2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.
A 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.
Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
Purine bases found in body tissues and fluids and in some plants.
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).
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
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.
An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.
Copolymer of divinyl ether and maleic anhydride that acts as an immunostimulant with antineoplastic and anti-infective properties. It is used in combination with other antineoplastic agents.
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)
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.
An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.
A toxic alkaloid found in Amanita muscaria (fly fungus) and other fungi of the Inocybe species. It is the first parasympathomimetic substance ever studied and causes profound parasympathetic activation that may end in convulsions and death. The specific antidote is atropine.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Hydrazine substituted by one methyl group.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
The study of the origin, nature, properties, and actions of drugs and their effects on living organisms.
The branch of pharmacology that deals directly with the effectiveness and safety of drugs in humans.
An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.
Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.
Small kinetoplastid mitochondrial RNA that plays a major role in RNA EDITING. These molecules form perfect hybrids with edited mRNA sequences and possess nucleotide sequences at their 5'-ends that are complementary to the sequences of the mRNA's immediately downstream of the pre-edited regions.
Peptides composed of two amino acid units.
A naturally occurring dipeptide neuropeptide found in muscles.
Substances that are toxic to the intestinal tract causing vomiting, diarrhea, etc.; most common enterotoxins are produced by bacteria.
The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments.
Human colonic ADENOCARCINOMA cells that are able to express differentiation features characteristic of mature intestinal cells, such as ENTEROCYTES. These cells are valuable in vitro tools for studies related to intestinal cell function and differentiation.
Fluids originating from the epithelial lining of the intestines, adjoining exocrine glands and from organs such as the liver, which empty into the cavity of the intestines.
Round, granular, mononuclear phagocytes found in the alveoli of the lungs. They ingest small inhaled particles resulting in degradation and presentation of the antigen to immunocompetent cells.
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.)
A form of hypersensitivity affecting the respiratory tract. It includes ASTHMA and RHINITIS, ALLERGIC, SEASONAL.
Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood.
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.
The process of altering the morphology and functional activity of macrophages so that they become avidly phagocytic. It is initiated by lymphokines, such as the macrophage activation factor (MAF) and the macrophage migration-inhibitory factor (MMIF), immune complexes, C3b, and various peptides, polysaccharides, and immunologic adjuvants.
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
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.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
Serine proteinase inhibitors which inhibit trypsin. They may be endogenous or exogenous compounds.
A darkly stained mat-like EXTRACELLULAR MATRIX (ECM) that separates cell layers, such as EPITHELIUM from ENDOTHELIUM or a layer of CONNECTIVE TISSUE. The ECM layer that supports an overlying EPITHELIUM or ENDOTHELIUM is called basal lamina. Basement membrane (BM) can be formed by the fusion of either two adjacent basal laminae or a basal lamina with an adjacent reticular lamina of connective tissue. BM, composed mainly of TYPE IV COLLAGEN; glycoprotein LAMININ; and PROTEOGLYCAN, provides barriers as well as channels between interacting cell layers.
A cluster of convoluted capillaries beginning at each nephric tubule in the kidney and held together by connective tissue.
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.
A hydroxylated form of the imino acid proline. A deficiency in ASCORBIC ACID can result in impaired hydroxyproline formation.
Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES).
A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.

Interruption of transmembrane signaling as a novel antisecretory strategy to treat enterotoxigenic diarrhea. (1/208)

Bacteria that produce heat-stable enterotoxins (STs), a leading cause of secretory diarrhea, are a major cause of morbidity and mortality worldwide. ST stimulates guanylyl cyclase C (GCC) and accumulation of intracellular cyclic GMP ([cGMP]i), which opens the cystic fibrosis transmembrane conductance regulator (CFTR)-related chloride channel, triggering intestinal secretion. Although the signaling cascade mediating ST-induced diarrhea is well characterized, antisecretory therapy targeting this pathway has not been developed. 2-ChloroATP (2ClATP) and its cell-permeant precursor, 2-chloroadenosine (2ClAdo), disrupt ST-dependent signaling in intestinal cells. However, whether the ability to disrupt guanylyl cyclase signaling translates into effective antisecretory therapy remains untested. In this study, the efficacy of 2ClAdo to prevent ST-induced water secretion by human intestinal cells was examined. In Caco-2 human intestinal cells, ST increased [cGMP]i, induced a chloride current, and stimulated net basolateral-to-apical water secretion. This effect on chloride current and water secretion was mimicked by the cell-permeant analog of cGMP, 8-bromo-cGMP. Treatment of Caco-2 cells with 2ClAdo prevented ST-induced increases in [cGMP]i, chloride current and water secretion. Inhibition of the downstream consequences of ST-GCC interaction reflects proximal disruption of cGMP production because 8-bromo-cGMP stimulated chloride current and water secretion in 2ClAdo-treated cells. Thus, this study demonstrates that disruption of guanylyl cyclase signaling is an effective strategy for antisecretory therapy and provides the basis for developing mechanism-based treatments for enterotoxigenic diarrhea.  (+info)

Depletion of alveolar macrophages by treatment with 2-chloroadenosine aerosol. (2/208)

Alveolar macrophages (AMs) are localized in the alveoli and alveolar ducts of the lung and are the only macrophages living in an aerobic environment. Recent studies have demonstrated that AMs play a central role in lung diseases, such as pneumonia and acute respiratory distress syndrome. It has become important to find a simple, effective way to eliminate AMs in order to investigate the function of AMs in vivo. 2-Chloroadenosine (2-CA), a purine analog, is reported to be selectively cytotoxic to cultured macrophages, and we hypothesized that it would deplete the number of AMs in the bronchoalveolar lavage fluid (BALF) of mice without any effect on neutrophil or lymphocyte counts. After mice had inhaled 1 mM aerosolized 2-CA for 2 h, AMs were found to be significantly depleted at 0 h [(4.42 +/- 0.16) x 10(4)/ml], 24 h [(4.17 +/- 0.89) x 10(4)/ml], 48 h [(3.17 +/- 0.21) x 10(4)/ml], and 72 h [(5.00 +/- 0.64) x 10(4)/ml] compared with concentrations in untreated controls [(12.1 +/- 0.21) x 10(4)/ml]. Neutrophil and lymphocyte counts in BALF did not change and histological changes in the lung were not observed after 2-CA treatment. The lung wet-to-dry weight ratio did not change at 0, 24, and 48 h after 2-CA aerosol application. The 2-CA aerosol had no effect on lung vascular permeability, as assessed by the intravenous administration of Evans blue, or on other phagocytes, as assessed by Kupffer cell counts. Our study demonstrates the efficacy of 2-CA in reducing AM numbers in vivo.  (+info)

A(2B) receptors mediate antimitogenesis in vascular smooth muscle cells. (3/208)

Adenosine inhibits growth of vascular smooth muscle cells. The goals of this study were to determine which adenosine receptor subtype mediates the antimitogenic effects of adenosine and to investigate the signal transduction mechanisms involved. In rat aortic vascular smooth muscle cells, platelet-derived growth factor-BB (PDGF-BB) (25 ng/mL) stimulated DNA synthesis ([(3)H]thymidine incorporation), cellular proliferation (cell number), collagen synthesis ([(3)H]proline incorporation), total protein synthesis ([(3)H]leucine incorporation), and mitogen-activated protein (MAP) kinase activity. The adenosine receptor agonists 2-chloroadenosine and 5'-N-methylcarboxamidoadenosine, but not N(6)-cyclopentyladenosine or CGS21680, inhibited the growth effects of PDGF-BB, an agonist profile consistent with an A(2B) receptor-mediated effect. The adenosine receptor antagonists KF17837 and 1,3-dipropyl-8-p-sulfophenylxanthine, but not 8-cyclopentyl-1, 3-dipropylxanthine, blocked the growth-inhibitory effects of 2-chloroadenosine and 5'-N-methylcarboxamidoadenosine, an antagonist profile consistent with an A(2) receptor-mediated effect. Antisense, but not sense or scrambled, oligonucleotides to the A(2B) receptor stimulated basal and PDGF-induced DNA synthesis, cell proliferation, and MAP kinase activity. Moreover, the growth-inhibitory effects of 2-chloroadenosine, 5'-N-methylcarboxamidoadenosine, and erythro-9-(2-hydroxy-3-nonyl) adenine plus iodotubericidin (inhibitors of adenosine deaminase and adenosine kinase, respectively) were abolished by antisense, but not scrambled or sense, oligonucleotides to the A(2B) receptor. Our findings strongly support the hypothesis that adenosine causes inhibition of vascular smooth muscle cell growth by activating A(2B) receptors coupled to inhibition of MAP kinase activity. Pharmacological or molecular biological activation of A(2B) receptors may prevent vascular remodeling associated with hypertension, atherosclerosis, and restenosis following balloon angioplasty.  (+info)

Altered regulation of potassium and calcium channels by GABA(B) and adenosine receptors in hippocampal neurons from mice lacking Galpha(o). (4/208)

To examine the role of G(o) in modulation of ion channels by neurotransmitter receptors, we characterized modulation of ionic currents in hippocampal CA3 neurons from mice lacking both isoforms of Galpha(o). In CA3 neurons from Galpha(o)(-/-) mice, 2-chloro-adenosine and the GABA(B)-receptor agonist baclofen activated inwardly rectifying K(+) currents and inhibited voltage-dependent Ca(2+) currents just as effectively as in Galpha(o)(+/+) littermates. However, the kinetics of transmitter action were dramatically altered in Galpha(o)(-/-) mice in that recovery on washout of agonist was much slower. For example, recovery from 2-chloro-adenosine inhibition of calcium current was more than fourfold slower in neurons from Galpha(o)(-/-) mice [time constant of 12.0 +/- 0.8 (SE) s] than in neurons from Galpha(o)(+/+) mice (time constant of 2.6 +/- 0.2 s). Recovery from baclofen effects was affected similarly. In neurons from control mice, effects of both baclofen and 2-chloro-adenosine on Ca(2+) currents and K(+) currents were abolished by brief exposure to external N-ethyl-maleimide (NEM). In neurons lacking Galpha(o), some inhibition of Ca(2+) currents by baclofen remained after NEM treatment, whereas baclofen activation of K(+) currents and both effects of 2-chloro-adenosine were abolished. These results show that modulation of Ca(2+) and K(+) currents by G protein-coupled receptors in hippocampal neurons does not have an absolute requirement for Galpha(o). However, modulation is changed in the absence of Galpha(o) in having much slower recovery kinetics. A likely possibility is that the very abundant Galpha(o) is normally used but, when absent, can readily be replaced by G proteins with different properties.  (+info)

Possible role of immune surveillance at the initial phase of metastasis produced by B16BL6 melanoma cells. (5/208)

The relationship among the real-time trafficking of lung metastatic B16BL6 cells, metastatic potential, and the injected number of the cells was examined, since the smaller the number of tumor cells injected, the more clearly the immune defense may be observed. When 1x10(6) or 1x10(5) B16BL6 cells were injected into mice via the tail vein, both numbers of cells accumulated in the lung at a similar rate: there was an approximately 10-fold difference in the number of accumulated cells between the two doses. Elimination from the lung was not dependent on the cell number but on the proportion of accumulated cells. However, the injection of 1x10(4) cells resulted in lung accumulation less than one-tenth of that obtained with 1x10(5) cell injection. Metastasis was observed when 1x10(5) or 1x10(6) B16BL6 cells were injected, but not after injection of 1x10(4) cells. To clarify the roles of the immune defense system at the initial phase of metastasis, we challenged macrophage-depleted mice with 1x10(4) tumor cells. Treatment of mice with 2-chloroadenosine prior to the tumor cell challenge cancelled the suppression of not only metastasis but also the lung accumulation. Furthermore, the administration of 2-chloroadenosine following the tumor cell challenge had little effect on the metastatic potential. These results suggest that the immune surveillance whose action was obvious at the low dose of challenged tumor cells functions strongly at the initial phase but not at the advanced stages of the metastatic process, and that macrophages play an important role in the suppression of metastasis.  (+info)

Adenosine A(2A) and A(2B) receptors in cultured human and porcine coronary artery endothelial cells. (6/208)

We investigated the role of the cAMP link to the signal transduction mechanism coupled with adenosine A(2A) and A(2B) receptors in cultured human coronary artery endothelial cells (HCAEC) and porcine coronary artery endothelial cells (PCAEC). 2-[4-[2- inverted question mark2-[(4-aminophenyl)methylcarbonylamino]ethylaminocarbon yl inverted question marketh yl]phenyl]ethylamino-5'- ethylcarboxamidoadenosine ((125)I-PAPA-APEC) (PAPA-APEC) was used to demonstrate the specific binding in PCAEC membranes. The specific binding was saturable and reversible with a maximal number of binding sites (B(max)) of 240 fmol/mg protein, and scatchard analysis revealed a single class of binding site with an equilibrium dissociation constant (K(d)) of 1. 17 +/- 0.035 nM. In competition experiments, adenosine receptor agonists showed the following order of potency (based on IC(50)): 5'-(N-ethylcarboxamido)adenosine (NECA) >/= CGS-21680 > 2-chloroadenosine. This order appears to be consistent with the A(2) adenosine receptor classification. We also studied the effects of adenosine agonists on the accumulation of cAMP as an indirect approach to show the presence of functional A(2) receptors. Similarly, the same adenosine agonists (10(-7)-10(-4) M) elicited the production of cAMP in intact endothelial cells in a dose-dependent manner, exhibiting consistently with the A(2) adenosine receptor classification. A selective A(2A) adenosine receptor antagonist (ZM-241385, 10(-8) M) significantly inhibited the effect of CGS-21680 on cAMP but only partly inhibited the effect of NECA, suggesting the presence of both A(2A) and A(2B) receptors. Western blot analysis further showed the immunoreactivity of A(2A) and A(2B) receptor at 45 and 36 kDa, respectively, in both HCAEC and PCAEC. Direct evidence for the presence of A(2A) and A(2B) receptors in cultured HCAEC and PCAEC by reverse transcription-polymerase chain reaction (RT-PCR), revealed expected PCR product sizes (205 and 173 bp) for A(2A) and A(2B) receptors in HCAEC and PCAEC, respectively. The data show that adenylate cyclase-coupled adenosine A(2A) and A(2B) receptors are present in coronary endothelial cells.  (+info)

Selective transport of adenosine into porcine coronary smooth muscle. (7/208)

Adenosine (ADO), an endogenous regulator of coronary vascular tone, enhances vasorelaxation in the presence of nucleoside transport inhibitors such as dipyridamole. We tested the hypothesis that coronary smooth muscle (CSM) contains a high-affinity transporter for ADO. ADO-mediated relaxation of isolated large and small porcine coronary artery rings was enhanced 12-fold and 3.4-fold, respectively, by the transport inhibitor, S-(4-nitrobenzyl)-6-thioinosine (NBTI). Enhanced relaxation was independent of endothelium and was selective for ADO over synthetic analogs. Uptake of [(3)H]ADO into freshly dissociated CSM cells or endothelium-denuded rings was linear and concentration dependent. Kinetic analysis yielded a maximum uptake (V(max)) of 67 +/- 7.0 pmol. mg protein(-1). min(-1) and a Michaelis constant (K(m)) of 10. 5 +/- 5.8 microM in isolated cells and a V(max) of 5.1 +/- 0.5 pmol. min(-1). mg wet wt(-1) and a K(m) of 17.6 +/- 2.6 microM in intact rings. NBTI inhibited transport into small arteries (IC(50) = 42 nM) and cells. Analyses of extracellular space and diffusion kinetics using [(3)H]sucrose indicate the V(max) and K(m) for ADO transport are sufficient to clear a significant amount of extracellular adenosine. These data indicate CSM possess a high-affinity nucleoside transporter and that the activity of this transporter is sufficient to modulate ADO sensitivity of large and small coronary arteries.  (+info)

A1 adenosine receptors inhibit multiple voltage-gated Ca2+ channel subtypes in acutely isolated rat basolateral amygdala neurons. (8/208)

1. The anticonvulsant properties of 2-chloroadenosine (CADO) in the basolateral amygdala rely on the activation of adenosine-specific heptahelical receptors. We have utilized whole-cell voltage-clamp electrophysiology to examine the modulatory effects of CADO and other adenosine receptor agonists on voltage-gated calcium channels in dissociated basolateral amygdala neurons. 2. CADO, adenosine, and the A1 subtype-selective agonists N6-(L-2-Phenylisopropyl)adenosine (R-PIA) and 2-chloro-N6-cyclopentyladenosine (CCPA) reversibly modulated whole cell Ba2+ currents in a concentration-dependent fashion. CADO inhibition of barium currents was also sensitive to the A1 antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX). 3. The A2A-selective agonist 4-[2-[[6-Amino-9-(N-ethyl-beta-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl ]benzenepropanoic acid (CGS21680) was without effect. 4. CADO inhibition was predominantly voltage-dependent and sensitive to the sulphydryl-modifying reagent N:-ethylmaleimide, implicating a membrane-delimited, G(i/o)-coupled signal transduction pathway in the channel regulation. 5. Using Ca2+ channel subtype-selective antagonists, CADO inhibition appeared to target multiple channel subtypes, with the inhibition of omega-conotoxin GVIA-sensitive calcium channels being more prominent. 6. Our results indicate that the anti-convulsant effects CADO in the basolateral amygdala may be mediated, in part, by the A1 receptor-dependent inhibition of voltage gated calcium channels.  (+info)

The nucleoside analogues 8-amino-adenosine and 8-chloro-adenosine have been investigated in the context of B-lineage lymphoid malignancies by our laboratories because of the selective cytotoxicity they exhibit toward multiple myeloma (MM), chronic lymphocytic leukemia (CLL), and mantle cell lymphoma (MCL) cell lines and primary cells. personal of seven exclusive genes including which encodes the rate-determining enzyme from the pentose phosphate pathway (PPP), blood sugar-6-phosphate dehydrogenase. Bioinformatic evaluation of major cell gene manifestation data proven that G6PD is generally overexpressed in CLL and MM, highlighting the clinical implications of the finding. Using the combined resistant and delicate MM and MCL cell lines like a model program, we continue to show through loss-of-function and gain-of-function research that raised G6PD manifestation is necessary to keep up level of resistance to 8-amino- and 8-chloro-adenosine but inadequate to induce level of resistance in delicate ...
TY - GEN. T1 - 2-Chloroadenosine prevents inhibition of H+-coupled dipeptide transport by E.coli STa enterotoxin in Caco-2 epithelia.. AU - Marsh, Susan E.. AU - McEwan, Gordon T.A.. PY - 2000. Y1 - 2000. M3 - Conference contribution. VL - 528P. SP - 92P. BT - Journal of Physiology. ER - ...
The involvement of a guanine-nucleotide-binding regulatory protein (G protein) in the relaxing responses to adenosine receptor agonists was investigated in bovine coronary vessels. Ring segments of left anterior descending artery branches were suspended in organ baths for measurement of isometric tension. The adenosine analogs, 5-N-ethylcarboxamidoadenosine (NECA) and 2-chloroadenosine (CAD) caused concentration-dependent relaxations of coronary rings contracted with KCl. The relaxing effects of NECA and CAD were antagonized by the adenosine receptor antagonist 8-phenyltheophylline indicating the involvement of an adenosine receptor. In a separate series of experiments, incubation with cholera toxin inhibited the relaxing responses to NECA, CAD and isoproterenol but not those produced by sodium nitroprusside. Treatment with forskolin did not reduce the relaxing responses to NECA or CAD. N-ethylmaleimide and NaF/AlCl3 caused significant inhibition of the relaxations produced by both NECA and ...
BACKGROUND: Epidermal keratinocytes continuously proliferate and differentiate to form the mechanical and water permeability barrier that makes terrestrial life possible. In certain skin diseases, these processes become dysregulated, resulting in abnormal barrier formation. In particular, skin diseases such as psoriasis, actinic keratosis and basal and squamous cell carcinomas are characterized by hyperproliferation and aberrant or absent differentiation of epidermal keratinocytes. We previously demonstrated that 8-Cl-adenosine (8-Cl-Ado) can induce keratinocyte growth arrest without inducing differentiation. RESULTS: To determine if this agent might be useful in treating hyperproliferative skin disorders, we investigated whether 8-Cl-Ado could enhance the ability of 1,25-dihydroxyvitamin D3 [1,25(OH)2D3], a known keratinocyte differentiating agent and a clinical treatment for psoriasis, to inhibit keratinocyte growth. We found that low concentrations of 8-Cl-Ado and 1,25(OH)2D3 appeared to act ...
Treatment, Adenosine, Nitric Oxide, Pressure, Cardiomyocyte, Cardiomyocytes, Hypertrophy, Mice, Phenylephrine, Role, Cell, Blood, Exercise, Heart, Heart Failure, Hearts, Myocardium, Oxygen, Time, 2-chloroadenosine
8-Chloroadenosine is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP, which incorporates into RNA during transcription and inhibits RNA synthesis and exhibits cytotoxicity in MM.1S, RPMI-8226 and U266 cancer cell lines; induces G2/M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. Learn More ...
Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.. ...
The AQHA will require a five panel test for all breeding stallions for 2015. The panel includes testing for GBED (glycogen branching enzyme deficiency), HERDA (hereditary equine regional dermal
Deliberate hypotension is defined as lowering the systolic blood pressure to 80-90mmHg, or the mean blood pressure to 50-65mmHg. This technique is usually employed for operations that have a high risk of intraoperative hemorrhage, such as orthognathic surgery. Several different regimens are used to lower the patients blood pressure, such as vasodilators, autonomic nervous system inhibitors, opioids and inhalation anesthetics. However, the effects that these agents have on the QTc and Tp-e intervals during deliberate hypotension is not known. Virtually every kind of anesthetic is reported to have some effect on the QTc and Tp-e intervals. Because orthognathic surgery usually takes 3-4 hours to complete, the amount of anesthetics and drugs used to maintain low blood pressure is not small. Therefore, the effect that these agents may have on the QTc and Tp-e intervals may not be negligible. The investigators of the present study found that the high dose of commonly used hypotensive agents tend to ...
Cyclic 3, 5-[14C]AMP was measured in platelets that had first been incubated with [14C]adenine. Maximum increases of 2-4-fold were observed 0.5 min after addition of 10-40 µM adenosine. Smaller increases were obtained with higher concentrations of adenosine. In 0.5-min incubations 2-chloroadenosine was less effective than adenosine at concentrations below 20 µM and more effective at concentrations above 100 µM. Incorporation of 1-10 µM adenosine into platelets was inhibited at least 96% by p-nitrobenzylthioguanosine without any effect on the increase in cyclic [14C]AMP caused by these concentrations of adenosine, suggesting that adenosine acts at an extracellular site. With higher adenosine concentrations, p-nitrobenzylthioguanosine was less effective in inhibiting incorporation of adenosine but blocked the decline in cyclic [14C]AMP levels observed on increasing the adenosine concentration above 40 µM. This inhibitory effect of high adenosine concentrations on the accumulation of cyclic ...
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Eczema symptoms is noticed in diverse forms in different individual from dry itchy skin, skin eruptions, darkening of the skin, scaling and more.
TY - JOUR. T1 - Determination of adenosine effects and adenosine receptors in murine corpus cavernosum. AU - Tostes, Rita C.. AU - Giachini, Fernanda R.C.. AU - Carneiro, Fernando S.. AU - Leite, Romulo. AU - Inscho, Edward W.. AU - Webb, R. Clinton. PY - 2007/8. Y1 - 2007/8. N2 - This study tested the hypothesis that adenosine, in murine corpora cavernosa, produces direct relaxation of smooth muscle cells and inhibition of contractile responses mediated by sympathetic nerve stimulation. Penes were excised from anesthetized male C57BL/6 mice, dissected, and cavernosal strips were mounted to record isometric force. Adenosine, 2-chloroadenosine (stable analog of adenosine), and 2-phenylaminoadenosine (CV1808) (A2 A/A2B agonist) produced concentration-dependent relaxations of phenylephrine-contracted tissues. Relaxation to 2-chloroadenosine was inhibited, in a concentration-dependent manner, by 2-(2-furanyl)-7-(2- phenylethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine (SCH58261; A2A ...
TY - CHAP. T1 - Human erythrocytes. T2 - a possible tool for identification of adenosine analogs of chemotherapeutic potential. AU - Agarwal, R. P.. AU - Crabtree, G. W.. AU - Agarwal, K. C.. PY - 1976/12/1. Y1 - 1976/12/1. UR - http://www.scopus.com/inward/record.url?scp=0017161126&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0017161126&partnerID=8YFLogxK. M3 - Chapter. AN - SCOPUS:0017161126. VL - vol.17. BT - Proceedings of the American Association for Cancer Research. ER - ...
Rep. Anthony Weiner (D-N.Y.) pauses during a news conference in New York on Monday, after acknowledging inappropriate online communications with women ...
It started with ringing in her ears that got progressively worse. Then, Cheryl Cado started losing her balance. She was worried. The treatment her
Revitalize and illuminate your skin with the phytonutrient-rich Perricone MD Chloro Plasma Purifying Mask, an ultra-effective anti-ageing treatment mask. Space NK
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Minuzzo-Hartmann, Renata et al. Effect of glutamine on liver injuries induced by intestinal ischemia-reperfusion in rats. Nutr. Hosp., June 2017, vol.34, no.3, p.540-547. ISSN 0212- ...
OBJECTIVE: Adenosine deaminase (ADA) may be multifunctional, regulating adenosine levels and adenosine receptor (AR) agonism, and potentially modifying AR functionality. Herein we assess effects of ADA (and A(1)AR) deficiency on AR-mediated responses and ischaemic tolerance. METHODS: Normoxic function and responses to 20 or 25min ischaemia and 45min reperfusion were studied in isolated hearts from wild-type mice and from mice deficient in ADA and/or A(1)ARs. RESULTS: Neither ADA or A(1)AR deficiency significantly modified basal contractility, although ADA deficiency reduced resting heart rate (an effect abrogated by A(1)AR deficiency). Bradycardia and vasodilation in response to AR agonism (2-chloroadenosine) were unaltered by ADA deficiency, while A(1)AR deficiency eliminated the heart rate response. Adenosine efflux increased 10- to 20-fold with ADA deficiency (at the expense of inosine). Deletion of ADA improved outcome from 25min ischaemia, reducing ventricular diastolic pressure (by 45%; ...
1. Noradrenaline and histamine, when added to superfused guinea-pig cerebral-cortical tissues, increased both cyclic AMP-dependent and -independent histone kinase activities of some, but not of all, subsequently isolated subcellular fractions, and decreased their cyclic [3H]AMP-binding capacity, which was concluded to be due to an increase in endogenously bound cyclic AMP. 2. Adenosine and 2-chloroadenosine also diminished the cyclic [3H]AMP-binding capacities, but did not affect the histone kinase activities. 3. DEAE-cellulose chromatography and stability to KCl additions showed that the greater part of the histone kinase of the present preparations corresponded to the type II enzyme [of Corbin, Keely & Park (1975) J. Biol. Chem. 250, 218-225], with a lesser amount of type I activity. Different sites of cyclic AMP accumulation in relation to these or other kinases are considered in interpreting the differential tissue responses to the neurohumoural agents examined.. ...
Rat islets were used to compare the mechanisms whereby adenosine and adrenaline inhibit insulin release. Adenosine (1 microM-2.5 mM) and its analogue N6(-)-phenylisopropyladenosine (L-PIA) (1 nM-10 microM) caused a concentration-dependent but incomplete (45-60%) inhibition of glucose-stimulated release. L-PIA was more potent than D-PIA [the N6(+) analogue], but much less than adrenaline, which caused nearly complete inhibition (85% at 0.1 microM). 8-Phenyltheophylline prevented the inhibitory effect of L-PIA and 50 microM-adenosine, but not that of 500 microM-adenosine or of adrenaline. In contrast, yohimbine selectively prevented the inhibition by adrenaline. Adenosine and L-PIA thus appear to exert their effects by activating membrane A1 receptors, whereas adrenaline acts on alpha 2-adrenergic receptors. Adenosine, L-PIA and adrenaline slightly inhibited 45Ca2+ efflux, 86Rb+ efflux and 45Ca2+ influx in glucose-stimulated islets. The inhibition of insulin release by adenosine or L-PIA was ...
Adenosine kinase inhibitors. 4. 6,8-Disubstituted purine nucleoside derivatives. Synthesis, conformation, and enzyme inhibition.: 6,8-Disubstituted purine nucle
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Rep. Joe Crowley (D-N.Y.), chairman of the House Democratic Caucus, is the highest ranking Democrat to call for Frankens resignation.
Sen. Byron Dorgan (D-N.D.) this week offered legislation identical to the V-chip bill sponsored in the House by Rep. Ed Markey (D-Mass.).
Sen. Kirsten Gillibrand, D-N.Y., added $1.6 million to her campaign warchest during the first three months of this year - marking nearly $9 million raised since the former lawmaker was sworn into the … ...
U.S. Rep. Annie Kuster, D-N.H., and Rep. Bruce Westerman, R-Airzona, sent a bipartisan letter of support for biomass power to the U.S. EPA.
Sen. Jeanne Shaheen, D-N.H., has put forth a bipartisan bill that would give small-forest owners incentives to manage their land to store more carbon, the latest legislative effort to help curb global warming.
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TY - JOUR. T1 - Alterations in cyclic AMP generation and G protein subunits following transient ischemia in gerbil hippocampus. AU - Suyama, Kazuhiko. AU - Saito, Kuniaki. AU - Chen, Guang. AU - Pan, Bai Shen. AU - Manji, Husseini K.. AU - Potter, William Z.. PY - 1995. Y1 - 1995. N2 - We examined alterations in the cyclic AMP generating system and G protein subunits in gerbil hippocampus following 10 min of transient ischemia. In hippocampal slices, basal and isoproterenol- and forskolin-stimulated cyclic AMP accumulations were markedly increased at 6 and 24 h after ischemia. Interestingly, both the inhibition of forskolin-stimulated cyclic AMP and the potentiation of β-adrenoceptor-stimulated cyclic AMP by a γ-aminobutyric acid(B) receptor agonist were attenuated at these time points. Ischemia did not affect the immunolabeling of any of the G protein α subunits; only that of β subunits was significantly decreased, by 28.2%, 4 days after ischemia. In contrast, pertussis toxin-catalyzed ...
Looking for online definition of L-PIA or what L-PIA stands for? L-PIA is listed in the Worlds largest and most authoritative dictionary database of abbreviations and acronyms
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TY - JOUR. T1 - Outcome of pediatric patients with Langerhans cell histiocytosis treated with 2 chlorodeoxyadenosine. T2 - A nationwide survey in Japan. AU - Imamura, Toshihiko. AU - Sato, Takashi. AU - Shiota, Yoko. AU - Kanegane, Hirokazu. AU - Kudo, Kazuko. AU - Nakagawa, Shinichirou. AU - Nakadate, Hisaya. AU - Tauchi, Hisamichi. AU - Kamizono, Junji. AU - Morimoto, Akira. PY - 2010/5. Y1 - 2010/5. N2 - The aim of this study was to assess the outcome of treatment with 2-chlorodeoxyadenosine (2-CdA) in pediatric patients with Langerhans cell histiocytosis (LCH) in Japan. We retrospectively identified 17 pediatric LCH patients treated with 2-CdA. All patients were refractory or reactivated cases who had been initially treated according to the JLSG-02 protocol of the Japan LCH study group. At initiation of 2-CdA therapy, 4 patients had primary refractory multisystem (MS) disease with risk organ (RO) involvement (MS?), 9 patients had reactivated MS disease [5 MS+ and 4 without RO involvement ...
Afferent chemoreceptor activity was recorded from the peripheral cut end of the carotid sinus nerve in pentobarbitone anaesthetized cats. The effects of purines, peptides and ouabain on chemosensory activity were studied. Purines. It was found that intracarotid injections of adenosine: AMP; ADP; ATP; CoA;Me-adenosine analogues: N6-methyladenosine, 2-chloroadenosine, 3-deoxyudenosine but not 2-deoxyadenosine; cyclic AMP; dibutyryl cyclic AMP increased spontaneous chemoreceptor discharge. The ATP analogues, a-5- methylene ATP decreased spontaneous chemoreceptor discharge, whereas the f-y-methylene ATP caused a slight increase in discharge. Adenine and the purine nucleosides inosine and guanosine had little or no effect on the discharge. The pyrimidine nucleosides cytidine and uridine were also studied and had little or no effect on spontaneous chemoreceptor discharge. Intracarotid injection of theophylline transiently depressed spontaneous chemosensory activity and potentiated the action of ...
The initial therapies of choice for hairy cell leukemia are either cladribine (2-chlorodeoxyadenosine, 2-CdA) or pentostatin. [1] [2] These drugs have comparable response rates but have not been compared in phase III trials. Cladribine is administered as a one-time continuous infusion or series of subcutaneous injections and is associated with a high rate of febrile neutropenia. [3] [4] [5] [6] Rarely, more than one course of treatment is required to induce a desirable response. Treatment should be discontinued once complete remission or stable partial remission with normalization of peripheral blood counts is reached. The presence of residual disease may be predictive of relapse but does not seem to affect survival. [5] [7] The role of consolidation or maintenance therapy in preventing relapse or progression of the disease after treatment with purine analogs has not been evaluated and remains unproven. Pentostatin is administered intermittently for a longer time but may result in a lower ...
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Garcetti spoke Tuesday at the Center for American Progress Ideas Conference in Washington at a time when many Democrats are trying to determine whats next for their party after unexpected electoral losses in November. The conference is seen by many as an early cattle call of potential 2020 presidential candidates. Garcetti, who was just reelected to a second term, and others whove been floated as possible candidates are participating in the daylong event - including Sens. Kamala Harris (D-Calif.), Amy Klobuchar (D-Minn.), Elizabeth Warren (D-Mass.) and Cory Booker (D-N.J.).. ...
Rep. Alexandria Ocasio-Cortez, D-N.Y., stunned the political world last year when she pulled off an upset victory against a 10-term incumbent who held a leadership position in the Democratic caucus. Now candidates are looking to replicate some of her tactics to take on Democratic incumbents across the
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Charousová, Ivana; Javoreková, Soňa; Wink, Joachim (2 February 2015). "Isolation and characterization of Streptomyces ... Streptomyces rishiriensis produces coumermycin A1, notomycin, 2-chloroadenosine, phosphophenylalanarginine and lactonamycin. ...
2-chloroadenosine MeSH D13.570.583.138.300.200 - cladribine MeSH D13.570.583.138.325 - deoxyadenosines MeSH D13.570.583.138. ... 2-chloroadenosine MeSH D13.570.800.096.300.200 - cladribine MeSH D13.570.800.096.500 - isopentenyladenosine MeSH D13.570. ...
Buy 2-Chloroadenosine (CADO) (CAS 146-77-0), an adenosine receptor agonist. Join researchers using high quality 2- ... Effect of intraperitoneal and intrahippocampal (CA1) 2-chloroadenosine in amygdaloid kindled rats.. Brain Res 751:259-64 (1997 ...
2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a ...
... chloroadenosine with staurosporine, a cell cycle checkpoint dysregulator, enhances the killing potential of the antineoplastic ... chloroadenosine with staurosporine, a cell cycle checkpoint dysregulator, enhances the killing potential of the antineoplastic ... Abstract: 2-Chloroadenosine is an adenosine analog capable of inducing apoptosis in several cell lines by acting either via ... Cytostatic Effect of the Nucleoside Analogue 2-Chloroadenosine on Human Prostate Cancer Cell Line. Author(s): Ilaria Bellezza, ...
2-chloroadenosine-5-triphosphate ligand page. Quantitative data and detailed annnotation of the targets of licensed and ...
2-chloroadenosine-5-triphosphate ligand page. Quantitative data and detailed annnotation of the targets of licensed and ... 2R,3S,4R,5R)-5-(6-amino-2-chloropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl (hydroxy-phosphonooxyphosphoryl) hydrogen phosphate ...
8-Chloro-Adenosine in Chronic Lymphocytic Leukemia. The safety and scientific validity of this study is the responsibility of ... 8-Chloro-adenosine is a new drug similar to other drugs already approved by the FDA for the treatment of CLL and other types of ... 8-Chloro-adenosine is not approved by the FDA and is not commercially available. A total of up to 28 patients will take part in ... Experimental: 8-Chloro-Adenosine Starting dose for first cohort of patients 45 mg/m2 intravenous over 1 hr daily for 5 days ...
|p|Agonists are substances that activate cellular receptor molecules to which they attach. In a nutshell, agonists bind to cellular receptors and elicit a biological response. The agonists enhance the signal transduction by binding to the receptor in cellular systems. They can be full agonists, activating the receptor to maximal activity, or partial agonists. There are also inverse agonists. These ligands bind receptors and cause the reverse biological response of the natural ligand. Alfa Aesar supplies receptor agonists for many different cellular protein receptors. These reagents include both natural receptor ligands as well as synthetic agonists. In addition, the conformational changes brought about by the agonists activate or increase the activation of secondary intracellular messenger.|/p|
2-Chloroadenosine prevents inhibition of H+-coupled dipeptide transport by E.coli STa enterotoxin in Caco-2 epithelia. In ... 2-Chloroadenosine prevents inhibition of H+-coupled dipeptide transport by E.coli STa enterotoxin in Caco-2 epithelia. / Marsh ... Marsh, S. E., & McEwan, G. T. A. (2000). 2-Chloroadenosine prevents inhibition of H+-coupled dipeptide transport by E.coli STa ... Marsh, Susan E. ; McEwan, Gordon T.A. / 2-Chloroadenosine prevents inhibition of H+-coupled dipeptide transport by E.coli STa ...
We investigated the ability of adenosine and its stable analogue 2-chloroadenosine (CADO) to inhibit cytokine production and ...
InChI=1S/C10H12ClN5O4/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(19)5(18)3(1-17)20-9/h2-3,5-6,9,17-19H,1H2,(H2,12,14,15) ... Other names: Cl AS; 2 ClAdo; 2-Chloroadenosine; Cl-Ado; 2-chloroadenosinehemihydrate ... Adenosine, 2-chloro-. *Formula: C10H12ClN5O4 ...
2⇓B), although mast cell-derived TNF-α has been demonstrated to be at the center in the OVA-induced asthma model (30, 31). ... 2⇓A). IL-17 expression of the macrophages stimulated by mast cell-derived mediator(s) was not affected by blocking TNF-α (Fig. ... 2⇓A). However, the direct stimulation of macrophages with OVA/IgE or with the supernatant from control mast cells did not ... 2⇓B). These data indicate that OVA/IgE-activated mast cells release mediator(s) to induce IL-17 expression in alveolar ...
INHIBITION BY SK-AND-F-96365 OF CA2+ CURRENT, IL-2 PRODUCTION AND ACTIVATION IN T-LYMPHOCYTES BRITISH JOURNAL OF PHARMACOLOGY ... INTERLEUKIN-2 TRANSCRIPTIONAL BLOCK BY MULTIFUNCTIONAL CA2+/CALMODULIN KINASE NATURE Nghiem, P., OLLICK, T., Gardner, P., ... Secretion of interferon-gamma, IL-2, and IL-4 was comparable in CF and control TCC after both forms of activation, while IL-5 ... 2. SK&F 96365 also inhibits [3H]-thymidine incorporation and interleukin-2 (IL-2) synthesis in peripheral blood lymphocytes. 3 ...
D-Ala2,D-Leu5]-enkephalin, which decreased cyclic AMP levels and reversed the 2-chloroadenosine-stimulated phosphorylation of ... NCB-20 cells were labeled with [32P]orthophosphate under conditions where 2-chloroadenosine gave maximum increases of 32P ...
2. [3H]cAMP accumulation in response to 2C-CPA (a and b) and AAC (c and d) in the absence and presence of DPCPX in CHO-A1-CRE- ... 2; Table 2), and all of these responses were inhibited by DPCPX to yield comparable log KD values (Fig. 2; Table 3). However, ... TABLE 2 Log IC50 values (without PTX) and log EC50 values (following preincubation with PTX) for A1-agonist-induced changes in ... For the Gi efficacy estimates, the KD values were obtained from inhibition of [3H]DPCPX binding (see Table 1, column 2), and ...
Adenosine exerts multiple functions through activation of individual adenosine receptor subtypes.2-5 A1 receptors (A1R) and A3 ... Our finding that A3R KO attenuated the TAC-induced increase of COX-2 and tended to decrease TNF-α after TAC supports a role for ... Male C57BL/6 (Taconic, Germantown, NY) body weight-matched A3R KO mice2 (crossed back to Taconic C57BL/6 mice at least 16 times ... However, the A3R agonist 2-chloro-N6-(3-iodobenzyl)adenosine-5′-N-methylcarboxamide (Cl-IB-MECA) or adenosine dose- and time- ...
Charousová, Ivana; Javoreková, Soňa; Wink, Joachim (2 February 2015). "Isolation and characterization of Streptomyces ... Streptomyces rishiriensis produces coumermycin A1, notomycin, 2-chloroadenosine, phosphophenylalanarginine and lactonamycin. ...
SRIF is labile in the medium, with a half-life of about 2 h during culture incubation. SRIF did not disturb the insulin binding ... Prostaglandin E2, 2-chloroadenosine, and isoproterenol increased short-circuit current (Isc) and the rate of Na+ absorption. In ... We have used a genomic Ig gamma 1 probe which detects polymorphisms in the gamma 1, gamma 2, gamma 3 and pseudogamma genes to ... Release remained impaired with retinoic acid (RA) repletion, 2 micrograms/g diet compared to release from islets of rats ...
Ceyla Konca 1 , Zübeyde N Özkurt 2 , Müge Deger 3 , Zeynep Akı 2 , Münci Yağcı 2 ... Ceyla Konca 1 , Zübeyde N Özkurt 2 , Müge Deger 3 , Zeynep Akı 2 , Münci Yağcı 2 ... Extranodal Multifocal Rosai-Dorfman Disease: Response to 2-chlorodeoxyadenosine Treatment Ceyla Konca et al. Int J Hematol. Jan ... Haematologica 105 (2), 348-357. 2020. PMID 31004029. Rosai-Dorfman disease is a rare subtype of non-Langerhans cell ...
It was found that intracarotid injections of adenosine: AMP; ADP; ATP; CoA;Me-adenosine analogues: N6-methyladenosine, 2- ... chloroadenosine, 3-deoxyudenosine but not 2-deoxyadenosine; cyclic AMP; dibutyryl cyclic AMP increased spontaneous ...
2. ROS Balance in Cancer Cells. One of the main features of cancer cells, when compared to the normal ones, is a persistent pro ... Protoc. 2007, 2, 2719-2727. [Google Scholar] [CrossRef]. *Lo, J.F.; Wang, H.F.; Tam, M.F.; Lee, T.C. Glutathione S-transferase ... Figure 2. The role of quercetin in the metabolism of ROS in cancer cells. Reactive oxygen species (ROS) are continuously ... Figure 2. The role of quercetin in the metabolism of ROS in cancer cells. Reactive oxygen species (ROS) are continuously ...
2A). Fig. 2 B and C shows examples of PMN, MΦ, and NK surrounding S180 in rosettes. In contrast, CD8+ and CD4+ T cells and ... Tumor volume (V) was calculated by using the formula V = (W× W× L)/2, where W was the shorter of the two diameters and L was ... 2. Formation of leukocyte rosettes during the killing of cancer cells in SR/CR mice. SR/CR mice were challenged i.p. with 107 ... For PMN depletion, three i.p. injections of 500 μg of anti-Ly6G (10) were given to each SR/CR mouse at 2-day intervals. For NK ...
Dora, E., 1985c, Effect of adenosine and its stabile analogue 2-chloroadenosine on cerebrocortical microcirculation and NAD/ ...
a href=/no_cache/products/eshop/product/C_028/,C 028,/a,), Clofarabine, 2-Cl-cAMP (Cat. No. ,a href=/no_cache/products/eshop ... C_020/,C 020,/a,) and 2- chloroadenosine (Cat. No. ,a hre ... chloroadenosine (Cat. No. C 017), respectively. Detailed ... 2. Bontemps F., Delacauw A., Cardoen S., Van Den Neste E.Van den Berghe G., Biochem Pharmacol., 59, 1237 - 1243 (2000), " ... C 028), Clofarabine, 2-Cl-cAMP (Cat. No. C 020) and 2- ... "Metabolism and cytotoxic effects of 2-chloroadenine, the major ...
Putative kappa-2 Opioid Agonists Are Antihyperalgesic in a Rat Model of Inflammation Janice Ho, Andrew J. Mannes, Ronald Dubner ... Somatostatin Inhibition of Acid and Histamine Release by Activation of Somatostatin Receptor Subtype 2 Receptors in Rats K. ... Identification of Insulin-Like Growth Factor Binding Protein-2 as a Biochemical Surrogate Marker for the in Vivo Effects of ... In Vivo Evidence for Carrier-Mediated Efflux Transport of 3′-Azido-3′-Deoxythymidine and 2′,3′-Dideoxyinosine Across the Blood- ...
... chloroadenosine to rat brain cortical membranes. Can. J. Physiol. Pharmacol. 58, 576-579 (1980).CrossRefPubMedGoogle Scholar ... Williams, M., Risley, E.A.: Biochemical characterization of putative purinergic receptors by using 2-chloro[3H]adenosine, a ... Wu, P. H., Phillis, J. W., Balls, K., Rinaldi, B.: Specific binding of 2-[3H] ...
2: Metabolic perturbation on de novo purine synthesis leads to BRD4 inhibition.. ... The log2 fold change of the RFP intensity was normalized with cells cultured in medium supplemented with 10% FBS. Mean ± s.d., ... The log2 fold change of metabolites level was calculated relatively to sgRen cells. AA, amino acids; NT, nucleotides; NB, ... 2 Generation of SLC nucleoside transporters knockout.. To generate the SLC knockout cells, we co-infected REDS cells with ...
The RNA-directed nucleoside analogue 8-chloro-adenosine is currently in phase I clinical trials and as high as 500 nmol/L ... Unique and promising RNA-directed treatments for myeloma are the nucleoside analogs 8-chloro-adenosine (currently in phase I ... 8-Chloro-adenosine has recently proved cytotoxic to breast cancer cells through depletion of cyclin E (11). However, no study ... The outcomes of 8-chloro-adenosine studies should help to pave the way for the consideration of 8-NH2-Ado as an agent to treat ...
LFS (2 Hz, 10 min) was applied at various times after LTP induction: A, 1 min after;C, 3 min after; or E, 10 min after.B, D, F ... Figure 2 summarizes experiments in which LFS was applied 1 (A, B), 3 (C, D) or 10 (E, F) min after the induction of LTP . As ... The composition of the ACSF solution was (in mm): NaCl 117, KCl 4.7, CaCl2 2.5, MgCl2 1.2, NaHCO3 25, NaH2PO4 1.2, and glucose ... C, A2 adenosine receptor antagonist DMPX (5 μm) does not affect the LFS-induced depotentiation. D, Pooled data from six ...
Epac1 and 2 are guanine nucleotide exchange factors for members of the Ras GTPase family, Rap1 and Rap2. These can activate an ... An endogenous A~2~B adenosine receptor coupled to cyclic AMP generation in human embryonic kidney (HEK 293) cells British ... The 2-chloroadenosine inhibition of histamine-induced inositol phosphates accumulation in mouse brain and calcium ions. British ... A(1) And A(2) Adenosine Receptor Modulation Of Contractility In The Cauda Epididymis Of The Guinea-Pig British Journal Of ...
  • We investigated the ability of adenosine and its stable analogue 2-chloroadenosine (CADO) to inhibit cytokine production and cytotoxic activity of lymphokine-activated killer (LAK) cells and determined whether both these effects are initiated via a common pathway. (nih.gov)
  • 6,7 Liao et al 8 demonstrated that the adenosine analogue 2-chloroadenosine (CADO) also attenuated pressure overload-induced LV hypertrophy through activation of the A 1 R. Similar to A 1 R, the A 3 R are Gi protein-coupled receptors that have been shown to activate similar downstream signaling pathways. (ahajournals.org)
  • 2 CADO, adenosine, and the A1 subtype-selective agonists N6-(L-2-Phenylisopropyl)adenosine (R- PIA) and 2-chloro-N6-cyclopentyladenosine (CCPA) reversibly modulated whole cell Ba2+ currents in a concentration-dependent fashion. (gotomydoctor.com)
  • 1991). However, direct regulation studies outlined below, infusion of the non-selective of postsynaptic processes by amygdala adenosine receptors adenosine receptor agonist 2-chloroadenosine (CADO) has not been examined. (gotomydoctor.com)
  • Each tissue specimen was randomly allocated to either control group or 2-chloroadenosine (CADO, 10 μM) group. (bvsalud.org)
  • 2-chloroadenosine (2-CAdo) is an adenosine deaminase-resistant analogue of adenosine, widely used as an adenosine receptor agonist. (courtfield.ml)
  • Antibodies of 2-Chloroadenosine (CADO) anti STAT3 (#9139), anti phospho-STAT3 at Con705 (#9145) or anti phospho-STAT3 at S727 (#94994) had been from Cell Signaling (Davers, MA). (unisoyazilim.com)
  • Gauge the absorbance using Multi-scan Move (Thermo 2-Chloroadenosine (CADO) Scientific) at 450nm with 620nm as research wavelength. (unisoyazilim.com)
  • On the other hand, cells had been stained with pI and examined by movement cytometry as previously referred 2-Chloroadenosine (CADO) to 31. (unisoyazilim.com)
  • Journal of Pharmacology and Experimental Therapeutics , 322 (2), 678-685. (elsevier.com)
  • The employment of the full agonist, 2-chloroadenosine, in flies mimicked in vivo the phenotype of DmAdoR over-expression, whereas the antagonist, SCH58261, rescued the flies from the lethality caused by DmAdoR over-expression. (gate2biotech.com)
  • The ADA-resistant, AR agonist 2-chloroadenosine (2-CA) (10 microM) potentiated I(GABA) run-down but only in approximately 20% of tested oocytes. (uniroma1.it)
  • 2. Adenosine and 2-chloroadenosine also diminished the cyclic [ 3 H]AMP-binding capacities, but did not affect the histone kinase activities. (biochemj.org)
  • Moreover, the pan-caspase inhibitor Z-VAD blocked the 8-NH 2 -Ado-induced MCF-7 cell death. (aacrjournals.org)
  • The selective caspase-2 inhibitor N-benzyloxy carbonyl-Val-Asp-Val-Ala-Asp-fmk significantly reduced both adenosine analogs-induced caspase-2 activation and the associated cell death. (unimi.it)
  • 1-32 Hz) of adrenergic nerves produced frequency-dependent contractions that were inhibited by compounds that increase adenosine levels, such as 5′-iodotubercidin (adenosine kinase inhibitor), erythro-9-(2-hydroxy-3- nonyl)adenine (adenosine deaminase inhibitor), and dipyridamole (inhibitor of adenosine transport). (elsevier.com)
  • Adenosine was from one to two orders of magnitude less potent than 2‐chloroadenosine as an inhibitor of this release. (northwestern.edu)
  • 2005). A Phase 1-2 clinical study of a second generation oral MEK inhibitor, PD0325901 in patients with advanced cancer. (pharmacologicalsciences.us)
  • 2-Chloroadenosine, acting as metabolic precursor of an S-phase specific nucleoside analogue in human prostate cancer PC3 cells, inhibited DNA synthesis so that the cell population accumulated in the S-phase. (eurekaselect.com)
  • In neonatal rat cardiomyocytes induced to hypertrophy with phenylephrine, the adenosine analogue 2-chloroadenosine reduced cell area, protein synthesis, atrial natriuretic peptide, and 3′-nitrotyrosine. (ahajournals.org)
  • Dora, E., 1985c, Effect of adenosine and its stabile analogue 2-chloroadenosine on cerebrocortical microcirculation and NAD/NADH redox state, Pflügers Arch. (springer.com)
  • 8-Amino-adenosine (8-NH 2 -Ado) is a ribose sugar nucleoside analogue that reduces cellular ATP levels and inhibits mRNA synthesis. (aacrjournals.org)
  • Borowicz KK, Luszczki J, Czuczwar SJ (2002) 2-Chloroadenosine, a preferential agonist of adenosine A1 receptors, enhances the anticonvulsant activity of carbamazepine and clonazepam in mice. (springer.com)
  • The anticonvulsant action of 2-ClAdo was reversed by pretreatment with theophylline. (oregonstate.edu)
  • This anticonvulsant action of 2-ClAdo and the proconvulsant effect of theophylline were observed with other chemoconvulsants such as bicuculline (BIC) and picrotoxinin (PTX). (oregonstate.edu)
  • The inability of theophylline to antagonize the anticonvulsant action of diazepam and pentobarbital demonstrates the selectivity of the anticonvulsant effect of 2-ClAdo. (oregonstate.edu)
  • 2-Chloroadenosine is an adenosine analog capable of inducing apoptosis in several cell lines by acting either via adenosine receptors or via uptake that is followed by metabolic transformations leading to nucleotide analogs. (eurekaselect.com)
  • Taken together, these observations suggest that the modulatory effect of adenine derivatives in the CNS depends on (1) the release of nucleotides and subsequent breakdown to A and (2) the presence of Al-adenosine receptors. (springer.com)
  • In the acid-secreting parietal cells of the gastric mucosa, the use of various radioligands for adenosine receptors suggested the presence of the A 2 adenosine receptor subtype(s) on the cell surface. (physiology.org)
  • 2] Interestingly, evidence is growing for a certain role of adenosine receptors in the field of oncology . (axonmedchem.com)
  • 2-Chloroadenosine (1-500 muM) and R-PIA (50 muM) , which are not substrates for either the nucleoside transporters or adenosine deaminase were inactive in the absence of calcium. (gla.ac.uk)
  • Effect of intraperitoneal and intrahippocampal (CA1) 2-chloroadenosine in amygdaloid kindled rats. (abcam.com)
  • Fig. 2: Metabolic perturbation on de novo purine synthesis leads to BRD4 inhibition. (nature.com)
  • In contrast, heroic doses of the A 2 selective ligand, 2-phenylaminoadenosine, afforded no protection against seizures. (elsevier.com)
  • Dose-response curves for R-phenylisopropyladenosine (PIA), cyclohexyladenosine (CHA), 2-chloroadenosine (2-ClAdo), Nethylcarboxamidoadenosine (NECA) and S-PIA were generated against PTZ seizure thresholds in the rat. (oregonstate.edu)
  • The adenosine agonists, 5'-N-(ethyl)carboxamido-adenosine (NECA), cyclohexyladenosine, cyclopentyladenosine, 2-chloroadenosine and R- and S-phenylisopropyladenosine (R- and S-PIA), protected animals against seizures in a dose-dependent, and extremely potent manner. (elsevier.com)
  • D-Ala2,D-Leu5]- enkephalin , which decreased cyclic AMP levels and reversed the 2-chloroadenosine-stimulated phosphorylation of tyrosine hydroxylase in differentiated PC12 cells, also reversed the stimulation of phosphorylation of the 90-kDa protein in NCB-20 cells. (curehunter.com)
  • However, this defect was not associated with an altered phosphorylation of the documented in vitro DUSP3 substrates, ERK1/2, JNK1/2 and EGFR but was associated with an increased PKC phosphorylation. (ac.be)
  • display that liver organ tumor cells show heterogeneous sensitivities to sorafenib induced cell loss of life also, which co-relates using the STAT3-Y705 phosphorylation amounts and JAK1/2 manifestation amounts in Hep3B, Huh7 and HepG2 cells. (unisoyazilim.com)
  • To examine possible metabolic adaptations to these elevated pressures, fresh blood samples from marine and terrestrial mammals were incubated for 2 h at 37 degrees C under 136 atm (2000 psi) of hydrostatic pressure. (saladgaffe.ml)
  • 2-Chloroadenosine prevents inhibition of H+-coupled dipeptide transport by E.coli STa enterotoxin in Caco-2 epithelia. (elsevier.com)
  • Inhibition of MDA-MB-231 cell autophagy, by reduction of ATG7 or 3-methyladenine treatment, did not block this 8-NH 2 -Ado-mediated cytotoxicity. (aacrjournals.org)
  • Klapstein, G.J. and Colmers, W.F. (1992) 4-Aminopyridine and low Ca++ differentiate presynaptic inhibition mediated by Neuropeptide Y, Baclofen and 2-Chloroadenosine in rat hippocampal CA1 in vitro. (tu.edu)
  • Activation and inhibition of blood platelet adenylate cyclase by adenosine or by 2-chloroadenosine. (pianolarge.ml)
  • BCL-2 inhibition through venetoclax (VEN) targets acute myeloid leukemia (AML) blast cells and leukemic stem cells (LSCs). (biomed.news)
  • 2-ClAdo-induced elevation of BIC seizure threshold was not antagonized by the benzodiazepine antagonists RO 15-1788 and CGS 8216, establishing the specificity of 2-ClAdo as an adenosine receptor agonist. (oregonstate.edu)
  • 10 -8 - 10 -6 M). The combination of both antagonists abrogated 2-chloroadenosine-induced relaxation. (elsevier.com)
  • Adenosine, 2-chloroadenosine (stable analog of adenosine), and 2-phenylaminoadenosine (CV1808) (A2 A /A2 B agonist) produced concentration-dependent relaxations of phenylephrine-contracted tissues. (elsevier.com)
  • Male C57BL/6 (Taconic, Germantown, NY) body weight-matched A 3 R KO mice 2 (crossed back to Taconic C57BL/6 mice at least 16 times), 8 to 12 weeks old, were used for TAC or control. (ahajournals.org)
  • The interactions of Nocardia asteroides GUH-2 with pulmonary epithelial cells of C57BL/6 mice and with HeLa cells were studied. (biomedsearch.com)
  • The cyclic AMP contents of slices incubated with or without adenosine and 2-chloroadenosine were determined in four cortical areas after electroencephalography and behavioral examination in cobalt-injected rats. (okayama-u.ac.jp)
  • Both the anticancer agent 2-chloro-2'-deoxy-adenosine (Cladribine) and its derivative 2-chloro-adenosine induce apoptosis of human astrocytoma cells (J Neurosci Res 60:388-400, 2000). (unimi.it)
  • 8-NH 2 -Ado induced apoptotic death of MCF-7 cells and apoptosis was not inhibited by knockdown of functional p53. (aacrjournals.org)
  • Barbieri D, Abbracchio MP, Salvioli S, Monti D, Cossarizza A, Ceruti S, Brambilla R, Cattabeni F, Jacobson KA, Franceschi C (1998) Apoptosis by 2-chloro-2′-deoxy-adenosine and 2-chloro-adenosine in human peripheral blood mononuclear cells. (springer.com)
  • During the induction of apoptosis, expression of Bcl-2, Bcl-xL and survivin was decreased, and that of p 53, Bad and Bax was increased. (wjgnet.com)
  • The modulation of expression of p 53 and Bcl-2 family proteins, and activation of Caspase-3 might be involved in the induction of apoptosis. (wjgnet.com)
  • We conclude that adenosine analogs induce the apoptosis of human astrocytoma cells by activating an atypical apoptotic cascade involving caspase-2 as an initiator caspase, and effector caspase-3. (unimi.it)
  • A key role for caspase-2 and caspase-3 in the apoptosis induced by 2-chloro-2'-deoxy-adenosine (cladribine) and 2-chloro-adenosine in human astrocytoma cells / S. Ceruti, E. Beltrami, P. Matarrese, A. Mazzola, F. Cattabeni, W. Malorni, M. P. Abbracchio. (unimi.it)
  • A strong synergism was observed for apoptosis induction through an increase in caspase-9 and caspase-3 activation and significantly decreased expression of the Bcl-xL Bcl-2 family member. (biomed.news)
  • Spontaneous regression/complete resistance (SR/CR) mice possess a unique autosomal dominant trait that allows them to survive challenges with aggressive mouse cancer cells at up to millions of times the lethal doses for WT mice ( 1 , 2 ). (pnas.org)
  • Klapstein, G.J. and Levine, M.S. (2005) Age-dependent biphasic changes in ischemic sensitivity in the striatum of Huntington's Disease R6/2 transgenic mice. (tu.edu)
  • Open up in another window Number 2 Contractile reactions to phenylephrine, alpha1-adrenergic receptor agonist, in cavernosal pieces from slim () and db/db () mice. (conferencedequebec.org)
  • Nevertheless, similar inhibitory ramifications of 5-iodotubercidin, dipyridamole, and C-8031 had been seen in the cavernosal pieces from slim and db/db mice, as well as the variations in the cavernosal contractile reactions between slim and db/db weren't abolished by these medicines (Number 1, Desk 2). (conferencedequebec.org)
  • I(GABA) run-down from wt mice was not affected by 2-CA, suggesting maximal ARs activity by endogenous adenosine. (uniroma1.it)
  • In mitochondria, superoxide anion (O 2 − ) can be dismutated to hydrogen peroxide (H 2 O 2 ) by two enzymes, namely copper-zinc superoxide dismutase (CuZnSOD) and manganese superoxide dismutase (MnSOD), that are present in the mitochondrial matrix and in the intermembrane space, respectively. (mdpi.com)
  • Once generated, H 2 O 2 can be quenched by GPx in mitochondria, or by catalase in the cytosol. (mdpi.com)
  • Th1 cytokine IFN-γ was thought to prevent this process ( 2 , 3 ), however, recent studies indicate that IFN-γ secreted by Th1 cells may cause severe airway inflammation under certain conditions ( 4 , 5 ). (jimmunol.org)
  • Regardless of the breast cancer subtype tested or the p53 status of the cells, 8-NH 2 -Ado was more cytotoxic than either gemcitabine or etoposide. (aacrjournals.org)
  • Importantly 8-NH 2 -Ado was highly cytotoxic to triple-negative breast cancer cells and worked through a pathway that did not require wild-type p53 for cytoxicity. (aacrjournals.org)
  • These effects are associated with an accumulation of 8-chloroadenosine triphosphate (8Cl-ATP), an effect not seen in experiments utilizing other chlorinated nucleosides. (ku.dk)
  • The cyclic AMP accumulation elicited by adenosine or 2-chloroadenosine was increased in the primary cortical area of cobalt-induced epilepsy, but in the other cortical areas there was no deviation in cyclic AMP accumulation. (okayama-u.ac.jp)
  • EXP BRAIN RES , 49 (2) 174 - 180. (ucl.ac.uk)
  • Transporter function was assessed by the site-specific binding of [ 3 H]NBMPR and the cellular uptake of [ 3 H]2-chloroadenosine. (aspetjournals.org)
  • S-(2-Hydroxy-5 nitrobenzy1)-6-thioinosine , an adenosine uptake blocker, at a concentration of 100 M-M had no effect on secondary potential size and did not restore adenosine sensitivity in calcium free medium. (gla.ac.uk)
  • Parathyroid hormone and 2‐chloroadenosine also stimulated preadipocyte adenylyl cyclase. (elsevier.com)
  • Comparison of 8 -chloroadenosine (NSC - 354258) and 8 - chloro - cyclic - AMP (NSC - 614491) toxic-ity in dogs. (pharmacologicalsciences.us)
  • The combination of 2- chloroadenosine with staurosporine, a cell cycle checkpoint dysregulator, enhances the killing potential of the antineoplastic agent and diminishes the effective antineoplastic dose. (eurekaselect.com)
  • The primary stimulatory processes are considered to be of histaminergic nature via G s -coupled H 2 receptor activation and of cholinergic nature via activation of G q -coupled muscarinic receptors or receptors for gastrin ( 69 ), but other actors are also on the stage. (physiology.org)
  • Dexmedetomidine is a α-2 receptor agonist that can sedate without significant respiratory depression. (bvsalud.org)
  • 5-n-ethylcarboxamidadenosine, 2-chloro-adenosine and R-phenylisopropyl adenosine also blocked tumor necrosis factor release in a potency suggestive of A2 receptor activity. (duke.edu)
  • 2] Clinical evidence for utilization of the A3 adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial. (axonmedchem.com)
  • 8-NH 2 -Ado treatment inhibited cell proliferation, activated cell death, and did not activate transcription of the p53 target gene p21 or increase protein levels of either p53 or p21. (aacrjournals.org)
  • Interestingly, 8-NH 2 -Ado caused the MDA-MB-231 cells to detach from the plate with only limited evidence of apoptotic cell death markers and the cell death was not inhibited by Z-VAD. (aacrjournals.org)
  • Maximum increases of 2-4-fold were observed 0.5 min after addition of 10-40 µM adenosine. (aspetjournals.org)
  • The purpose of this study was to investigate current usage status of NMBAs and antagonist with neuromuscular monitoring, among anesthesiologists in Korea.METHODS: Anesthesiologists working in Korea were invited to participate in an online survey via email January 2-February 28, 2018. (bvsalud.org)
  • Antagonism of A 3 R significantly potentiated the antihypertrophic effects of 2-chloroadenosine. (ahajournals.org)
  • CONCLUSIONS: Deficiency of ADA does not alter sensitivities of cardiovascular A(1) or A(2)ARs (despite markedly elevated [adenosine]), but significantly improves ischaemic tolerance. (edu.au)