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Journal articles on the topic 'Adenosine receptor antagonists'

Author: Grafiati

Published: 4 June 2021

Last updated: 11 March 2023

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1

Shang, Liangcheng, Yaobiao Huang, Xin Xie, Sudan Ye, and Chun Chen. "Effect of Adenosine Receptor Antagonists on Adenosine-Pretreated PC12 Cells Exposed to Paraquat." Dose-Response 20, no. 2 (April 2022): 155932582210934. http://dx.doi.org/10.1177/15593258221093411.

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Previous studies evaluated the adenosine receptor antagonists alone to determine their effects on oxidative stress, but little is known about adenosine’s protective efficacy when oxidative injury occurs in vivo. Adenosine is a crucial signaling molecule recognized by four distinct G-protein-coupled receptors (GPCRs) (i.e., A1R, A2AR, A2BR, and A3R) and protects cells against pathological conditions. The present study was performed to evaluate the role of antagonist modulation in the setting of paraquat toxicity with adenosine pretreatment. First, PC12 cells were exposed to paraquat (850 μM) an

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2

Shi, Yanrong, Xiaoguang Liu, Debebe Gebremedhin, John R. Falck, David R. Harder, and Raymond C. Koehler. "Interaction of Mechanisms Involving Epoxyeicosatrienoic Acids, Adenosine Receptors, and Metabotropic Glutamate Receptors in Neurovascular Coupling in Rat Whisker Barrel Cortex." Journal of Cerebral Blood Flow & Metabolism 28, no. 1 (May 23, 2007): 111–25. http://dx.doi.org/10.1038/sj.jcbfm.9600511.

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Adenosine, astrocyte metabotropic glutamate receptors (mGluRs), and epoxyeicosatrienoic acids (EETs) have been implicated in neurovascular coupling. Although A2A and A2B receptors mediate cerebral vasodilation to adenosine, the role of each receptor in the cerebral blood flow (CBF) response to neural activation remains to be fully elucidated. In addition, adenosine can amplify astrocyte calcium, which may increase arachidonic acid metabolites such as EETs. The interaction of these pathways was investigated by determining if combined treatment with antagonists exerted an additive inhibitory eff

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3

Bozarov, Andrey, Yu-Zhong Wang, Jun Ge Yu, Jacqueline Wunderlich, Hamdy H. Hassanain, Mazin Alhaj, Helen J. Cooke, Iveta Grants, Tianhua Ren, and Fievos L. Christofi. "Activation of adenosine low-affinity A3 receptors inhibits the enteric short interplexus neural circuit triggered by histamine." American Journal of Physiology-Gastrointestinal and Liver Physiology 297, no. 6 (December 2009): G1147—G1162. http://dx.doi.org/10.1152/ajpgi.00295.2009.

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We tested the novel hypothesis that endogenous adenosine (eADO) activates low-affinity A3 receptors in a model of neurogenic diarrhea in the guinea pig colon. Dimaprit activation of H2 receptors was used to trigger a cyclic coordinated response of contraction and Cl− secretion. Contraction-relaxation was monitored by sonomicrometry (via intracrystal distance) simultaneously with short-circuit current ( Isc, Cl− secretion). The short interplexus reflex coordinated response was attenuated or abolished by antagonists at H2 (cimetidine), 5-hydroxytryptamine 4 receptor (RS39604), neurokinin-1 recep

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4

Muller, C. "A3 Adenosine Receptor Antagonists." Mini-Reviews in Medicinal Chemistry 1, no. 4 (November 1, 2001): 417–27. http://dx.doi.org/10.2174/1389557510101040417.

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5

Müller, Christa E. "A1-Adenosine receptor antagonists." Expert Opinion on Therapeutic Patents 7, no. 5 (May 1997): 419–40. http://dx.doi.org/10.1517/13543776.7.5.419.

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6

Pérez-Pinzón, Miguel A., Peter L. Lutz, Thomas J. Sick, and Myron Rosenthal. "Adenosine, a “Retaliatory” Metabolite, Promotes Anoxia Tolerance in Turtle Brain." Journal of Cerebral Blood Flow & Metabolism 13, no. 4 (July 1993): 728–32. http://dx.doi.org/10.1038/jcbfm.1993.93.

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Contrary to what is found in most vertebrates, the brains of certain turtle species maintain ATP levels and ion homeostasis and survive prolonged anoxia. The hypothesis tested here is that the release of adenosine and its binding to A1 receptors are essential for this anoxic tolerance. Studies were conducted in the isolated turtle cerebellum, which did release adenosine to the extracellular space during anoxia. When adenosine receptor antagonists [theophylline, 8-cyclopentyltheophylline (CPT), or 8-cyclopentyl-1,3-dipropylxanthine (DPCPX)] were added to the superfusate under control conditions

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7

Temirak, Ahmed, Jonathan G. Schlegel, Jan H. Voss, Victoria J. Vaaßen, Christin Vielmuth, Tobias Claff, and Christa E. Müller. "Irreversible Antagonists for the Adenosine A2B Receptor." Molecules 27, no. 12 (June 13, 2022): 3792. http://dx.doi.org/10.3390/molecules27123792.

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Blockade of the adenosine A2B receptor (A2BAR) represents a potential novel strategy for the immunotherapy of cancer. In the present study, we designed, synthesized, and characterized irreversible A2BAR antagonists based on an 8-p-sulfophenylxanthine scaffold. Irreversible binding was confirmed in radioligand binding and bioluminescence resonance energy transfer(BRET)-based Gα15 protein activation assays by performing ligand wash-out and kinetic experiments. p-(1-Propylxanthin-8-yl)benzene sulfonyl fluoride (6a, PSB-21500) was the most potent and selective irreversible A2BAR antagonist of the

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8

Fan, Ming, Weixi Qin, and S. Jamal Mustafa. "Characterization of adenosine receptor(s) involved in adenosine-induced bronchoconstriction in an allergic mouse model." American Journal of Physiology-Lung Cellular and Molecular Physiology 284, no. 6 (June 1, 2003): L1012—L1019. http://dx.doi.org/10.1152/ajplung.00353.2002.

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We recently reported that adenosine caused bronchoconstriction and enhanced airway inflammation in an allergic mouse model. In this study, we further report the characterization of the subtype of adenosine receptor(s) involved in bronchoconstriction. 5′-( N-ethylcarboxamido)adenosine (NECA), a nonselective adenosine agonist, elicited bronchoconstriction in a dose-dependent manner. Little effects of N 6-cyclopentyladenosine (A1-selective agonist) and 2- p-(2-carboxyethyl)phenethylamino-5′- N-ethylcarboxamidoadenosine (A2A-selective agonist) compared with NECA were observed in this model. 2-Chlo

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9

Baraldi, P. G., B. Cacciar, G. Spalluto, A. Borioni, M. Viziano, S. Dionisotti, and E. Ongini. "Current Developments of A2a Adenosine Receptor Antagonists." Current Medicinal Chemistry 2, no. 3 (October 1995): 707–22. http://dx.doi.org/10.2174/092986730203220223144628.

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<P>Adenosine regulates a wide range of physiological functions through specific cell membrane receptors. On the basis of pharmacological studies and molecular cloning, four distinct adenosine receptors have been identified and classified as A1, A2a. A2b and A3. These adenosine receptors are members of the G-protein-coupled receptor family. <P> An intense medicinal chemistry effort made over the last 20 years has led to a variety of selective adenosine receptor agonists and antagonists. While all the agonists thus far identified are related to the adenosine structure, the antagonist

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10

Tay, Apple Hui Min, Rubén Prieto-Díaz, Shiyong Neo, Le Tong, Xinsong Chen, Valentina Carannante, Björn Önfelt, et al. "A_2B adenosine receptor antagonists rescue lymphocyte activity in adenosine-producing patient-derived cancer models." Journal for ImmunoTherapy of Cancer 10, no. 5 (May 2022): e004592. http://dx.doi.org/10.1136/jitc-2022-004592.

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BackgroundAdenosine is a metabolite that suppresses antitumor immune response of T and NK cells via extracellular binding to the two subtypes of adenosine-2 receptors, A2ARs. While blockade of the A2AARs subtype effectively rescues lymphocyte activity, with four A2AAR antagonists currently in anticancer clinical trials, less is known for the therapeutic potential of the other A2BAR blockade within cancer immunotherapy. Recent studies suggest the formation of A2AAR/A2BAR dimers in tissues that coexpress the two receptor subtypes, where the A2BAR plays a dominant role, suggesting it as a promisi

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11

Norton, Gavin R., Angela J. Woodiwiss, Robert J. McGinn, Mojca Lorbar, Eugene S. Chung, Thomas W. Honeyman, Richard A. Fenton, James G. Dobson, and Theo E. Meyer. "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 (February 1, 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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12

PARSONS, WILLIAM J. "Methylxanthines as Adenosine Receptor Antagonists." Annals of Internal Medicine 103, no. 4 (October 1, 1985): 643. http://dx.doi.org/10.7326/0003-4819-103-4-643_1.

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13

Ongini, Ennio, Angela Monopoli, Barbara Cacciari, and Pier Giovanni Baraldi. "Selective adenosine A2A receptor antagonists." Il Farmaco 56, no. 1-2 (March 2001): 87–90. http://dx.doi.org/10.1016/s0014-827x(01)01024-2.

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14

Nadeem, Ahmed, and S. Jamal Mustafa. "Adenosine receptor antagonists and asthma." Drug Discovery Today: Therapeutic Strategies 3, no. 3 (September 2006): 269–75. http://dx.doi.org/10.1016/j.ddstr.2006.09.006.

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15

Khimenko, P. L., T. M. Moore, L. W. Hill, P. S. Wilson, S. Coleman, A. Rizzo, and A. E. Taylor. "Adenosine A2 receptors reverse ischemia-reperfusion lung injury independent of beta-receptors." Journal of Applied Physiology 78, no. 3 (March 1, 1995): 990–96. http://dx.doi.org/10.1152/jappl.1995.78.3.990.

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To evaluate the adenosine systems ability to reverse the endothelial damage produced by ischemia and reperfusion (I/R), we studied several different selective adenosine-receptor agonists and antagonists, a protein kinase A inhibitor, and a beta-adrenoreceptor antagonist in isolated buffer-perfused rat lungs. I/R (45 min/105 min) produced a sixfold increase in endothelial permeability as measured by the capillary filtration coefficient. Both a selective A2-receptor agonist (CGS-21680, 300 nM) and a beta-receptor agonist (isoproterenol, 10 microM) reversed the increased microvascular permeabilit

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16

Carlström, Mattias, Christopher S. Wilcox, and William J. Welch. "Adenosine A2 receptors modulate tubuloglomerular feedback." American Journal of Physiology-Renal Physiology 299, no. 2 (August 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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17

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 (February 15, 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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18

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 (January 7, 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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19

Gorman, Mark W., Kayoko Ogimoto, Margaret V. Savage, Kenneth A. Jacobson, and Eric O. Feigl. "Nucleotide coronary vasodilation in guinea pig hearts." American Journal of Physiology-Heart and Circulatory Physiology 285, no. 3 (September 2003): H1040—H1047. http://dx.doi.org/10.1152/ajpheart.00981.2002.

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The role of P1 receptors and P2Y1 receptors in coronary vasodilator responses to adenine nucleotides was examined in the isolated guinea pig heart. Bolus arterial injections of nucleotides were made in hearts perfused at constant pressure. Peak increase in flow was measured before and after addition of purinoceptor antagonists. Both the P1 receptor antagonist 8-( p-sulfophenyl)theophylline and adenosine deaminase inhibited adenosine vasodilation. AMP-induced vasodilation was inhibited by P1 receptor blockade but not by adenosine deaminase or by the selective P2Y1 antagonist N6-methyl-2′-deoxya

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20

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 (April 10, 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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21

Carlsson, Per-Ola, Richard Olsson, Örjan Källskog, Birgitta Bodin, Arne Andersson, and Leif Jansson. "Glucose-induced islet blood flow increase in rats: interaction between nervous and metabolic mediators." American Journal of Physiology-Endocrinology and Metabolism 283, no. 3 (September 1, 2002): E457—E464. http://dx.doi.org/10.1152/ajpendo.00044.2002.

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This study investigated the mechanisms for glucose-induced islet blood flow increase in rats. The effects of adenosine, adenosine receptor antagonists, and vagotomy on islet blood flow were evaluated with a microsphere technique. Vagotomy prevented the islet blood flow increase expected 3, 10, and 20 min after injection of glucose, whereas theophylline (a nonspecific adenosine receptor antagonist) prevented the islet blood flow increase from occurring 10 and 20 min after glucose administration. Administration of selective adenosine receptor antagonists suggested that the response to theophylli

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22

Bivalacqua, Trinity J., Hunter C. Champion, David G. Lambert, and Philip J. Kadowitz. "Vasodilator responses to adenosine and hyperemia are mediated by A1 and A2 receptors in the cat vascular bed." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 282, no. 6 (June 1, 2002): R1696—R1709. http://dx.doi.org/10.1152/ajpregu.00394.2001.

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Hemodynamic responses to adenosine, the A1 receptor agonists N 6-cyclopentyladenosine (CPA) and adenosine amine congener (ADAC), and the A2 receptor agonist 5′-( N-cyclopropyl)-carboxamido-adenosine (CPCA) were investigated in the hindquarter vascular bed of the cat under constant-flow conditions. Injections of adenosine, CPA, ADAC, CPCA, ATP, and adenosine 5′- O-(3-thiotriphosphate) (ATPγS) into the perfusion circuit induced dose-related decreases in perfusion pressure. Vasodilator responses to the A1 agonists were reduced by the A1 receptor antagonists KW-3902 and CGS-15943, whereas response

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Lorbar, Mojca, Eugene S. Chung, Arash Nabi, Katarina Skalova, Richard A. Fenton, James G. Dobson, Jr., and Theo E. Meyer. "Receptors subtypes involved in adenosine-mediated modulation of norepinephrine release from cardiac nerve terminals." Canadian Journal of Physiology and Pharmacology 82, no. 11 (November 1, 2004): 1026–31. http://dx.doi.org/10.1139/y04-108.

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The objective of this study was to determine which adenosine receptor subtypes were involved in the modulation of norepinephrine release from cardiac nerve terminals. In addition, the persistence of adenosine-mediated effects was evaluated. Rat hearts attached to the stellate ganglion were isolated and perfused. The ganglion was electrically stimulated twice (S1 and S2), allowing 10 min between the stimulations. To determine adenosine receptor subtypes, selective and nonselective adenosine agonists and antagonists were infused following S1 and until the end of S2. To evaluate the persistence o

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Gao, Zhan-Guo, and Kenneth A. Jacobson. "A2B Adenosine Receptor and Cancer." International Journal of Molecular Sciences 20, no. 20 (October 17, 2019): 5139. http://dx.doi.org/10.3390/ijms20205139.

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There are four subtypes of adenosine receptors (ARs), named A1, A2A, A2B and A3, all of which are G protein-coupled receptors (GPCRs). Locally produced adenosine is a suppressant in anti-tumor immune surveillance. The A2BAR, coupled to both Gαs and Gαi G proteins, is one of the several GPCRs that are expressed in a significantly higher level in certain cancer tissues, in comparison to adjacent normal tissues. There is growing evidence that the A2BAR plays an important role in tumor cell proliferation, angiogenesis, metastasis, and immune suppression. Thus, A2BAR antagonists are novel, potentia

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Dubey, Raghvendra K., Delbert G. Gillespie, and Edwin K. Jackson. "A2B Adenosine Receptors Mediate the Anti-Mitogenic Effects of Adenosine in Cardiac Fibroblasts." Hypertension 36, suppl_1 (October 2000): 708. http://dx.doi.org/10.1161/hyp.36.suppl_1.708-b.

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P85 Adenosine inhibits growth of CFs; however, the adenosine receptor subtype that mediates this anti-mitogenic effect remains undefined. Using specific ADE receptor antagonists and agonists and antisense oligonucleotides (OLIGO) against A2B receptors, we investigated the role of A2B receptors in inhibiting cardiac fibroblast growth. PDGF (25ng/ml)-induced DNA synthesis, cell number and collagen synthesis in CFs were inhibited by A2 (chloroadenosine [Cl-Ad]and MECA), but not by A1 (CPA), A2a ( CGS21680 ) or A3 (AB-MECA),receptor agonists.The inhibitory effects of 1μM MECA and Cl-Ad were revers

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Marala, R. B., and S. J. Mustafa. "Adenosine analogues prevent phorbol ester-induced PKC depletion in porcine coronary artery via A1 receptor." American Journal of Physiology-Heart and Circulatory Physiology 268, no. 1 (January 1, 1995): H271—H277. http://dx.doi.org/10.1152/ajpheart.1995.268.1.h271.

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This study was undertaken to determine the adenosine receptor involved in the modulation of protein kinase C (PKC) in porcine coronary artery. Endothelium-denuded arterial rings were incubated with phorbol 12,13-dibutyrate (PDBu) in the presence or absence of adenosine receptor agonists and antagonists for 24 h. After incubation, contractile responses to endothelin-1 (ET-1) were compared in various treatment groups. Arterial rings incubated with PDBu alone failed to produce significant contractions in response to ET-1. (2s)-N6-[2-endo-norbornyl]adenosine (ENBA), an A1-receptor agonist, attenua

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Donoso, M. Verónica, Rodrigo López, Ramiro Miranda, René Briones, and J. Pablo Huidobro-Toro. "A2B adenosine receptor mediates human chorionic vasoconstriction and signals through arachidonic acid cascade." American Journal of Physiology-Heart and Circulatory Physiology 288, no. 5 (May 2005): H2439—H2449. http://dx.doi.org/10.1152/ajpheart.00548.2004.

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Because adenosine is a vascular tone modulator, we examined the effect of adenosine and congeners in the vascular reactivity of isolated human placental vessels and in perfused cotyledons. We characterized its vasomotor action and tentatively identified the receptor subtypes and their intracellular signaling mechanisms. We recorded isometric tension from the circular layer of chorionic vessel rings maintained under 1.5 g of basal tension or precontracted with KCl. The relative order of potency of adenosine and structural analogs is consistent with the expression of A2B receptors, 5′-( N-ethylc

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Bonaventura, Jordi, Gemma Navarro, Verònica Casadó-Anguera, Karima Azdad, William Rea, Estefanía Moreno, Marc Brugarolas, et al. "Allosteric interactions between agonists and antagonists within the adenosine A2A receptor-dopamine D2 receptor heterotetramer." Proceedings of the National Academy of Sciences 112, no. 27 (June 22, 2015): E3609—E3618. http://dx.doi.org/10.1073/pnas.1507704112.

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Adenosine A2A receptor (A2AR)-dopamine D2 receptor (D2R) heteromers are key modulators of striatal neuronal function. It has been suggested that the psychostimulant effects of caffeine depend on its ability to block an allosteric modulation within the A2AR-D2R heteromer, by which adenosine decreases the affinity and intrinsic efficacy of dopamine at the D2R. We describe novel unsuspected allosteric mechanisms within the heteromer by which not only A2AR agonists, but also A2AR antagonists, decrease the affinity and intrinsic efficacy of D2R agonists and the affinity of D2R antagonists. Striking

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Jin, Jianguo, Todd M. Quinton, Jin Zhang, Susan E. Rittenhouse та Satya P. Kunapuli. "Adenosine diphosphate (ADP)–induced thromboxane A2generation in human platelets requires coordinated signaling through integrin αIIbβ3 and ADP receptors". Blood 99, № 1 (1 січня 2002): 193–98. http://dx.doi.org/10.1182/blood.v99.1.193.

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Adenosine diphosphate (ADP) is a platelet agonist that causes platelet shape change and aggregation as well as generation of thromboxane A2, another platelet agonist, through its effects on P2Y1, P2Y12, and P2X1 receptors. It is now reported that both 2-propylthio-D-βγ-dichloromethylene adenosine 5′-triphosphate (AR-C67085), a P2Y12 receptor–selective antagonist, and adenosine-2′-phosphate-5′-phosphate (A2P5P), a P2Y1 receptor–selective antagonist, inhibited ADP-induced thromboxane A2 generation in a concentration-dependent manner, indicating that coactivation of the P2Y12 and P2Y1 receptors i

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Merighi, Stefania, Pier Andrea Borea, Katia Varani, Fabrizio Vincenzi, Alessia Travagli, Manuela Nigro, Silvia Pasquini, et al. "Pathophysiological Role and Medicinal Chemistry of A2A Adenosine Receptor Antagonists in Alzheimer’s Disease." Molecules 27, no. 9 (April 21, 2022): 2680. http://dx.doi.org/10.3390/molecules27092680.

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The A2A adenosine receptor is a protein belonging to a family of four GPCR adenosine receptors. It is involved in the regulation of several pathophysiological conditions in both the central nervous system and periphery. In the brain, its localization at pre- and postsynaptic level in striatum, cortex, hippocampus and its effects on glutamate release, microglia and astrocyte activation account for a crucial role in neurodegenerative diseases, including Alzheimer’s disease (AD). This ailment is considered the main form of dementia and is expected to exponentially increase in coming years. The pa

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Neely, C. F., J. Jin, and I. M. Keith. "A1-adenosine receptor antagonists block endotoxin-induced lung injury." American Journal of Physiology-Lung Cellular and Molecular Physiology 272, no. 2 (February 1, 1997): L353—L361. http://dx.doi.org/10.1152/ajplung.1997.272.2.l353.

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Endotoxin produces a variety of biological effects on different cell types, such as priming of neutrophils and macrophages, which then release a number of important mediators of endotoxin-induced lung injury. However, the specific mechanism by which endotoxin initiates its cascade of pathophysiological events in the lung has not been described. Both A1 adenosine receptor activation and endotoxin induce the release of thromboxane A2 from the lung and inhibit adenylate cyclase. By acting on A1 adenosine receptors, adenosine promotes neutrophil chemotaxis and adherence to endothelial cells. We hy

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Monahan, Thomas S., Darrell R. Sawmiller, Richard A. Fenton, and James G. Dobson. "Adenosine A2a-receptor activation increases contractility in isolated perfused hearts." American Journal of Physiology-Heart and Circulatory Physiology 279, no. 4 (October 1, 2000): H1472—H1481. http://dx.doi.org/10.1152/ajpheart.2000.279.4.h1472.

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Adenosine A2a-receptor activation enhances shortening of isolated cardiomyocytes. In the present study the effect of A2a-receptor activation on the contractile performance of isolated rat hearts was investigated by recording left ventricular pressure (LVP) and the maximal rate of LVP development (+dP/d t max). With constant-pressure perfusion, adenosine caused concentration-dependent increases in LVP and +dP/d t max, with detectable increases of 4.1 and 4.8% at 10−6 M and maximal increases of 12.0 and 11.1% at 10−4 M, respectively. The contractile responses were prevented by the A2a-receptor a

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Chen, J., B. Dinger, and S. J. Fidone. "cAMP production in rabbit carotid body: role of adenosine." Journal of Applied Physiology 82, no. 6 (June 1, 1997): 1771–75. http://dx.doi.org/10.1152/jappl.1997.82.6.1771.

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Chen, J., B. Dinger, and S. J. Fidone. cAMP production in rabbit carotid body: role of adenosine. J. Appl. Physiol. 82(6): 1771–1775, 1997.—In the present study, we have investigated the possible role of adenosine in the hypoxia-mediated increase in adenosine 3′,5′-cyclic monophosphate (cAMP) in the carotid body. cAMP levels in rabbit carotid bodies superfused in vitro for 10 min were increased in the presence of adenosine (100 μM and 1.0 mM; maximum increase = 127%, P < 0.01). These effects were reduced by the nonspecific adenosine-receptor antagonist 1,3-dipropyl-8[ p-sulfophenyl]xanthine

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Cacciari, Barbara, Giorgia Pastorin, Chiara Bolcato, Giampiero Spalluto, Magdalena Bacilieri, and Stefano Moro. "A2B Adenosine Receptor Antagonists: Recent Developments." Mini-Reviews in Medicinal Chemistry 5, no. 12 (December 1, 2005): 1053–60. http://dx.doi.org/10.2174/138955705774933374.

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Roy, Kunal. "QSAR of Adenosine Receptor Antagonists II:." QSAR & Combinatorial Science 22, no. 6 (August 2003): 614–21. http://dx.doi.org/10.1002/qsar.200330821.

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Cheong, Siew Lee, Gopalakrishnan Venkatesan, Priyankar Paira, Ramasamy Jothibasu, Alexander Laurence Mandel, Stephanie Federico, Giampiero Spalluto, and Giorgia Pastorin. "Pyrazolo Derivatives as Potent Adenosine Receptor Antagonists: An Overview on the Structure-Activity Relationships." International Journal of Medicinal Chemistry 2011 (April 7, 2011): 1–15. http://dx.doi.org/10.1155/2011/480652.

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In the past few decades, medicinal chemistry research towards potent and selective antagonists of human adenosine receptors (namely, A1, A2A, A2B, and A3) has been evolving rapidly. These antagonists are deemed therapeutically beneficial in several pathological conditions including neurological and renal disorders, cancer, inflammation, and glaucoma. Up to this point, many classes of compounds have been successfully synthesized and identified as potent human adenosine receptor antagonists. In this paper, an overview of the structure-activity relationship (SAR) profiles of promising nonxanthine

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Shultz, P. J., J. R. Sedor, and H. E. Abboud. "Dopaminergic stimulation of cAMP accumulation in cultured rat mesangial cells." American Journal of Physiology-Heart and Circulatory Physiology 253, no. 2 (August 1, 1987): H358—H364. http://dx.doi.org/10.1152/ajpheart.1987.253.2.h358.

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Dopamine (DA) alters renal hemodynamics, and DA receptors have been demonstrated in isolated glomeruli. To determine the glomerular cell type bearing DA receptors, we studied the effect of dopaminergic agonists and antagonists on adenosine 3',5'-cyclic monophosphate (cAMP) accumulation in rat glomerular mesangial and epithelial cells in culture. DA caused a marked dose- and time-dependent increase in cAMP accumulation in mesangial but not epithelial cells. The stimulatory effect of DA was abolished by the DA antagonists haloperidol, trifluoperazine, and cis-thiothixene but not by beta- or alph

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Thümmler, Susanne, and Thomas V. Dunwiddie. "Adenosine Receptor Antagonists Induce Persistent Bursting in the Rat Hippocampal CA3 Region Via an NMDA Receptor-Dependent Mechanism." Journal of Neurophysiology 83, no. 4 (April 1, 2000): 1787–95. http://dx.doi.org/10.1152/jn.2000.83.4.1787.

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Adenosine receptor antagonists initiate repetitive bursting activity in the CA3 region of hippocampal slices. Although some studies have suggested that this effect is irreversible, this has been difficult to establish because many adenosine antagonists wash out of brain slices extremely slowly. Furthermore the cellular mechanism that underlies persistent bursting is unknown. To resolve these issues, we studied the effects of nonselective (8-p-sulfophenyltheophylline, 8SPT, 50–100 μM), Al-selective (8-cyclopentyl-1,3-dipropylxanthine, 100 nM; xanthine carboxylic acid congener, 200 nM), and A2A-

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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 (February 1, 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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Castaldo, C., T. Benicchi, M. Otrocka, E. Mori, E. Pilli, P. Ferruzzi, S. Valensin, et al. "CXCR4 Antagonists." Journal of Biomolecular Screening 19, no. 6 (March 14, 2014): 859–69. http://dx.doi.org/10.1177/1087057114526283.

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The CXC chemokine receptor 4 (CXCR4) is a widely expressed G protein–coupled receptor implicated in several diseases. In cancer, an increased number of surface CXCR4 receptors, in parallel with aberrant signaling, have been reported to influence several aspects of malignancy progression. CXCR4 activation by the specific ligand C-X-C motif chemokine 12 (CXCL12) induces several intracellular signaling pathways that have been selectively related to malignancy depending on the tissue or cell type. We developed a panel of CXCR4 screening assays investigating Gαi-mediated cyclic adenosine monophosph

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Schepp, W., A. H. Soll, and J. H. Walsh. "Dual modulation by adenosine of gastrin release from canine G-cells in primary culture." American Journal of Physiology-Gastrointestinal and Liver Physiology 259, no. 4 (October 1, 1990): G556—G563. http://dx.doi.org/10.1152/ajpgi.1990.259.4.g556.

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The effects of adenosine on gastrin release were studied in enzymatically dispersed canine antral cells after 24-36 h in primary culture. We found two contrasting actions for adenosine: inhibition of forskolin-stimulated gastrin release and potentiation of bombesin-stimulated gastrin release. These actions appeared to be mediated by A1 and A2 receptors, respectively. Forskolin-stimulated gastrin release was reduced by adenosine and the A1-selective agonist N6-(L-2-phenylisopropyl)adenosine (L-PIA) but not by the A2-selective agonist 2-phenylaminoadenosine (CV 1808). This inhibition by adenosin

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Glenn, Jackie, Ann White, Sue Fox, Hans van Giezen, Sven Nylander, Stan Heptinstall, and David Iyú. "Mode of action of P2Y12 antagonists as inhibitors of platelet function." Thrombosis and Haemostasis 105, no. 01 (2011): 96–106. http://dx.doi.org/10.1160/th10-07-0482.

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SummaryP2Y12 receptor antagonists are antithrombotic agents that inhibit platelet function by blocking the effects of adenosine diphosphate (ADP) at P2Y12 receptors. However, some P2Y12 receptor antagonists may affect platelet function through additional mechanisms. It was the objective of this study to investigate the possibility that P2Y12 antagonists inhibit platelet function through interaction with G-protein-coupled receptors other than P2Y12 receptors. We compared the effects of cangrelor, ticagrelor and the prasugrel active metabolite on platelet aggregation and on phosphorylation of va

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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 (May 1, 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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Pan, Sheng-Jun, and Li-Rong Li. "Adenosine A2 receptors are involved in the activation of ATP-sensitive K+ currents during metabolic inhibition in guinea pig ventricular myocytes." Canadian Journal of Physiology and Pharmacology 89, no. 3 (March 2011): 187–96. http://dx.doi.org/10.1139/y11-010.

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It has been hypothesized that an interaction among adenosine A1 receptors, protein kinase C (PKC) activation, and ATP-sensitive potassium channels (KATP) mediates ischemic preconditioning in experiments on different animal species. The purpose of this study was to determine if activation of KATP is functionally coupled to A1 receptors and (or) PKC activation during metabolic inhibition (MI) in guinea pig ventricular myocytes. Perforated-patch using nystatin and conventional whole-cell recording methods were used to observe the effects of adenosine and adenosine-receptor antagonists on the acti

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LIU, Chengqian, Yulia Mukienko, Chengxiang Wu, and Andrey Zavialov. "Human adenosine deaminases control the immune cell responses to activation signals by reducing extracellular adenosine concentration." Journal of Immunology 196, no. 1_Supplement (May 1, 2016): 124.63. http://dx.doi.org/10.4049/jimmunol.196.supp.124.63.

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Abstract Adenosine rapidly accumulates in the sites of inflammation and tumor growth. It binds to adenosine receptors expressed on the cell surface of immune cells and induces either suppression or activation of inflammatory responses to pathogens. In humans the level of extracellular adenosine is regulated by two adenosine deaminases ADA1 and ADA2. Decrease in ADAs concentration due to genetic defects in the ADA genes leads to serious perturbation in the immune system function while increase in ADA activity associates with numerous immune diseases and cancers. The immune responses to extracel

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Kaplan, G. B., and M. T. Sears. "Adenosine receptor agonists attenuate and adenosine receptor antagonists exacerbate opiate withdrawal signs." Psychopharmacology 123, no. 1 (January 1996): 64–70. http://dx.doi.org/10.1007/bf02246282.

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Zhang, Jinfeng, Wenzhong Yan, Wenwen Duan, Kurt Wüthrich, and Jianjun Cheng. "Tumor Immunotherapy Using A2A Adenosine Receptor Antagonists." Pharmaceuticals 13, no. 9 (September 8, 2020): 237. http://dx.doi.org/10.3390/ph13090237.

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The A2A adenosine receptor (A2AAR) plays critical roles in human physiology and pathophysiology, which makes it an important drug target. Previous drug-discovery efforts targeting the A2AAR have been focused on the use of A2AAR antagonists for the treatment of Parkinson’s disease. More recently, the A2AAR has attracted additional attention for its roles in immuno-oncology, and a number of A2AAR antagonists are currently used as lead compounds for antitumor drugs in both preclinical models and clinical trials. This review surveys recent advances in the development of A2AAR antagonists for cance

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Koscso, Balazs, Zsolt Selmeczy, Leonora Himer, Balazs Csoka, and Gyorgy Hasko. "Adenosine receptor activation augments IL-10 production by murine microglial cells (116.31)." Journal of Immunology 186, no. 1_Supplement (April 1, 2011): 116.31. http://dx.doi.org/10.4049/jimmunol.186.supp.116.31.

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Abstract Microglia, the intrinsic macrophages of the central nervous system produce the anti-inflammatory cytokine IL-10 following activation with the bacterial cell wall product peptidoglycan (PGN), which is recognized by Toll-like receptor 2 (TLR2). Adenosine is an endogenous purine nucleoside that binds to specific G protein-coupled receptors (A1, A2A, A2B, and A3), and is a well known modulator of the immune system. In this study we investigated the effect of adenosine on IL-10 production by microglia. Cells were treated with adenosine, or selective adenosine receptor agonists and antagoni

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Sarkar, Bidisha, Santanu Maiti, Gajanan Raosaheb Jadhav, and Priyankar Paira. "Discovery of benzothiazolylquinoline conjugates as novel human A 3 receptor antagonists: biological evaluations and molecular docking studies." Royal Society Open Science 5, no. 2 (February 2018): 171622. http://dx.doi.org/10.1098/rsos.171622.

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Adenosine is known as an endogenous purine nucleoside and it modulates a wide variety of physiological responses by interacting with adenosine receptors. Among the four adenosine receptor subtypes, the A 3 receptor is of major interest in this study as it is overexpressed in some cancer cell lines. Herein, we have highlighted the strategy of designing the h A 3 receptor targeted novel benzothiazolylquinoline scaffolds. The radioligand binding data of the reported compounds are rationalized with the molecular docking results. Compound 6a showed best potency and selectivity at h A 3 among other

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Tung, Avery, Stacy Herrera, Martin J. Szafran, Kristen Kasza, and Wallace B. Mendelson. "Effect of Sleep Deprivation on Righting Reflex in the Rat Is Partially Reversed by Administration of Adenosine A1 and A2 Receptor Antagonists." Anesthesiology 102, no. 6 (June 1, 2005): 1158–64. http://dx.doi.org/10.1097/00000542-200506000-00015.

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Background Similarities between naturally occurring sleep and general anesthesia suggest that the two states may interact physiologically. The authors have previously demonstrated that sleep deprivation potentiates anesthetic-induced loss of righting reflex (LORR) in rats. One possible mediator for this effect is adenosine, which accumulates in the brains of sleep-deprived animals and reduces anesthetic requirements. The authors tested in rats the hypothesis that potentiating effects of sleep deprivation on LORR can be altered by adenosine A1 and A2a receptor antagonists. Methods Five experime

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