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adenosine a2a receptor

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https://www.readbyqxmd.com/read/28934532/preemptive-caffeine-administration-blocks-the-increase-in-postoperative-pain-caused-by-previous-sleep-loss-in-the-rat-a-potential-role-for-preoptic-adenosine-a2a-receptors-in-sleep-pain-interactions
#1
Viviane S Hambrecht-Wiedbusch, Maya Gabel, Linda J Liu, John P Imperial, Angelo V Colmenero, Giancarlo Vanini
Sleep and pain are reciprocally related, but the precise mechanisms underlying this relationship are poorly understood. This study used a rat model of surgical pain to examine the effect of previous sleep loss on postoperative pain and tested the hypothesis that preoptic adenosinergic mechanisms regulate sleep-pain interactions. Relative to ad libitum sleep, 6 hours of total sleep deprivation prior to a surgical incision significantly enhanced postoperative mechanical hypersensitivity in the affected paw and prolonged the time to recovery from surgery...
September 1, 2017: Sleep
https://www.readbyqxmd.com/read/28928465/endothelial-adenosine-a2a-receptor-mediated-glycolysis-is-essential-for-pathological-retinal-angiogenesis
#2
Zhiping Liu, Siyuan Yan, Jiaojiao Wang, Yiming Xu, Yong Wang, Shuya Zhang, Xizhen Xu, Qiuhua Yang, Xianqiu Zeng, Yaqi Zhou, Xuejiao Gu, Sarah Lu, Zhongjie Fu, David J Fulton, Neal L Weintraub, Ruth B Caldwell, Wenbo Zhang, Chaodong Wu, Xiao-Ling Liu, Jiang-Fan Chen, Aftab Ahmad, Ismail Kaddour-Djebbar, Mohamed Al-Shabrawey, Qinkai Li, Xuejun Jiang, Ye Sun, Akrit Sodhi, Lois Smith, Mei Hong, Yuqing Huo
Adenosine/adenosine receptor-mediated signaling has been implicated in the development of various ischemic diseases, including ischemic retinopathies. Here, we show that the adenosine A2a receptor (ADORA2A) promotes hypoxia-inducible transcription factor-1 (HIF-1)-dependent endothelial cell glycolysis, which is crucial for pathological angiogenesis in proliferative retinopathies. Adora2a expression is markedly increased in the retina of mice with oxygen-induced retinopathy (OIR). Endothelial cell-specific, but not macrophage-specific Adora2a deletion decreases key glycolytic enzymes and reduces pathological neovascularization in the OIR mice...
September 19, 2017: Nature Communications
https://www.readbyqxmd.com/read/28921456/blood-brain-barrier-in-a-haemophilus-influenzae-type-a-in-vitro-infection-role-of-adenosine-receptors-a2a-and-a2b
#3
N Caporarello, M Olivieri, M Cristaldi, M Scalia, M A Toscano, C Genovese, A Addamo, M Salmeri, G Lupo, C D Anfuso
The blood-brain barrier (BBB) is mainly made up of tightly connected microvascular endothelial cells (BMECs), surrounded by pericytes (BMPCs) which regulate BBB tightness by providing soluble factors that control endothelial proliferation. Haemophilus influenzae type a (Hia) is able to reach the BBB, crossing it, thus causing meningitis. In this study, by using an in vitro model of BBB, performed with human BMECs and human BMPCs in co-culture, we demonstrated that, after Hia infection, the number of hBMPCs decreased whereas the number of hBMECs increased in comparison with non-infected cells...
September 18, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28890385/reduced-coronary-reactive-hyperemia-in-mice-was-reversed-by-the-soluble-epoxide-hydrolase-inhibitor-t-aucb-role-of-adenosine-a2a-receptor-and-plasma-oxylipins
#4
Ahmad Hanif, Matthew L Edin, Darryl C Zeldin, Christophe Morisseau, John R Falck, Catherine Ledent, Stephen L Tilley, Mohammed A Nayeem
Coronary reactive hyperemia (CRH) protects the heart against ischemia. Adenosine A2AAR-deficient (A2AAR(-/-)) mice have increased expression of soluble epoxide hydrolase (sEH); the enzyme responsible for breaking down the cardioprotective epoxyeicosatrienoic acids (EETs) to dihydroxyeicosatrienoic acids (DHETs). sEH-inhibition enhances CRH, increases EETs, and modulates oxylipin profiles. We investigated the changes of oxylipins and their impact on CRH in A2AAR(-/-) and wild type (WT) mice. We hypothesized that the attenuated CRH in A2AAR(-/-) mice is mediated by changes in oxylipin profiles, and that it can be reversed by either sEH- or ω-hydroxylases-inhibition...
July 2017: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/28884118/the-role-of-adenosine-a2a-receptor-cyp450s-and-ppars-in-the-regulation-of-vascular-tone
#5
REVIEW
Maan T Khayat, Mohammed A Nayeem
Adenosine is an endogenous mediator involved in a myriad of physiologic functions, including vascular tone regulation. It is also implicated in some pathologic conditions. Four distinct receptor subtypes mediate the effects of adenosine, such as its role in the regulation of the vascular tone. Vascular tone regulation is a complex and continuous process which involves many mechanisms and mediators that are not fully disclosed. The vascular endothelium plays a pivotal role in regulating blood flow to and from all body organs...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28881253/5-substituted-2-benzylidene-1-tetralone-analogues-as-a1-and-or-a2a-antagonists-for-the-potential-treatment-of-neurological-conditions
#6
H D Janse van Rensburg, G Terre'Blanche, M M van der Walt, L J Legoabe
Adenosine A1 and A2A receptors are attracting great interest as drug targets for their role in cognitive and motor deficits, respectively. Antagonism of both these adenosine receptors may offer therapeutic benefits in complex neurological diseases, such as Alzheimer's and Parkinson's disease. The aim of this study was to explore the affinity and selectivity of 2-benzylidene-1-tetralone derivatives as adenosine A1 and A2A receptor antagonists. Several 5-hydroxy substituted 2-benzylidene-1-tetralone analogues with substituents on ring B were synthesized and assessed as antagonists of the adenosine A1 and A2A receptors via radioligand binding assays...
August 30, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28875031/serial-millisecond-crystallography-of-membrane-and-soluble-protein-microcrystals-using-synchrotron-radiation
#7
Jose M Martin-Garcia, Chelsie E Conrad, Garrett Nelson, Natasha Stander, Nadia A Zatsepin, James Zook, Lan Zhu, James Geiger, Eugene Chun, David Kissick, Mark C Hilgart, Craig Ogata, Andrii Ishchenko, Nirupa Nagaratnam, Shatabdi Roy-Chowdhury, Jesse Coe, Ganesh Subramanian, Alexander Schaffer, Daniel James, Gihan Ketwala, Nagarajan Venugopalan, Shenglan Xu, Stephen Corcoran, Dale Ferguson, Uwe Weierstall, John C H Spence, Vadim Cherezov, Petra Fromme, Robert F Fischetti, Wei Liu
Crystal structure determination of biological macromolecules using the novel technique of serial femtosecond crystallography (SFX) is severely limited by the scarcity of X-ray free-electron laser (XFEL) sources. However, recent and future upgrades render microfocus beamlines at synchrotron-radiation sources suitable for room-temperature serial crystallography data collection also. Owing to the longer exposure times that are needed at synchrotrons, serial data collection is termed serial millisecond crystallography (SMX)...
July 1, 2017: IUCrJ
https://www.readbyqxmd.com/read/28870576/istradefylline-improves-daytime-sleepiness-in-patients-with-parkinson-s-disease-an-open-label-3-month-study
#8
Keisuke Suzuki, Masayuki Miyamoto, Tomoyuki Miyamoto, Tomoyuki Uchiyama, Yuka Watanabe, Shiho Suzuki, Taro Kadowaki, Hiroaki Fujita, Takeo Matsubara, Hirotaka Sakuramoto, Koichi Hirata
BACKGROUND: Istradefylline, a selective adenosine A2A receptor antagonist, has been reported to improve daily "off time" and motor symptoms in patients with Parkinson's disease (PD). However, the effect of istradefylline on sleep problems has not been thoroughly investigated. METHODS: We evaluated the effect of istradefylline on daytime sleepiness, sleep disturbances, and motor symptoms in 22 PD patients who were affected by the wearing off phenomenon in an open-label, 3-month study...
September 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28864241/theacrine-a-purine-alkaloid-from-camellia-assamica-var-kucha-with-a-hypnotic-property-via-the-adenosine-system
#9
Haoyi Qiao, Xiansheng Ye, Xiaoyu Bai, Jun He, Tingli Li, Jia Zhang, Weiku Zhang, Jiekun Xu
Theacrine (l,3,7,9-tetramethyluric acid), a purine alkaloid from Camellia assamica var. kucha, has diverse pharmacological properties, including sedative and hypnotic activities, anti-inflammatory and analgesic activities, antidepressant effects, and a protective effect against stress-provoked liver damage. The present study aims to investigate the possible mechanism of the hypnotic activity of theacrine. The results revealed that theacrine significantly enhanced pentobarbital-induced sleep at a dose of 3.0mg/kg (i...
August 31, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28858361/quantification-of-green-fluorescent-protein-gfp-tagged-membrane-proteins-by-capillary-gel-electrophoresis
#10
Azeem Danish, Sang-Yong Lee, Christa E Müller
A fast and robust procedure for the quantification of GFP-tagged membrane proteins in cell homogenates was developed employing capillary gel electrophoresis coupled to laser-induced fluorescence detection (CGE-LIF). The new method was found to be highly sensitive and applicable to structurally diverse membrane proteins including synaptic vesicle protein 2A (SV2A), adenosine A2A receptor (A2AAR), and connexin 43 (Cx43). Quantification of SV2A and A2AAR using radioligand binding assays confirmed the results obtained with CGE-LIF...
August 31, 2017: Analyst
https://www.readbyqxmd.com/read/28857746/purinergic-regulation-of-brain-catecholamine-neurotransmission-in-vivo-electrophysiology-and-microdialysis-study-in-rats
#11
Eliyahu Dremencov, Lubica Lacinova, Gunnar Flik, Joost Ha Folgering, Thomas Ifh Cremers, Ben Hc Westerink
It was previously reported that adenosine-2A (A2A) receptors interact with dopamine-2 (D2) receptors on a molecular level. The aim of the current study was to investigate the functional output of this interaction. In vivo microdialysis was used to assess the effects of an antagonist of A2A receptors, ZM 241385, and an antagonist of D2 receptors haloperidol, either alone or in combination, on brain catecholamine levels. It was found that ZM 241385 did not alter catecholamine levels by its own, but potentiated haloperidol-induced dopamine and norepinephrine release in the nucleus accumbens and prefrontal cortex, respectively...
August 31, 2017: General Physiology and Biophysics
https://www.readbyqxmd.com/read/28844595/cognitive-impairments-associated-with-alterations-in-synaptic-proteins-induced-by-the-genetic-loss-of-adenosine-a2a-receptors-in-mice
#12
Maria Moscoso-Castro, Marc López-Cano, Irene Gracia-Rubio, Francisco Ciruela, Olga Valverde
The study of psychiatric disorders usually focuses on emotional symptoms assessment. However, cognitive deficiencies frequently constitute the core symptoms, are often poorly controlled and handicap individual's quality of life. Adenosine receptors, through the control of both dopamine and glutamate systems, have been implicated in the pathophysiology of several psychiatric disorders such as schizophrenia and attention deficit/hyperactivity disorder. Indeed, clinical data indicate that poorly responsive schizophrenia patients treated with adenosine adjuvants show improved treatment outcomes...
August 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28842709/the-parkinson-s-disease-associated-gpr37-receptor-interacts-with-striatal-adenosine-a2a-receptor-controlling-its-cell-surface-expression-and-function-in-vivo
#13
Xavier Morató, Rafael Luján, Marc López-Cano, Jorge Gandía, Igor Stagljar, Masahiko Watanabe, Rodrigo A Cunha, Víctor Fernández-Dueñas, Francisco Ciruela
G protein-coupled receptor 37 (GPR37) is an orphan receptor associated to Parkinson's disease (PD) neuropathology. Here, we identified GPR37 as an inhibitor of adenosine A2A receptor (A2AR) cell surface expression and function in vivo. In addition, we showed that GPR37 and A2AR do oligomerize in the striatum. Thus, a close proximity of GPR37 and A2AR at the postsynaptic level of striatal synapses was observed by double-labelling post-embedding immunogold detection. Indeed, the direct receptor-receptor interaction was further substantiated by proximity ligation in situ assay...
August 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28837114/polydeoxyribonucleotide-ameliorates-lipopolysaccharide-induced-lung-injury-by-inhibiting-apoptotic-cell-death-in-rats
#14
Jin An, So Hee Park, Il-Gyu Ko, Jun-Jang Jin, Lakkyong Hwang, Eun-Sang Ji, Sang-Hoon Kim, Chang-Ju Kim, So Young Park, Jae-Joon Hwang, Cheon Woong Choi
Lung injury is characterized by diffuse lung inflammation, alveolar-capillary destruction, and alveolar flooding, resulting in respiratory failure. Polydexyribonucleotide (PDRN) has an anti-inflammatory effect, decreasing inflammatory cytokines, and suppressing apoptosis. Thus, we investigated its efficacy in the treatment of lung injury, which was induced in rats using lipopolysaccharide (LPS). Rats were randomly divided into three groups according to sacrifice time, and each group split into control, lung injury-induced, and lung injury-induced + PDRN-treated groups...
August 24, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28835798/discovery-of-potent-and-selective-a2a-antagonists-with-efficacy-in-animal-models-of-parkinson-s-disease-and-depression
#15
Sujay Basu, Dinesh A Barawkar, Vidya Ramdas, Minakshi Naykodi, Yogesh D Shejul, Meena Patel, Sachin Thorat, Anil Panmand, K Kashinath, Rajesh Bonagiri, Vandna Prasad, Ganesh Bhat, Azfar Quraishi, Sumit Chaudhary, Amol Magdum, Ashwinkumar V Meru, Indraneel Ghosh, Ravi K Bhamidipati, Amol A Raje, Vamsi L M Madgula, Siddhartha De, Sreekanth R Rouduri, Venkata P Palle, Anita Chugh, Narayanan Hariharan, Kasim A Mookhtiar
Adenosine A2A receptor (A2AAdoR) antagonism is a nondopaminergic approach to Parkinson's disease treatment that is under development. Earlier we had reported the therapeutic potential of 7-methoxy-4-morpholino-benzothiazole derivatives as A2AAdoR antagonists. We herein described a novel series of [1,2,4]triazolo[5,1-f]purin-2-one derivatives that displays functional antagonism of the A2A receptor with a high degree of selectivity over A1, A2B, and A3 receptors. Compounds from this new scaffold resulted in the discovery of highly potent, selective, stable, and moderate brain penetrating compound 33...
August 10, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28830843/inhibition-of-tpa-induced-hemorrhagic-transformation-involves-adenosine-a2b-receptor-activation-after-cerebral-ischemia
#16
Qiang Li, Xiaoning Han, Xi Lan, Xiaohua Hong, Qian Li, Yufeng Gao, Tianqi Luo, Qingwu Yang, Raymond C Koehler, Yu Zhai, Jinyuan Zhou, Jian Wang
Tissue plasminogen activator (tPA) is administered after ischemic stroke to dissolve intravascular clots, but its use can lead to hemorrhagic transformation (HT). Therapeutic strategies to reduce hemorrhagic complications of tPA might be of benefit for stroke patients. Adenosine A2b receptor (A2bR) plays pivotal roles in regulating vascular protection in peripheral organs. This study explored whether A2bR agonist BAY 60-6583 reduces hemorrhage risk after tPA usage. Using a rat transient middle cerebral artery occlusion model, we showed that mRNA and protein expression of A2bR increased to a greater extent after ischemia-reperfusion than did expression of the other three adenosine receptors (A1, A2a, and A3)...
August 19, 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/28807491/adenosine-a2a-receptor-signaling-affects-il-21-il-22-cytokines-and-gata3-t-bet-transcription-factor-expression-in-cd4-t-cells-from-a-btbr-t-itpr3tf-j-mouse-model-of-autism
#17
Sheikh F Ahmad, Mushtaq A Ansari, Ahmed Nadeem, Saleh A Bakheet, Mashal M Almutairi, Sabry M Attia
Autism is a complex heterogeneous neurodevelopmental disorder; previous studies have identified altered immune responses among individuals diagnosed with autism. An imbalance in the production of pro- and anti-inflammatory cytokines and transcription factors plays a role in neurodevelopmental behavioral and autism disorders. BTBR T(+) Itpr3tf/J (BTBR) mice are used as a model for autism, as they exhibit social deficits, communication deficits, and repetitive behaviors compared with C57BL/6J (B6) mice. The adenosine A2A receptor (A2AR) appears to be a potential target for the improvement of behavioral, inflammatory, immune, and neurological disorders...
August 9, 2017: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/28801916/adenosine-and-dopamine-oppositely-modulate-a-hyperpolarization-activated-current-ih-in-chemosensory-neurons-of-the-rat-carotid-body-in-co-culture
#18
Min Zhang, Cathy Vollmer, Colin A Nurse
Adenosine and dopamine (DA) act as neurotransmitters or neuromodulators at the carotid body (CB) chemosensory synapse, however, their mechanisms of action are not fully understood. Using a functional co-culture model of rat CB chemoreceptor (type I) cell clusters and juxtaposed afferent petrosal neurons (PNs), we tested the hypothesis that adenosine and DA act postsynaptically to modulate a hyperpolarization-activated, cyclic nucleotide-gated (HCN) cation current (Ih ). In whole-cell recordings from hypoxia-responsive PNs, cAMP mimetics enhanced Ih whereas the HCN blocker ZD7288 (2 μm) reversibly inhibited Ih ...
August 12, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28795281/selective-a2a-receptor-antagonist-sch-58261-modulates-striatal-oxidative-stress-and-alleviates-toxicity-induced-by-3-nitropropionic-acid-in-male-wistar-rats
#19
Cristiani F Bortolatto, Angélica S Reis, Mikaela P Pinz, Guilherme T Voss, Renata L Oliveira, Ane G Vogt, Silvane Roman, Cristiano R Jesse, Cristiane Luchese, Ethel A Wilhelm
The aim of the present study was to investigate the effects of SCH58261, a selective adenosine A2A receptor antagonist, on striatal toxicity induced by 3-nitropropionic acid (3-NP) in rats. The experimental protocol consisted of 10 administrations (once a day) of SCH58261 (0.01 or 0.05 mg/kg/day, intraperitoneal, i.p.). From 7th to 10th day, 3-NP (20 mg/kg/day, i.p.) was injected 1 h after SCH58261 administration. Twenty-four hours after the last 3-NP injection, the body weight gain, locomotor activity (open-field test), motor coordination (rotarod test), striatal succinate dehydrogenase (SDH) activity and parameters linked to striatal oxidative status were evaluated in rats...
August 9, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28789895/imidazo-1-2-%C3%AE-pyridines-possess-adenosine-a1-receptor-affinity-for-the-potential-treatment-of-cognition-in-neurological-disorders
#20
Roslyn Lefin, Mietha M van der Walt, Pieter J Milne, Gisella Terre'Blanche
Previous research has shown that bicyclic 6:5-fused heteroaromatic compounds with two N-atoms have variable degrees of adenosine A1 receptor antagonistic activity. Prompted by this imidazo[1,2-α]pyridine analogues were synthesized and evaluated for their adenosine A1 and A2A receptor affinity via radioligand binding studies and subjected to a GTP shift assay to determine its adenosine A1 receptor agonistic or antagonistic functionality. Imidazo[1,2-α]pyridine, the parent scaffold, was found devoid of affinity for the adenosine A1 and A2A receptors...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
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