Academic literature on the topic 'Adenosine A1 antagonist'

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Journal articles on the topic "Adenosine A1 antagonist"

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Jackson, Edwin K., Dongmei Cheng, Stevan P. Tofovic, and Zaichuan Mi. "Endogenous adenosine contributes to renal sympathetic neurotransmission via postjunctional A1 receptor-mediated coincident signaling." American Journal of Physiology-Renal Physiology 302, no. 4 (2012): F466—F476. http://dx.doi.org/10.1152/ajprenal.00495.2011.

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Adenosine A1 receptor antagonists have diuretic/natriuretic activity and may be useful for treating sodium-retaining diseases, many of which are associated with increased renal sympathetic tone. Therefore, it is important to determine whether A1 receptor antagonists alter renal sympathetic neurotransmission. In isolated, perfused rat kidneys, renal vasoconstriction induced by renal sympathetic nerve simulation was attenuated by 1) 1,3-dipropyl-8-p-sulfophenylxanthine (xanthine analog that is a nonselective adenosine receptor antagonist, but is cell membrane impermeable and thus does not block
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Lee, H. Thomas, and Charles W. Emala. "Protective effects of renal ischemic preconditioning and adenosine pretreatment: role of A1 and A3receptors." American Journal of Physiology-Renal Physiology 278, no. 3 (2000): F380—F387. http://dx.doi.org/10.1152/ajprenal.2000.278.3.f380.

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Renal ischemia and reperfusion during aortic and renal transplant surgery result in ischemic-reperfusion injury. Ischemic preconditioning and adenosine infusion before ischemia protect against ischemic-reperfusion injury in cardiac and skeletal muscle, but these protective phenomena have not been demonstrated in the kidney. Rats were randomized to sham operation, 45-min renal ischemia, ischemic preconditioning with four cycles of 8-min renal ischemia and 5-min reperfusion followed by 45-min renal ischemia, systemic adenosine pretreatment before 45-min renal ischemia, or pretreatments with sele
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Carlström, Mattias, Christopher S. Wilcox, and William J. Welch. "Adenosine A2 receptors modulate tubuloglomerular feedback." American Journal of Physiology-Renal Physiology 299, no. 2 (2010): F412—F417. http://dx.doi.org/10.1152/ajprenal.00211.2010.

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Adenosine can mediate the tubuloglomerular (TGF) response via activation of A1 receptors on the afferent arteriole, but both adenosine A1 and A2 receptors can regulate preglomerular resistance. We tested the hypothesis that adenosine A2 receptors offset the effect of A1 receptors and modulate the TGF. Maximal TGF responses were measured in male Sprague-Dawley rats as changes in proximal stop-flow pressure (ΔPSF) in response to increased perfusion of the loop of Henle (0 to 40 nl/min) with artificial tubular fluid (ATF). The maximal TGF response was studied after 5 min of intratubular perfusion
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Mozaffari, Mahmood S., Worku Abebe, and Brett K. Warren. "Renal adenosine A3 receptors in the rat: assessment of functional role." Canadian Journal of Physiology and Pharmacology 78, no. 5 (2000): 428–32. http://dx.doi.org/10.1139/y00-007.

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The functional roles of adenosine A3 receptors in the rat kidney were assessed for the first time with respect to A1 receptor-mediated responses. Utilizing a chronically instrumented conscious rat preparation, we tested renal excretory responses to acute administration of the A3 receptor antagonists 3-ethyl - 5-benzyl-2-methyl-6-phenyl- 4-phenylethynyl-1,4-(+)-dihydropridine-3,5-dicarboxylate (MRS-1191) and 9-chloro-2-(2-furyl)-5-phenylacetylamino- [1,2,4]-triazolo[1,5-c]quinazoline (MRS-1220) with reference to the effects of the A1 receptor antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX
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Auchampach, J. A., and G. J. Gross. "Adenosine A1 receptors, KATP channels, and ischemic preconditioning in dogs." American Journal of Physiology-Heart and Circulatory Physiology 264, no. 5 (1993): H1327—H1336. http://dx.doi.org/10.1152/ajpheart.1993.264.5.h1327.

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The objective of the present study was to characterize the role of adenosine in myocardial ischemic preconditioning in the canine heart. Preconditioning with 5 min of ischemia resulted in a marked reduction in infarct size after 60 min of left circumflex coronary artery occlusion and 5 h of reperfusion in barbital-anesthetized dogs compared with dogs that were not preconditioned (4.8 +/- 1.9 vs. 27.9 +/- 4.5%; P < 0.05). Pretreatment with either the nonselective adenosine receptor antagonist PD 115199 or the selective adenosine A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine block
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Olivera, A., M. Tomas, and J. M. Lopez-Novoa. "Effect of adenosine A1 and A2 agonists and antagonists on cAMP and Ca2+ in cultured rat mesangial cells." American Journal of Physiology-Cell Physiology 262, no. 4 (1992): C840—C844. http://dx.doi.org/10.1152/ajpcell.1992.262.4.c840.

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Rat glomeruli have been shown to exhibit A1 and A2 adenosine (ADO) receptors. Adenosine also contracts isolated glomeruli and cultured mesangial cells (MC). We studied the effect of the relatively selective ADO agonists R-N6-(1-methyl-1-phenylethyl)adenosine (R-PIA; A1) and 5'-(N-ethylcarboxamido)-adenosine (NECA; A2) on adenosine 3',5'-cyclic monophosphate (cAMP) levels and 45Ca influx in MC. R-PIA (10(-6) M) induced a 55% decrease in cAMP content in 5 microM forskolin-pretreated MC. NECA (10(-6) M) significantly increases by 68% the cAMP levels of forskolin-stimulated MC. NECA-included incre
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van Rensburg, HelenaDorathea Janse, LesetjaJ Legoabe, Gisella Terre’Blanche, and MiethaM Van der Walt. "2–Benzylidene–1–Indanone Analogues as Dual Adenosine A1/A2a Receptor Antagonists for the Potential Treatment of Neurological Conditions." Drug Research 69, no. 07 (2019): 382–91. http://dx.doi.org/10.1055/a-0808-3993.

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AbstractPrevious studies explored 2-benzylidine-1-tetralone derivatives as innovative adenosine A1 and A2A receptor antagonists for alternative non-dopaminergic treatment of Parkinson’s disease. This study’s aim is to investigate structurally related 2-benzylidene-1-indanones with substitutions on ring A and B as novel, potent and selective adenosine A1 and A2A receptor blockers. 2-Benzylidene-1-indanone derivatives were synthesised via acid catalysed aldol condensation reactions and evaluated via radioligand binding assays to ascertain structure activity relationships to govern A1 and A2A AR
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Coulson, R., P. S. Proch, R. A. Olsson, C. E. Chalfant, and D. R. Cooper. "Upregulated renal adenosine A1 receptors augment PKC and glucose transport but inhibit proliferation." American Journal of Physiology-Renal Physiology 270, no. 2 (1996): F263—F274. http://dx.doi.org/10.1152/ajprenal.1996.270.2.f263.

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Adenosine A1 receptor densities were increased in cultured LLC-PK1 and OK cells by chronic treatment with the adenosine receptor antagonists 1,3,7-trimethylxanthine (caffeine, 1 mM) and 1,3-dimethyl-8-cyclopentylxanthine [cyclopentyltheophylline (CPT), < or = 0.4 mM], respectively. The A1 receptor number per cell was increased twofold by 10-day treatments with 1 mM caffeine or 0.1 mM CPT, and the sodium-coupled glucose uptake was augmented twofold by 1 mM caffeine and sevenfold by 0.1 microM CPT (higher doses of CPT were progressively less stimulatory). Glucose uptake was blocked by acute (
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Montandon, Gaspard, Richard Kinkead, and Aida Bairam. "Disruption of adenosinergic modulation of ventilation at rest and during hypercapnia by neonatal caffeine in young rats: role of adenosine A1 and A2A receptors." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 292, no. 4 (2007): R1621—R1631. http://dx.doi.org/10.1152/ajpregu.00514.2006.

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Caffeine is commonly used to treat respiratory instabilities related to prematurity. However, the role of adenosinergic modulation and the potential long-term effects of neonatal caffeine treatment (NCT) on respiratory control are poorly understood. To address these shortcomings, we tested the following hypotheses: 1) adenosine A1- and A2A-receptor antagonists modulate respiratory activity at rest and during hypercapnia; 2) NCT has long-term consequences on adenosinergic modulation of respiratory control. Rat pups received by gavage either caffeine (15 mg/kg) or water (control) once a day from
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Norton, Gavin R., Angela J. Woodiwiss, Robert J. McGinn, et al. "Adenosine A1receptor-mediated antiadrenergic effects are modulated by A2a receptor activation in rat heart." American Journal of Physiology-Heart and Circulatory Physiology 276, no. 2 (1999): H341—H349. http://dx.doi.org/10.1152/ajpheart.1999.276.2.h341.

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Presently, the physiological significance of myocardial adenosine A2a receptor stimulation is unclear. In this study, the influence of adenosine A2a receptor activation on A1 receptor-mediated antiadrenergic actions was studied using constant-flow perfused rat hearts and isolated rat ventricular myocytes. In isolated perfused hearts, the selective A2a receptor antagonists 8-(3-chlorostyryl)caffeine (CSC) and 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol (ZM-241385) potentiated adenosine-mediated decreases in isoproterenol (Iso; 10−8 M)-elicited contractil
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Dissertations / Theses on the topic "Adenosine A1 antagonist"

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Gull, Mazhar [Verfasser], and André [Akademischer Betreuer] Brändli. "In vivo pharmacological profiling in Xenopus embryos defines a subset of A1 adenosine receptor-selective antagonists with potent anti-angiogenic activities / Mazhar Gull ; Betreuer: André Brändli." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2017. http://d-nb.info/1137226765/34.

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Affini, Anna [Verfasser]. "Histamine H3 receptor antagonists in combination with monoamine oxidase B and adenosine A1/A2A receptor ligands as multi-target approach for the treatment of Parkinson´s disease / Anna Affini." Düsseldorf : Universitäts- und Landesbibliothek der Heinrich-Heine-Universität Düsseldorf, 2019. http://d-nb.info/1190350807/34.

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Katsidzira, Runako Masline. "Affinity of dihydropyrimidone analogues for adenosine A1 and A2A receptors / Runako Masline Katsidzira." Thesis, 2014. http://hdl.handle.net/10394/10747.

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Parkinson’s disease (PD) is a neurodegenerative disorder that is characterised by a reduction of dopamine concentration in the striatum due to degeneration of dopaminergic neurons in the substantia nigra. Currently, first line treatment of PD includes the use of dopamine precursors, dopamine agonists and inhibitors of enzymatic degradation of dopamine, in an effort to restore dopamine levels and/or its effects. However, all these therapeutic strategies are only symptomatic and unfortunately do not slow, stop or reverse the progression of PD. From the discovery of adenosine A2A receptor-dopamin
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Kleynhans, Janke. "Aminopyrimidine derivatives as adenosine antagonists / Janke Kleynhans." Thesis, 2013. http://hdl.handle.net/10394/10857.

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Aims of this project - The aim of this study was to design and synthesise novel 2-aminopyrimidine derivatives as potential adenosine A1 and A2A receptor antagonists. Background and rationale - Parkinson’s disease is the second most common neurodegenerative disorder (after Alzheimer’s disease) and is characterised by the selective death of the dopaminergic neurons of the nigro-striatal pathway. Distinctive motor symptoms include bradykinesia, muscle rigidity and tremor, while non-motor symptoms, of which cognitive dysfunction is an example, also frequently occur. Current therapy provides sympto
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Book chapters on the topic "Adenosine A1 antagonist"

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Linden, J., C. Q. Earl, A. Patel, R. H. Craig, and S. M. Daluge. "Agonist and Antagonist Radioligands and Photoaffinity Labels for the Adenosine A1 Receptor." In Topics and Perspectives in Adenosine Research. Springer Berlin Heidelberg, 1987. http://dx.doi.org/10.1007/978-3-642-45619-0_1.

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Leid, M., P. H. Franklin, and T. F. Murray. "Antagonist Radioligand Binding to Solubilized Porcine Atrial A1 Adenosine Receptors." In Purines in Cellular Signaling. Springer New York, 1990. http://dx.doi.org/10.1007/978-1-4612-3400-5_11.

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Gao, Zhan-Guo, Dilip K. Tosh, Shanu Jain, Jinha Yu, Rama R. Suresh, and Kenneth A. Jacobson. "A1 Adenosine Receptor Agonists, Antagonists, and Allosteric Modulators." In The Adenosine Receptors. Springer International Publishing, 2018. http://dx.doi.org/10.1007/978-3-319-90808-3_4.

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Kiesman, William F., Elfatih Elzein, and Jeff Zablocki. "A1 Adenosine Receptor Antagonists, Agonists, and Allosteric Enhancers." In Adenosine Receptors in Health and Disease. Springer Berlin Heidelberg, 2009. http://dx.doi.org/10.1007/978-3-540-89615-9_2.

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Conference papers on the topic "Adenosine A1 antagonist"

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Jang, Sunyoung, Seunah Jun, Hosun Lee, et al. "Abstract 1704: Discovery and characterization of a novel triple A1/A2a/A2b adenosine receptor antagonist for cancer immunotherapy." In Proceedings: AACR Annual Meeting 2021; April 10-15, 2021 and May 17-21, 2021; Philadelphia, PA. American Association for Cancer Research, 2021. http://dx.doi.org/10.1158/1538-7445.am2021-1704.

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Ramos-Barbon, David, Nadia S. Brienza, Teresa Bigorra Rodríguez, et al. "PBF-680, an oral A1 adenosine receptor antagonist, inhibits adenosine monophosphate (AMP) airway hyperresponsiveness (AHR) in mild-to-moderate asthma: a Phase-IIa proof-of-concept trial." In ERS International Congress 2020 abstracts. European Respiratory Society, 2020. http://dx.doi.org/10.1183/13993003.congress-2020.2279.

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Ramos-Barbon, David, Nadia S. Brienza, Teresa Bigorra Rodríguez, et al. "PBF-680, an oral A1 adenosine receptor antagonist, inhibits the late allergic response (LAR) in mild-to-moderate atopic asthmatics: a Phase-IIa trial." In ERS International Congress 2020 abstracts. European Respiratory Society, 2020. http://dx.doi.org/10.1183/13993003.congress-2020.4784.

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Van Calenbergh, Serge, Andreas Link, Shelly Fujikawa та ін. "5'-Deoxy congeners of 9-(3-amido-3-deoxy-β-D-xylofuranosyl)-N6-cyclopentyladenine: New adenosine A1 receptor antagonists". У XIth Symposium on Chemistry of Nucleic Acid Components. Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 1999. http://dx.doi.org/10.1135/css199902273.

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