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)

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Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.
Structure, properties, spectra, suppliers and links for: 6-(6-Amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide.
6-Amino-1,3-dihydro-2H-purin-2-one; CAS Number: 3373-53-3; Linear Formula: C5H5N5O; find Ambeed, Inc.-AMBH46A96504 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich
You are viewing an interactive 3D depiction of the molecule 1-(7h-purin-6-yl)-n-[3-(trifluoromethyl)phenyl]-4-piperidinecarboxamide (C18H17F3N6O) from the PQR.
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This work done by an eminent group in the area raises concerns over the use of regadenoson for clinical stress testing, whether done by PET or SPECT. Invasive and pharmacologic studies had previously demonstrated peak regadenoson effect at approximately 1-2 minutes after injection, consistent with the findings of the present study. Stress labs which are not already following a 1- to 2-minute delay may wish to consider introducing one.. There are several reasons to view these results with caution, however. First, many prior studies had compared regadenoson to other vasodilators using a variety of techniques including PET, SPECT, and invasive methods. In general, no significant differences or only minimal differences, below the level of clinical relevance, were observed. The reasons for the discrepancies are unclear.. One longstanding concern with regards to regadenoson has been the use of a single fixed dose without weight adjustment, as is usually done for other vasodilators. The investigators ...
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3-[(6-azido-9H-purin-9-yl)methyl]phenylformamide - chemical structural formula, chemical names, chemical properties, synthesis references
Regadenoson produced higher stress MBF than dipyridamole and adenosine (3.58 ± 0.58 vs. 2.81 ± 0.67 vs. 2.78 ± 0.61 ml/min/g, p = 0.0009 and p = 0.0008 respectively). Regadenoson had a much higher heart rate response than adenosine and dipyridamole respectively (95 ± 11 vs. 76 ± 13 vs. 86 ± 12 beats/ minute) When stress MBF was adjusted for heart rate, there were no differences between regadenoson and adenosine (37.8 ± 6 vs. 36.6 ± 4 μl/sec/g, p = NS), but differences between regadenoson and dipyridamole persisted (37.8 ± 6 vs. 32.6 ± 5 μl/sec/g, p = 0.03). The unadjusted MPR was higher with regadenoson (3.11 ± 0.63) when compared with adenosine (2.7 ± 0.61, p = 0.02) and when compared with dipyridamole (2.61 ± 0.57, p = 0.04). Similar to stress MBF, these differences in MPR between regadenoson and adenosine were abolished when adjusted for heart rate (2.04 ± 0.34 vs. 2.12 ± 0.27, p = NS), but persisted between regadenoson and dipyridamole (2.04 ± 0.34 vs. 1.77 ± 0.33, p = ...
Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients.1-4 In addition, both adenosine and dipyridamole produce severe bronchoconstriction when given to asthmatics. Because of its ultrashort half-life, adenosine must be administered by a constant IV infusion.. Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A1, A2B, and A3.5 The discovery of highly selective and relatively short-acting adenosine receptor A2A agonists6-9 has opened the ...
Approximately 250 patients who are referred for a nuclear stress testing of the heart with regadenoson (Lexiscan®) will be recruited to participate in the study. Following regadenoson (administered as part of a stress routine test protocol) participants will receive either aminophylline (75 mg - intravenously) or a matching inactive placebo (sterile salt water) injection. Participants will be surveyed for gastrointestinal symptoms and other side effects related to regadenoson. The frequency and severity of such side effects will be compared between the two study groups (aminophylline vs. placebo ...
8-(1-hydroxyethyl)-1,3-dimethyl-7H-purine-2,6-dione,8-cyclohexyl-1,3-dimethyl-7H-purine-2,6-dione,8-(cyclohexylamino)-1,3-dimethyl-7H-purine-2,6-dione,8-[(4-aminophenyl)methyl]-1,3-dimethyl-7H-purine-2,6-dione,8-cyclohexyl-1,3,7-trimethyl-purine-2,6-dione,8-cyclohexyloxy-1,3,7-trimethyl-purine-2,6-dione,8-hexyl-1,3,7-trimethyl-purine-2,6-dione,8-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]octanoic acid,8-[1-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]ethyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[3-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]propyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[4-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]butyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[5-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]pentyl]-1,3-dimethyl-7H-purine-2,6-dione,8-[6-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]hexyl]-1,3-dimethyl-7H-purine-2,6-dione,8-(diphenylmethyl)-1,3,7-trimethyl-purine-2,6-dione,8-[8-[1,3-dimethyl-2,6-bis(oxidanylidene)-7H-purin-8-yl]octyl]-1,3
You are viewing an interactive 3D depiction of the molecule [(2s)-4-(2-amino-6-oxo-3h-purin-9-yl)-2-(hydroxymethyl)butyl] (hydroxy-phosphonooxy-phosphoryl) hydrogen phosphate (C10H19N5O12P3) from the PQR.
142130-73-2 - UZNXSBPBWFLVDK-NKWVEPMBSA-N - 3-(6-Amino-9H-purin-9-yl)-cyclopentanol - Similar structures search, synonyms, formulas, resource links, and other chemical information.
N,N,9-Trimethyl-9H-purin-6-amine | C8H11N5 | CID 221105 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Product Number: C6621 CAS number: 390409-17-3 unlabeled Synonyms: GS-7171 fumarate // [2H6]-N-[[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-1-methylethyl ester-L-alanine fumarate-d6. ...
Product Number: C6621 CAS number: 390409-17-3 unlabeled Synonyms: GS-7171 fumarate // [2H6]-N-[[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-1-methylethyl ester-L-alanine fumarate-d6. ...
Adenoscan® (adenosine) is an approved pharmacological stress agent indicated as an adjunct to thallium-201 myocardial perfusion scintigraphy in patients unable to exercise adequately. The investigational drug, regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist, the receptor responsible for coronary vasodilation, and is being studied for potential use as a pharmacologic stress agent in myocardial perfusion imaging (MPI) studies. This study will compare the safety and efficacy of regadenoson to that of Adenoscan in detecting reversible myocardial perfusion defects ...
Adenosine might provoke bronchospasm in certain susceptible patients such as those with asthma or those on maintenance doses of bronchodilators or steroids. The selectivity of regadenoson was therefore of great interest to study for its safety and efficacy in such patients. The final answer is not yet in, and more studies are needed, but there are some preliminary data.. Prior studies have suggested that with prophylactic pre-treatment with a B-2 agonist, adenosine could be given to patients with mild asthma or chronic obstructive lung disease (COPD). It should be noted the majority of patients with COPD but no bronchospasm could be tested with adenosine without any serious problem (39). Further, tachypnea is common after adenosine infusion and is not due to changes in airway resistance or pulmonary capillary wedge pressure but rather to stimulation of carotid body receptors (40,41).. A randomized double-blind, placebo-controlled cross-over trial assessed the safety of regadenoson in 48 patients ...
In a recent prospective, double-blind, randomized multicenter phase 3 trial, ADVANCE (Adenosine versus Regadenoson Comparative Evaluation for Myocardial Perfusion Imaging), the A2A selective adenosine receptor agonist, regadenoson, was shown to be noninferior to the nonselective vasodilator, adenosine, for detecting myocardial ischemia (1). The overall visual agreement was comparably low (in the low 60% range) for the adenosine-regadenoson and for the adenosine-adenosine comparisons. Conversely, when quantitative analysis was applied, regadenoson induced virtually identical results to adenosine-regarding the size and severity of left ventricular perfusion defect size and extent of ischemia (2). What are the regulatory implications of these findings? Should the regulatory bodies rely on subjective visual interpretation of myocardial perfusion studies, on objective quantitative programs to appraise the comparability between vasodilators, or both? What is the "true" standard?. In order to avoid the ...
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3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile chemical properties, What are the chemical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile 86375-28-2, What are the physical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile ect.
chemBlink provides information about CAS # 3945-69-5, 4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methyl morpholinium chloride, DMTMM, molecular formula: C10H17ClN4O3.
Methanol,[(4,6-dimethyl-1,3,5-triazin-2-yl)amino]-(9ci)/ACM84591888 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
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Structure, properties, spectra, suppliers and links for: N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide.
Are you stress now? Let me tell you about it. Stress is simply the bodys reaction the wear and tear of life. Every single activity you engage in, every emotion you feel, whether it is asking the boss for a raise, or trying to complete an assignment, set up stress. The way your body reacts to such stress agents has much to do with your health ...
Buy CGS 21680 (CAS 124182-57-6), a potent, selective A2A agonist. Join researchers using high quality CGS 21680 from Abcam and achieve your mission, faster.
A review. The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain G protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various species, including rat and human, and its sequences are highly similar across species, ranging from 85% identity between human and mouse and 95% identity between rat and mouse. The A2B receptors show a ubiquitous distribution, the highest levels are present in cecum, colon and bladder, followed by blood vessels, lung, eye and mast cells. Through A2B receptors adenosine seems to cause mast cells degranulation, vasodilation, cardiac fibroblast proliferation, inhibition of Tumor Necrosis Factor (TNF-α), increased synthesis of interleukin-6 (IL-6), stimulation of Cl- secretion in intestinal epithelia and hepatic glucose prodn. Hence, A2B adenosine receptor agonists could be useful ...
ALI is one of the leading causes of morbidity and mortality of critical illness with extremely limited therapeutic options. In the present study, we pursued the hypothesis that tissue-specific adenosine signaling events through the A2B adenosine receptor contribute to lung protection and can thus be targeted for ALI treatment. To make progress on this front, we performed a head-to-head comparison of mice with genetic deletion of Adora2b in the myeloid lineage, vascular endothelial cells, or alveolar epithelial cells. Interestingly, we only observed a phenotype in mice with tissue-specific Adora2b deletion in alveolar epithelial cells, closely resembling the observed detrimental effects of global Adora2b deletion during ALI. Interestingly, the injurious effects of our two-hit model where an inflammatory event (i.t. LPS treatment) is followed by injurious mechanical ventilation seem to be supra-additive compared with the effects of injurious ventilation or LPS i.t. alone. Based on these findings ...
Particularly preferably, Z21 is 2,4-dichloro-1,3,5-triazin-6-ylf 2-chloro-4-(3-(2-suifatoethylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-chloro-4-(4-(2-su!fatoethy!sulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-chloro-4-(3-(vinylsulfonyl)-phenylarnino)-1 t3,5-triazin-6-yl, 2-chloro4-(4-(vinylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl, 2-ch!oro-4-(N-methy!-N-(2-(2-sulfatoethylsulfonyl)-ethy!)-amino)-1,3,5-triazin-6-yl, 2-ch!oro-4-(N-phenyl-N-(2-(2-sulfatoethylsulfonyl)-ethyl)-amino)-1,3,5-tria2in-6-yl, 2-fluoro-4-morpholino-1,3,5-triazin-6-yI, 2-fluoro-4-(2-sulfophenyl-amino)-1,3,5-triazin-6-yl, 2-fluoro-4-(3-sulfophenylamino)-1,3,5-triazin-6-yl, 2-fluoro-4-(4-sulfophenylamino)-1,3,5-triazin-6-yl, 2-fiuoro-4-(3-trimethylammonio-phenylamino)-1,3,5-triazin-6-ylf 2-fIuoro-4-(4-trirnethylammoniophenylamino)-1,3,5-triazin-6-yl, 2-fluoro-4-(3-(2-sulfatoethylsulfonyl)-phenylamino)-1,3,5-triazin-6-yl( 2-fluoro-4-(4-(2-sulfatoethylsulfonyl,-phenylamino)-1 f3,5-triazin-6-yl, ...
Two main findings arise from this study: (1) the adenosine A2A receptor antagonist SCH 58261 shows neuroprotective effects in an excitotoxic rat model of HD; and (2) the inhibition of QA-evoked increase in extracellular glutamate seems to be the main mechanism of the effects elicited by SCH 58261.. The finding that SCH 58261 significantly prevented most of the effects induced by the intrastriatal injection of an excitotoxin is in line with some findings suggesting that activation of A2A receptors could participate in the generation of excitotoxicity. Adenosine A2A receptor agonists have been reported indeed to stimulate glutamate release in the rat striatum (Popoli et al., 1995; Corsi et al., 1999). Moreover, in previous experiments, we observed that the intrastriatal injection of the adenosine A2A receptor agonist CGS 21680, together with QA, potentiated QA-induced mortality in a dose-dependent way (50, 75, and 83% of mortality after 3, 6, and 12 nmol QA plus CGS 21680, respectively; P. Popoli, ...
... aims at providing comprehensive data on 9h-purin-2-amine, 9-methyl- (9ci)
While regadenoson has become the vasodilator stress agent of choice and has streamlined and simplified stress protocols in many nuclear stress laboratories, the adverse effect of dyspnea is still experienced by many patients, and even more so by those with COPD and asthma. While patients and practitioners should anticipate this symptom, several studies have shown that the subjective experience of dyspnea is not correlated with and is not caused by bronchoconstriction. Available data from observational studies as well as controlled clinical trials, as summarized in Table 1, indicate that the use of regadenoson in patients with mild to moderate asthma and mild to moderate COPD is safe. The current data in patients with severe COPD, while limited, are reassuring and indicate that regadenoson is probably safe, particularly in those with stable lung disease. Clinical data are limited in COPD patients who require 24-hour/day home oxygen administration, have previously been intubated for respiratory ...
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BioAssay record AID 243741 submitted by ChEMBL: Inhibition of [3H]CGS-21680 binding to Adenosine A2A receptor expressed in CHO cells.
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for h
DESCRIPTION: (Adapted from the Investigators Abstract): Adenosine administered as an aerosol to asthmatics causes bronchoconstriction, while in non-asthmatics adenosine causes bronchodilation. This occurs because the activation of A2B adenosine receptors on sensitized mast cells triggers degranulation, releasing histamine, leukotrienes, and other allergic mediators. A2B adenosine receptors are blocked by theophylline, a xanthine that is effective in treating asthma. However, theophylline is a non-selective antagonist of all four adenosine receptor subtypes and produces side effects due primarily to A1 receptor blockade, including insomnia and diuresis. The incidence of asthma is increasing and current treatment options are limited. New drugs that are potent and selective antagonists of A2B adenosine receptors have great potential for the treatment of asthma and other allergic diseases. Adenosine Therapeutics, LLC owns the first potent and selective A2B antagonists. The purpose of this phase I ...
Disclosed are processes for the synthesis of novel compounds that are A.sub.2B adenosine receptor antagonists, having the structure of Formula I or Formula II: ##STR00001## by cyclizing a compound of the formula (3): ##STR00002##
TY - JOUR. T1 - Modulating P1 Adenosine Receptors in Disease Progression of SOD1G93A Mutant Mice. AU - Armida, Monica. AU - Matteucci, Alessandra. AU - Pèzzola, Antonella. AU - Baqi, Younis. AU - Müller, Christa E. AU - Popoli, Patrizia. AU - Potenza, Rosa Luisa. PY - 2019/5. Y1 - 2019/5. N2 - Amyotrophic lateral sclerosis (ALS) is a fatal progressing neurodegenerative disease; to date, despite the intense research effort, only two therapeutic options, with very limited effects, are available. The purinergic system has been indicated as a possible new therapeutic target for ALS, but the results are often contradictory and generally confused. The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. Body weight, motor performance ...
2-[4,6-Bis(2,4-dimethylphenyl)-1,3,5-triazin-2-yl]-5-(octyloxy)phenol 2725-22-6 MSDS report, 2-[4,6-Bis(2,4-dimethylphenyl)-1,3,5-triazin-2-yl]-5-(octyloxy)phenol MSDS safety technical specifications search, 2-[4,6-Bis(2,4-dimethylphenyl)-1,3,5-triazin-2-yl]-5-(octyloxy)phenol safety information specifications ect.
You are looking for 2,6-di-tert-butyl-4-(4,6-bis(octylthio)-1,3,5-triazin-2-ylamino)phenol from Kuo Ching Chemical Co., LTD ? ...
View mouse Adora1 Chr1:134199225-134235431 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
View mouse Adora2a Chr10:75316877-75334784 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
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N-benzyl-N-ethyl-2-(7,8-dihydro-7-methyl-8-oxo-2-phenyl-9H-purin-9-yl)acetamide: mitochondrial benzodiazepine receptor ligand with anti-anxiety and antidepressant-like effects; structure in first source
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
... 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 ...
  • 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)
  • 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)
  • 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)
  • 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)
  • Maggio and co-workers showed in 1993 the ability of the muscarinic M3 receptor and α2C-adrenoceptor to heterodimerize. (wikipedia.org)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)