was assessed in a distal renal (A6) cell line. (rti.org)
- Previous studies indicated that extracellular nucleotide metabolites, predominantly adenosine, may trigger an endogenous protective mechanism during hypoxia and ischemia ( 12 - 15 ). (rupress.org)
- The nucleoside adenosine, a potent endogenous anti-inflammatory agent, is deeply involved in inflammatory diseases and, by interaction with the adenosine A 2 receptor (A 2A R) it immediately promotes a mechanism of defence against the inflammatory damage. (scirp.org)
- This receptor can bind to several different endogenous ligands, such as b-endorphin, enkephalin , and exogenous opioids. (thefreedictionary.com)
- Various platelet agonists like adenosine diphosphate (ADP), thrombin and thromboxane A2 (TXA2) activate platelets by acting via their respective surface receptors, which couple to one or more distinct G-proteins belonging to either the Gi, Gq, G12/13 or Gs families. (eurekaselect.com)
- A) Activating thromboxane A2. (knoowy.co.uk)
- Platelet G-proteinCcoupled receptors impact platelet function by mediating the reaction to various agonists, including ADP, thromboxane A2, and thrombin. (perlierusa.com)
- Platelet activation results in release of supplementary agonists, thromboxane A2 and adenosine diphosphate (ADP). (perlierusa.com)
- Thrombin changes fibrinogen to fibrin to help expand stabilize the plateletCfibrin clot.1 A significant section of controversy is available at the moment about the comparative contribution of every agonist-induced platelet activation pathway (ADP, thromboxane A2, and thrombin) towards the genesis of the in vivo steady thrombus. (perlierusa.com)
- ADP through P2Y1 and P2Y12, thrombin through PAR-1 and PAR-4, thromboxane A2 through TP, epinephrine with the -adrenergic receptor, and prostaglandin (PG)I2 with the IP.4,5 These signaling pathways are highly conserved as are regulatory 9-Dihydro-13-acetylbaccatin III mechanisms. (perlierusa.com)
- B) Blocking adenosine diphosphate receptor agonists. (knoowy.co.uk)
- Separate groups of reproductively senescent female Fischer 344 rats (F344) were exposed via vapor inhalation to D4 (700ppm, 9.3mg/L) or D5 (160ppm, 2.1mg/L) or to a diet containing 0.0045, 0.045, or 4.5ppm pergolide mesylate (PM), a potent dopamine agonist used here as a reference substance, from 11 through 24 months of age. (bireme.br)
- Potent, selective A 2A agonist (K i = 23 nM). (abcam.com)
- Intrarenal infusion of N6-cyclohexyladenosine, an adenosine A1 receptor agonist, but not of N' ethylcarboxamidoadenosine, a potent A2 receptor agonist, significantly increased water and sodium excretion. (aspetjournals.org)
- Introduction:Adenosine as a potent vasodilator has physiological role in regulation of regional cerebral blood flow (rCBF). (phypha.ir)
- Drugs that inhibit ADENOSINE DEAMINASE activity. (nih.gov)
- In adenosine deaminase-treated PMN, exogenous AA induced Ca 2+ mobilization and the translocation of 5-lipoxygenase to nuclear structures. (aspetjournals.org)
- We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker dipyridamole enhanced this response. (jneurosci.org)
- To avoid these undesirable effects, indirect approaches, such as allosteric adenosine receptor modulation or inhibition of adenosine kinase 9,10 or adenosine deaminase, 11 have been examined and show antinociceptive effects in neuropathic rats. (asahq.org)
- The actions of the A2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity. (wikipedia.org)
- The role of adenosine A2 receptors in regulation of pial vessels blood flow in anesthetized morphine dependent rats. (phypha.ir)
- Hoseini M, Hajizadeh S, Fathollahi Y, Golmohammadi M, Erfani B, Heidarian Pour A. The role of adenosine A2 receptors in regulation of pial vessels blood flow in anesthetized morphine dependent rats. (phypha.ir)
- The adenosine A 2A receptor (A 2A R) modulates normal vascularization and pathologic angiogenesis in many tissues and may contribute to the pathogenesis of retinopathy of prematurity (ROP) characterized by abnormal retinal vascularization in surviving premature infants. (arvojournals.org)
- A particular focus was placed on TrkB agonist 7, 8-dihydroxyflavone, which modulates multiple functions and has demonstrated remarkable therapeutic efficacy in a variety of central nervous system disease models. (elsevier.com)
- A1 and A2 adenosine receptor activation inversely modulates potassium currents and membrane potential in DDT1-MF2 smooth muscle cells. (otka-palyazat.hu)
- Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
- The effect of adenosine and its agonists on nitric oxide synthase (NOS) activity and the production of nitrite induced by lipopolysaccharide (LPS) in RAW 264.7 cells were investigated. (nus.edu.sg)
- A number of G-protein-linked receptors that are not directly coupled to adenylate cyclase increase cAMP accumulation by potentiating cAMP responses to other agonists. (jneurosci.org)
- ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells. (jci.org)
- The compound ATP gamma S inhibits agonist-stimulated adenylate cyclase activity in solubilized and in isobutylmethylxanthine (IBMX) and quinacrine pretreated membranes, suggesting that ATP gamma S inhibition occurs independent of AVP and A1 adenosine receptors and of phospholipase A2 activity. (jci.org)
- Neuroblastoma x glioma hybrid NG108-15 cells endogenously express at least three receptors which activate adenylate cyclase via the intermediacy of the stimulatory G-protein, Gs. (biochemj.org)
- The adenylate cyclase-coupled vasopressin V2-receptor is highly laterally mobile in membranes of LLC-PK, renal epithelial cells at physiological temperature. (springer.com)
- Jans DA, Peters R, Fahrenholz F. Lateral mobility of the phospholipase-C-activating vasopressin V,-type receptor in A7r5 smooth muscle cells: a comparison with the adenylate cyclase-coupled V2-receptor. (springer.com)
- Tolkovsky AM, Levitzki A. Mode of coupling between the (3-adrenergic receptor and adenylate cyclase in turkey erythrocytes. (springer.com)
- Tolkovsky AM, Levitzki A. Coupling of a single adenylate cyclase to two receptors: adenosine and catecholamine. (springer.com)
- Tolkovsky A, Braun S, Levitzki A. Kinetics of interaction between 3-receptors, GTP-proteins and the catalytic subunit of turkey erythrocyte adenylate cyclase. (springer.com)
- Hanski E, Rimon G, Levitzki A. Adenylate cyclase activation by the 3-adrenergic receptor as a diffusion controlled process. (springer.com)
- In sturlies on adenylate cyclase 2',3'-dideoxy-N\(^6\)-cyclohexyladenosine (ddCHA) did not show agonist properties at A\(_1\) or at A\(_2\) receptors. (uni-wuerzburg.de)
- A 30- to 45-fold selectivity for platelet A\(_2\) receptors compared to A\(_1\) receptors was found for compounds 8a-c in adenylate cyclase studies. (uni-wuerzburg.de)
- Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pharmacology of adenosine receptors: the state of the art. (eurekaselect.com)
- The effects profile and induction of uterine tumors share some similarity with that seen with chronic exposure to dopamine agonists. (bireme.br)
- The current study investigated the potential for D4 and D5 to elicit dopamine agonist-like effects on estrous cyclicity. (bireme.br)
- 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, drug addiction and Parkinson's disease. (wikipedia.org)
- As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. (wikipedia.org)
- Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. (nih.gov)
- In situ hybridization demonstrated that rat A2 adenosine receptor mRNA was co-expressed in the same striatal neurons as D2 dopamine receptor mRNA, and never co-expressed with striatal D1 dopamine receptor mRNA. (nih.gov)
- The co-expression of D2 dopamine and A2 adenosine receptors in a subset of striatal cells provides an anatomical basis for dopaminergic-adenosinergic interactions on motor behavior. (nih.gov)
- Adenosine also inhibits the release of most brain excitatory neurotransmitters, particularly dopamine (DA), and may reduce DA synthesis. (innovations-report.com)
- In 1991, the phenomenon of receptor crosstalk was observed between adenosine A2A (A2A) and dopamine D2 receptor (DRD2) thus suggesting the formation of heteromers. (wikipedia.org)
- While initially thought to be a receptor heterodimer, a review from 2015 determined that the A2A-DRD2 heteromer is a heterotetramer composed of A2A and DRD2 homodimers (i.e., two adenosine A2A receptors and two dopamine D2 receptors). (wikipedia.org)
- Salbutamol, isoproterenol and dopamine stimulate C-AMP production in human retinal pigment epithelium (RPE) cells by activation of β2-type receptors. (ulster.ac.uk)
- The concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug discovery, particularly in the field of G protein-coupled receptors (GPCRs). (pnas.org)
- G protein-coupled receptors (GPCRs) are the largest family of cell surface proteins and tractable drug targets ( 1 , 2 ). (pnas.org)
- Adenosine is a purine nucleoside, responsible for the regulation of a wide range of physiological and pathophysiological conditions by binding with four G-protein-coupled receptors (GPCRs), namely A1, A2A, A2B and A3 adenosine receptors (ARs). (eurekaselect.com)
- A GPCR oligomer is a protein complex that consists of a small number (ὀλίγοι oligoi "a few", μέρος méros "part, piece, component") of G protein-coupled receptors (GPCRs). (wikipedia.org)
- Receptor homodimers - which consist of two identical GPCRs - are the simplest homomeric GPCR oligomers. (wikipedia.org)
- Receptor heterodimers - which consist of two different GPCRs - are the simplest heteromeric GPCR oligomers. (wikipedia.org)
- The first direct evidence that GPCRs functioned as oligomers in vivo came from Overton and Blumer in 2000 by fluorescence resonance energy transfer (FRET) analysis of the α-factor receptor in the yeast Saccharomyces cerevisiae. (wikipedia.org)
- These released mediators stimulate G-protein coupled receptors (GPCRs) that are necessary for phospholipase C (PLC), protein kinase C (PKC), phosphoinositide-3 kinase (PI3K) [ 4 ], and MAP kinases activations [ 5 ]. (hindawi.com)
- An approach to use multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors (GPCRs) was recently introduced. (biomedcentral.com)
- Human genome evaluation has confirmed 1000 exclusive G-proteinCcoupled receptors (GPCRs) connected with several physiological features.2 GPCRs control lots of the cellular occasions in human beings through sign transduction activated by various 9-Dihydro-13-acetylbaccatin III agonists. (perlierusa.com)
- However, these analogues also possess good A1 receptor affinity resulting in low A2 selectivity. (unicam.it)
- The presence of an a-quaternary carbon such as the 3-hydroxy-3,5-dimethyl-1-hexynyl (12) and the 3-hydroxy-3-phenyl-1-butynyl(1 5) derivatives markedly reduced the antiaggregatory potency without affecting the A2 affinity. (unicam.it)
- The brain-derived neurotrophic factor (BDNF) and its high affinity receptor tropomyosin-receptor-kinase B (TrkB) play a critical role in neuronal differentiation and survival, synapse plasticity, and memory. (elsevier.com)
- Furthermore, it has negligible affinity to A2B and A3 adenosine receptors. (drugbank.ca)
- The tritiated analogue of 2-chloro-N6-cyclopentyladenosine (CCPA), an adenosine derivative with subnanomolar affinity and a 10000-fold selectivity for A1 adenosine receptors, has been examined as a new agonist radioligand. (uni-wuerzburg.de)
- Adenosine-dependent regulation of renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors (A 1 AR, A 2A AR, A 2B AR, A 3 AR). (springer.com)
- Adenoscan® (adenosine) is an approved pharmacological stress agent indicated as an adjunct to thallium-201 myocardial perfusion scintigraphy in patients unable to exercise adequately. (clinicaltrials.gov)
- To overcome these pharmacological limitations, we explored the consequences of deleting the A 2A adenosine receptor on brain damage after transient focal ischemia. (jneurosci.org)
- The pharmacological profile and anatomical distribution of this receptor indicate that it is of the A2a subtype. (nih.gov)
- This work represents the first cloning of an A2a receptor in a rodent species, offers a complete pharmacological characterization of the receptor and provides an anatomical comparison between binding profile and gene expression of the receptor. (nih.gov)
- Biochemical and pharmacological role of A1 adenosine receptors and their modulation as novel therapeutic strategy In: ed Protein Reviews. (eurekaselect.com)
- Because adenosine production increases in hypoxia, the issue of a role of the nucleoside in the renal injury following ischemia reperfusion has been studied extensively. (springer.com)
- We validate that the interaction of VCP746 with the A 1 AR is consistent with a bitopic mode of receptor engagement (i.e., concomitant association with orthosteric and allosteric sites) and that the compound displays biased agonism relative to prototypical A 1 AR ligands. (pnas.org)
- Thus, this study provides proof of concept that bitopic ligands can be designed as biased agonists to promote on-target efficacy without on-target side effects. (pnas.org)
- Adenosine receptors and their ligands. (abcam.com)
- The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. (elsevier.com)
- The aim of this work was the development and biological test of adenosine receptor ligands which are suitable for in vivo PET examinations. (otka-palyazat.hu)
- The biological distribution of the ligands as well as their binding kinetics to the receptors was tested in vivo by dynamic PET scans and ex vivo or in vitro experiments. (otka-palyazat.hu)
- Guanylyl cyclase C (GC-C), the receptor for diarrheagenic enterotoxins and the paracrine ligands guanylin and uroguanylin, regulates intestinal secretion. (naver.com)
- The compounds were studied in binding and functional assays to assess their potency for the A2 compared to A1 adenosine receptor. (unicam.it)
- The rank order potency of inhibition by ATP analogues suggests that a P2y type of ATP receptor is involved in this inhibition. (jci.org)
- The order of potency of adenosine receptor agonists to produce VC in the PV bed was the selective adenosine A1 receptor agonist R-phenylisopropyladenosine greater than the mixed A1, A2 receptor agonist, adenosine greater than the selective adenosine A2 receptor agonist, 2-phenylaminoadenosine. (aspetjournals.org)
- Maggio and co-workers showed in 1993 the ability of the muscarinic M3 receptor and α2C-adrenoceptor to heterodimerize. (wikipedia.org)
- Adenosine A1 receptor (ADORA1, also known as A1AR) is one of four subtypes of adenosine receptors that belong to a superfamily of protein G-coupled receptors. (ptglab.com)
- We recently reported the cloning of a cDNA (designated RFL9) that encodes a novel A2-adenosine receptor subtype. (pianolarge.cf)
- Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors. (patentgenius.com)
- In order to improve this selectivity, the correaponding 2-alkynyl derivatives of adenosine-5'-N-ethyluronamide 8a-d were synthesized and tested. (uni-wuerzburg.de)
- The aim of this paper was to examine the link between antiplatelet and anti-inflammatory roles of quercetin in agonist-induced platelet activation. (hindawi.com)
- In the search for more selective A2-receptor agonists and on the basis that appropriate substitution at C2 is known to impart selectivity for A\(_2\) receptors, 2-alkynyladenosines 2a-d were resynthesized and evaluated in radioligand binding, adenylate cycla.se, and platelet aggregation studies. (uni-wuerzburg.de)
- 2-Alkynyladenosines also exhibited high-affmity binding at solubilized A\(_2\) receptors from human platelet membranes. (uni-wuerzburg.de)
- Keywords: bloodstream platelet, heart disease, GTP-binding protein, purinerginc 2Y12 receptor agoists, receptors, thrombin Quick platelet activation and aggregation are necessary for the introduction of arterial thrombotic occasions. (perlierusa.com)
- These agonists amplify the reaction to damage and produce suffered platelet aggregation in the current presence of high arterial shear 9-Dihydro-13-acetylbaccatin III prices. (perlierusa.com)
- Concurrently, subpicomolar concentrations of thrombin are generated after publicity of bloodstream to tissues factorCbearing cells within the subendothelial area and activate platelets by cleaving platelet protease turned on receptors (PARs). (perlierusa.com)
- The investigational drug, regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist, the receptor responsible for coronary vasodilation, and is being studied for potential use as a pharmacologic stress agent in myocardial perfusion imaging (MPI) studies. (clinicaltrials.gov)
- As with the A1, the A2A receptors are believed to play a role in regulating myocardial oxygen consumption and coronary blood flow. (wikipedia.org)
- The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. (wikipedia.org)
- Objectives In the absence of effective clinical pharmacotherapy for prevention of reperfusion-mediated injury, this study re-evaluated the effects of intracoronary adenosine on infarct size and no-reflow in a porcine model of acute myocardial infarction using clinical bolus and experimental high-dose infusion regimens. (onlinejacc.org)
- Conclusions During reperfusion, intracoronary adenosine can limit infarct size and no-reflow in a porcine model of acute myocardial infarction. (onlinejacc.org)
- Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. (drugbank.ca)
- Cardioprotective signaling cascade of A2 adenosine receptor agonist 5'-N-ethylcarboxaminidoadenosine against myocardial reperfusion injury. (ekja.org)
- Preconditioning of cardiomyocytes with either A 1 or A 3 AR agonists protects against myocardial ischemia. (biomedcentral.com)
- Cerebral morphology, as well as vascular and physiological measures (before, during, and after ischemia) did not differ between A 2A receptor knock-out and wild-type littermates. (jneurosci.org)
- However, A2b and A3 receptors are relatively less active than A1 and A2a receptors under normal physiological conditions. (innovations-report.com)
- 9-13 Movement of the hormone-occupied receptor is not required subsequent to dimerization, and consistent with this, activated receptors appear to be aggregated and essentially immobile at physiological temperature (see section E, chapter 4). (springer.com)
- Adenosine-a physiological or pathophysiological agent? (eurekaselect.com)
- Adenosine mediates many physiological functions via activation of extracellular receptors. (nus.edu.sg)
- Schlessinger J. Signal transduction by allosteric receptor oligomerization. (springer.com)
- Schlessinger J. The epidermal growth factor receptor as a multifunctional allosteric protein. (springer.com)
- Among these indirect approaches, allosteric adenosine receptor modulation represents a novel drug development direction to potentiate A1 receptor function and agonist binding via a conformation change. (asahq.org)
- This study demonstrates that nucleotide receptors in this model of renal epithelium initiate distinct regulation of Na-K-Cl cotransport. (rti.org)
- In beta N22 cells the IP prostanoid receptor was expressed at similar levels to those in wild-type NG108-15 cells, and treatment with iloprost resulted in a similar down-regulation of cellular Gs alpha levels. (biochemj.org)
- These results demonstrate that the phenomenon of agonist-induced specific G-protein down-regulation is determined by the levels of expression of the receptor. (biochemj.org)
- an active role for receptor immobilization in down-regulation? (springer.com)
- Although adenosine agonists were shown to attenuate pain behaviors in a variety of animal models, adenosine agonists are also implicated in the regulation of many physiologic processes, especially cardiovascular and neurologic, which either reduce the activity of excitable tissues ( e.g. , by slowing heart rate) or increase the delivery of metabolic substrates ( e.g. , inducing vasodilation). (asahq.org)
- In addition, adenosine A1 receptor regulation after chronic oral T62 administration was examined. (asahq.org)
- Methods and aims: Using a well-characterized animal model of binge eating, we investigated the epigenetic regulation of the A 2A Adenosine Receptor (A 2A AR) and dopaminergic D2 receptor (D2R) genes. (elsevier.com)
- We suggest that A 2A AR activation, inducing receptor gene up-regulation, could be relevant to reduction of food consumption. (elsevier.com)
- The adenosine receptors play crucial role in the regulation of the function of the myocardium and the central nervous system. (otka-palyazat.hu)
- Wound healing is impaired in MyD88-deficient mice: a role for MyD88 in the regulation of wound healing by adenosine A2A receptors. (naver.com)
- Conclusion:Based on these results it could be concluded that the role of A2B receptors in regulation of rCBF in morphine-dependent rats is more effective than A2A receptors. (phypha.ir)
- Baranowski RL, Westenfelder C (1994) Estimation of renal interstitial adenosine and purine metabolites by microdialysis. (springer.com)
- Our data confirm that the modulation of adenosine receptors can elicit very different (and even opposite) effects during the progression of ALS course, thus strengthens the importance of further studies to elucidated their real therapeutic potential in this pathology. (elsevier.com)
- The modulation of cell growth by adenosine was found to be receptor-mediated. (nus.edu.sg)
- In contrast to the adenosine A2 receptor agonist 5'-N-ethylcarboxamidoadenosine, nucleotide analogues had no discernible effect on cytosolic adenosine 3',5'-cyclic monophosphate levels or adenylyl cyclase activity. (rti.org)
- On the other hand adenosine analogues have been shown to possess antinociceptive effects after peripheral and intrathecal administration in animals. (nih.gov)
- The dominant effect of an elevation of plasma adenosine in the renal vasculature is an A 2A AR- and A 2B AR-mediated vasodilatation that increases global as well as medullary renal blood flow and is in part endothelium-dependent. (springer.com)
- Experimental evidence supports the notion that adenosine protects against ischemia-induced acute kidney injury by directly acting on renal endothelial and tubular A 1 AR. (springer.com)
- Moreover, adenosine protects against renal ischemic reperfusion injury by the anti-inflammatory effect of enhancing the activity of regulatory T cell and by attenuating the inflammatory injury produced by neutrophils via A 2 AR activation. (springer.com)
- Beach RE, Watts BA 3rd, Good DW et al (1991) Effects of graded oxygen tension on adenosine release by renal medullary and thick ascending limb suspensions. (springer.com)
- The aim of the current study was to investigate further the effects of intrarenal administration of adenosine on renal excretory function in the rat. (aspetjournals.org)
- During infusion of adenosine by all three routes, there was a significant decline in glomerular filtration rate, but no change in renal plasma flow. (aspetjournals.org)
- Ammonium chloride affects receptor number and lateral mobility of the vasopressin V2-type receptor in the plasma membrane of LLC-PK, renal epithelial cells: role of the cytoskeleton. (springer.com)
- Renal actions of a new adenosine agonist, CGS 21680A selective for the A2 receptor. (toshan.ru)
- First, adenosine levels markedly increase in response to cerebral ischemia and hypoxia as ATP breakdown dramatically increases the formation of adenosine. (jneurosci.org)
- Adenosine is produced in response to trauma, ischemia, and hypoxia and plays an important role in preventing excessive tissue damage. (ptglab.com)
- Vascular leakage secondary to hypoxia was reversed in part by adenosine receptor agonists or reconstitution with soluble 5′-nucleotidase. (rupress.org)
- Some of the agents that are thought to be released during hypoxia, which may trigger the EPO cascade, are adenosine (A2 activation), eicosanoids (PGE2, PGI2, and 6-keto PGE1), oxygen-free radicals (superoxide and H2O2), and catecholamines with beta-2 adrenergic receptor agonist properties. (dailypeloton.com)
- Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (nih.gov)
- 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)
- Two other small molecules included in this review are adenosine A 2A receptor agonists that indirectly activate TrkB, and TrkB binding domains of BDNF, loop II-LM22A compounds that directly activate TrkB. (elsevier.com)
- Surface-localized CD73 converts AMP into adenosine, which in turn can activate transmembrane adenosine receptors or can be internalized through dipyridamole-sensitive carriers ( 14 ). (rupress.org)
- This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. (wikipedia.org)
- The gene encodes a protein which is one of several receptor subtypes for adenosine. (wikipedia.org)
- In this role, A2AR functions similarly to programmed cell death-1 (PD-1) and cytotoxic t-lymphocyte associated protein-4 (CTLA-4) receptors, namely to suppress immunologic response and prevent associated tissue damage. (wikipedia.org)
- Furthermore, adenosine significantly attenuated protein degradation of A2A and A3 receptors induced by LPS. (physiology.org)
- The adenosine A1 receptor (Adora1) is a G-protein coupled receptor (GPCR) that is involved in maintaining glucose homeostasis and regulating glucagon secretion ( 11 , 12 ). (diabetesjournals.org)
- A cDNA fragment homologous to other G protein-coupled receptors was isolated from rat brain using the PCR method and demonstrated to be abundantly expressed in striatum. (nih.gov)
- This cDNA encodes a protein of 410 amino acids and is highly homologous to previously isolated adenosine receptor cDNAs. (nih.gov)
- This cDNA contains a long open reading frame encoding a 409-amino acid-residue protein which is highly homologous to the A2 adenosine receptors previously cloned from other species. (nih.gov)
- Hydrophobicity analysis of the deduced protein sequence reveals seven hydrophobic regions, characteristic of a member of the G-protein-coupled receptor superfamily. (nih.gov)
- 300 fmol/mg of membrane protein of the receptor. (biochemj.org)
- Tyrosine kinase and GTP-binding protein activating receptors appear to be essentially different in terms of their lateral mobility properties, and it seems plausible to relate these differences to their distinct signal transduction mechanisms. (springer.com)
- Experimental studies with experimental rodent models and cultures (cardiac myocytes, endothelial cells) indicate that moderate alcohol exposure can promote anti-inflammatory processes involving adenosine receptors, protein kinase C (PKC), nitric oxide synthase, heat shock proteins, and others which could underlie cardioprotection. (pubmedcentralcanada.ca)
- Lipoprotein receptor-related protein-1 mediates amyloid-beta-mediated cell death of cerebrovascular cells. (naver.com)
- Conversely, blockade of adenosine A1 receptors from the presymptomatic stage significantly attenuated motor disease progression and induced a non-significant increase of median survival in ALS mice. (elsevier.com)
- Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
- Insulin indirectly relieves GS inhibition ( 4 , 5 ) through a signaling cascade beginning with phosphorylation of substrates, including insulin receptor substrate 1 (IRS-1), by the tyrosine kinase activity of activated insulin receptor ( 6 , 7 ). (diabetesjournals.org)
- The DRP is a gamma-aminobutyric acid A (GABA A ) receptor-mediated depolarization of primary afferent terminals, which reflects a feedback inhibition associated with analgesia. (asahq.org)
- In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. (nus.edu.sg)
- The increase in LPS-induced IL-10 production and suppression of LPS-induced TNF-α and NO production caused by adenosine receptor activation may explain some of the immunomodulatory actions of adenosine released in excess during inflammatory and/or ischemic insult. (utmb.edu)
- [3-In the central nervous system, two main types of receptors are believed to mediate the actions of adenosine: A 1 and A 2 types of adenosine receptors. (asahq.org)
- [19-Therefore, examination of the actions of adenosine agonists on these responses and characterization of the adenosine receptors involved may provide further information on the mechanism of adenosine-induced antinociception. (asahq.org)
- These low molecular weight compounds activated glycogen synthase at ∼100 nmol/l in cultured CHO cells transfected with the insulin receptor and in primary hepatocytes isolated from Sprague-Dawley rats, and at 500 nmol/l in isolated type 1 skeletal muscle of both lean Zucker and ZDF rats. (diabetesjournals.org)
- that the claimed compounds would have an A1-adenosine receptor antagonistic activity. (epo.org)
- 12,13 An adenosine receptor modulator, T62, belonging to a group of thiophene compounds first described a decade ago, 14 has been shown to reduce mechanical allodynia in spinal nerve-injured rats after oral, parenteral, or intrathecal application. (asahq.org)
- IFN-γ priming of macrophages selectively prevents the induction of the A2bR in macrophages to mitigate sensitivity to adenosine and to prevent this regulatory transition. (jimmunol.org)
- Thus, the generation of adenosine by macrophages is an important mechanism that prevents overactive inflammatory responses. (jimmunol.org)
- As a result, adenosine decreases the phagocytic activity of macrophages by suppressing the generation of nitric oxide (18), superoxide (19, 20) and pro-inflammatory cytokines (21). (deepdyve.com)
- Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear to mediate slow synaptic responses in the CNS. (jneurosci.org)
- Nucleotide receptors may effect their responses through primary activation of membrane chloride channels. (rti.org)
- It has been reported recently that adenosine and ATP produce dose- and tone-dependent responses in the feline pulmonary vascular (PV) bed. (aspetjournals.org)
- The present study was undertaken to investigate the mechanisms mediating vasoconstrictor (VC) responses to adenosine and ATP in the intact-chest, spontaneously breathing cat under conditions of controlled blood flow and constant left atrial pressure. (aspetjournals.org)
- One of the major pathways by which the oxidative damage produced by free radicals promotes inflammatory responses, involves the Toll-like-receptors (TLRs). (scirp.org)
- The volume of cerebral infarction, as well as the associated neurological deficit induced by transient filament occlusion of the middle cerebral artery, were significantly attenuated in A 2A receptor knock-out mice. (jneurosci.org)
- This neuroprotective phenotype of A 2A receptor-deficient mice was observed in different genetic backgrounds, confirming A 2A receptor disruption as its cause. (jneurosci.org)
- Cell counts, EBDA extravasation, as well as levels of proteins and inflammatory cytokines were decreased in adenosine-treated mice. (physiology.org)
- Here, we show that the expression of a potential glucagon inhibitor, the adenosine A1 receptor (Adora1), is gradually diminished in α-cells of NOD mice, autoantibody-positive (AA + ) and overtly type 1 diabetic (T1D) patients during the progression of disease. (diabetesjournals.org)
- Finally, when stimulated with cholinergic or cAMP agonists, cells from mice that lacked CFTR, as well as wild-type cells treated with a CFTR inhibitor, exhibited identical rates and magnitudes of shrinkage and Cl − efflux compared with control cells. (wiley.com)
- Influences of different adenosine receptor subtypes on catalepsy in mice. (nih.gov)
- In this study we report that i.p. pretreatment of mice with CGS-21680 HCl (CGS), a selective agonist of A 2 adenosine receptors, at 0.2 to 2 mg/kg caused an augmentation of plasma IL-10 levels induced by i.p. injection of LPS, but decreased plasma levels of LPS-induced TNF-α. (utmb.edu)
- Castillo A et al: "The neuroprotective effect of cannabidiol in an in vitro model of newborn hypoxic-ischemic brain damage in mice is mediated by CB(2) and adenosine receptors. (unboundmedicine.com)
- TY - JOUR T1 - The neuroprotective effect of cannabidiol in an in vitro model of newborn hypoxic-ischemic brain damage in mice is mediated by CB(2) and adenosine receptors. (unboundmedicine.com)
- Their theory is based on the fact that adenosine is produced within the body and inhibits neuronal excitability and synapse transmission. (innovations-report.com)
- Adenosine also inhibits neutrophil degranulation (22). (deepdyve.com)
- The aim of the present study was to investigate the effect of peripheral administration of adenosine agonists with different affinities for the A1 and A2 adenosine receptors on a persistent pain stimulus using the formalin test. (nih.gov)
- This contraction was also inhibited by ethacrynic acid, by inhibitors of Na+, K+-ATPase (ouabain), Ca2+- ATPase (thapsigargin), and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, by a non-selective phosphodiesterase inhibitor (papaverine), and by adenosine A2 (metrifudil), and cannabinoid receptor (CP-55940) agonists. (omicsonline.org)
- Abebe W, Hussain T, Olanrewaju H et al (1995) Role of nitric oxide in adenosine receptor-mediated relaxation of porcine coronary artery. (springer.com)
- It has been shown that an A2AR agonist protects against ischemia-reperfusion injury in porcine allogeneic lung transplantation ( 23 ). (physiology.org)
- We identified pTM cells, obtained from porcine eyeballs, by cell shape and expression of Low Density Lipoprotein (LDL) receptors. (omicsonline.org)
- Porcine pancreatic arteries appear to lack vasorelaxant P2Y2 and P2Y4 receptors. (nottingham.ac.uk)