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https://www.readbyqxmd.com/read/28646346/adenosine-and-sleep
#1
Michael Lazarus, Jiang-Fan Chen, Zhi-Li Huang, Yoshihiro Urade, Bertil B Fredholm
The classic endogenous somnogen adenosine promotes sleep via A1 and A2A receptors. In this chapter, we present an overview of the current knowledge regarding the regulation of adenosine levels, adenosine receptors, and available pharmacologic and genetic tools to manipulate the adenosine system. This is followed by a summary of current knowledge of the role of adenosine and its receptors in the regulation of sleep and wakefulness. Despite strong data implicating numerous brain areas, including the basal forebrain, the tuberomammillary nucleus, the lateral hypothalamus, and the nucleus accumbens, in the adenosinergic control of sleep, the complete neural circuitry in the brain involved in the sleep-promoting effects of adenosine remains unclear...
June 24, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28643232/caffeine-protects-against-anticonvulsant-induced-neurotoxicity-in-the-developing-rat-brain
#2
Stefanie Endesfelder, Ulrike Weichelt, Cornelia Schiller, Marco Sifringer, Ivo Bendix, Christoph Bührer
Phenobarbital is the most commonly used drug for the treatment of neonatal seizures but may induce neurodegeneration in the developing brain. Methylxanthine caffeine is used for the treatment of apnea in newborn infants and appears to be neuroprotective, as shown by antiapoptotic and anti-inflammatory effects in oxidative stress models in newborn rodents and reduced rates of cerebral palsy in human infants treated with caffeine. We hypothesized that caffeine may counteract the proapoptotic effects of phenobarbital in newborn rats...
June 22, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28639411/mapping-the-allosteric-sites-of-the-a2a-adenosine-receptor
#3
Alisha D Caliman, Yinglong Miao, J Andrew McCammon
The A2A adenosine receptor (A2A AR) is a G protein-coupled receptor that is pharmacologically targeted for the treatment of inflammation, sepsis, cancer, neuro-degeneration, and Parkinson's disease. Recently, we applied long-timescale molecular dynamics simulations on two ligand-free receptor conformations, starting from the agonist-bound (PDB ID:3QAK) and antagonist-bound (PDB ID:3EML) X-ray structures. This analysis revealed four distinct conformers of the A2A AR: the active, intermediate 1, intermediate 2, and inactive...
June 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28629145/synthesis-and-evaluation-of-phenylxanthine-derivatives-as-potential-dual-a2ar-antagonists-mao-b-inhibitors-for-parkinson-s-disease
#4
Xuebao Wang, Chao Han, Yong Xu, Kaiqi Wu, Shuangya Chen, Mangsha Hu, Luyao Wang, Yun Ye, Faqing Ye
The aim of this research was to prove the speculation that phenylxanthine (PX) derivatives possess adenosine A2A receptor (A2AR)-blocking properties and to screening and evaluate these PX derivatives as dual A2AR antagonists/MAO-B inhibitors for Parkinson's disease. To explore this hypothesis, two series of PX derivatives were prepared and their antagonism against A2AR and inhibition against MAO-B were determined in vitro. In order to evaluate further the antiparkinsonian properties, pharmacokinetic and haloperidol-induced catalepsy experiments were carried out in vivo...
June 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28628804/neuronal-substrates-of-sleep-homeostasis-lessons-from-flies-rats-and-mice
#5
REVIEW
Jeffrey M Donlea, Md Noor Alam, Ronald Szymusiak
Sleep homeostasis is a fundamental property of vigilance state regulation that is highly conserved across species. Neuronal systems and circuits that underlie sleep homeostasis are not well understood. In Drosophila, a neuronal circuit involving neurons in the ellipsoid body and in the dorsal Fan-shaped body is a candidate for both tracing sleep need during waking and translating it to increased sleep drive and expression. Sleep homeostasis in rats and mice involves multiple neuromodulators acting on multiple wake- and sleep-promoting neuronal systems...
June 16, 2017: Current Opinion in Neurobiology
https://www.readbyqxmd.com/read/28626529/photoaffinity-labeling-of-the-human-a2a-adenosine-receptor-and-cross-link-position-analysis-by-mass-spectrometry
#6
Hideyuki Muranaka, Takaki Momose, Chiaki Handa, Tomonaga Ozawa
Photoaffinity labeling (PAL) is widely used for the identification of ligand-binding proteins and elucidation of ligand-binding sites. PAL has also been employed for the characterization of G protein-coupled receptors (GPCRs); however, a limited number of reports has successfully identified their cross-linked amino acids. This report is the first of its kind to determine the cross-link position of the human A2A adenosine receptor by PAL with the novel diazirine-based photoaffinity probe 9.
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28606618/hypoxic-postconditioning-attenuates-apoptosis-via-activation-of-adenosine-a2a-receptors-on-dermal-microvascular-endothelial-cells-of-human-flaps
#7
Jiankun Cao, Wenzhi Li, Chao Cui, Binbin Li, Yi Xin, Lun Cai, Zhizhong Gong, Huang Lin
BACKGROUND: In recent years, many studies have demonstrated that endogenous adenosine induced by ischemia postconditioning reduces apoptosis in various models, but no study has clearly elucidated the effects of hypoxic postconditioning (HPC) in human dermal microvascular endothelial cells (HDMECs) of flaps, and the subtype of adenosine receptors involved remains unknown. In our study, we sought to identify the role of adenosine A2a receptor in the antiapoptotic effects of HPC. MATERIALS AND METHODS: The HDMECs were isolated from human upper eyelid tissue...
May 10, 2017: Journal of Surgical Research
https://www.readbyqxmd.com/read/28604342/role-of-adenosine-receptors-in-the-adipocyte-macrophage-interaction-during-obesity
#8
Miguel Meriño, Lautaro Briones, Verónica Palma, Kurt Herlitz, Carlos Escudero
Lipoinflamation is the inflammation generated in the adipose tissue. It can contribute to the development of insulin resistance. The lipoinflammation-associated mechanisms are related to the function of adipocytes and macrophages present in the adipose tissue. In this regard, the level of nucleoside adenosine is increased in individuals with obesity. Causes or consequences of this increase are unknown. Although, adenosine activating its receptors (A1, A2A, A2B and A3) is able to differentially modulate the function of adipocytes and macrophages, in order to avoid the reduction of insulin sensitivity and generate an anti-inflammatory state in subject with obesity...
June 2017: Endocrinología, diabetes y nutrición
https://www.readbyqxmd.com/read/28592285/blockade-of-adenosine-a2a-receptor-enhances-cd8-t-cells-response-and-decreases-regulatory-t-cells-in-head-and-neck-squamous-cell-carcinoma
#9
Si-Rui Ma, Wei-Wei Deng, Jian-Feng Liu, Liang Mao, Guang-Tao Yu, Lin-Lin Bu, Ashok B Kulkarni, Wen-Feng Zhang, Zhi-Jun Sun
BACKGROUND: Cancer immunotherapy offers a promising approach in cancer treatment. The adenosine A2A receptor (A2AR) could protect cancerous tissues from immune clearance via inhibiting T cells response. To date, the role of A2AR in head and neck squamous cell carcinoma (HNSCC) has not been investigated. Here, we sought to explore the expression and immunotherapeutic value of A2AR blockade in HNSCC. METHODS: The expression of A2AR was evaluated by immunostaining in 43 normal mucosae, 48 dysplasia and 165 primary HNSCC tissues...
June 7, 2017: Molecular Cancer
https://www.readbyqxmd.com/read/28590753/the-1-2-4-triazolo-4-3-a-pyrazin-3-one-as-a-versatile-scaffold-for-the-design-of-potent-adenosine-human-receptor-antagonists-structural-investigations-to-target-the-a2a-receptor-subtype
#10
Matteo Falsini, Lucia Squarcialupi, Daniela Catarzi, Flavia Varano, Marco Betti, Diego Dal Ben, Gabriella Marucci, Michela Buccioni, Rosaria Volpini, Teresa De Vita, Andrea Cavalli, Vittoria Colotta
In this work, we describe the identification of the 1,2,4-triazolo[4,3-a]pyrazin-3-one as a new versatile scaffold for the development of adenosine human (h) receptor antagonists. The new chemotype ensued from a molecular simplification approach applied to our previously reported 1,2,4-triazolo[4,3-a]quinoxalin-1-one series. Hence, a set of novel 8-amino-2-aryl-1,2,4-triazolopyrazin-3-one derivatives, featured by different substituents on the 2-phenyl ring (R) and at position 6 (R6), was synthesized with the main purpose of targeting the hA2A adenosine receptor (AR)...
June 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28583861/genetic-deletion-of-gpr52-enhances-the-locomotor-stimulating-effect-of-an-adenosine-a2a-receptor-antagonist-in-mice-a-potential-role-of-gpr52-in-the-function-of-striatopallidal-neurons
#11
Keiji Nishiyama, Hirobumi Suzuki, Minoru Maruyama, Tomoki Yoshihara, Hiroyuki Ohta
G protein-coupled receptor 52 (GPR52) is largely co-expressed with dopamine D2 receptor (DRD2) in the striatum and nucleus accumbens, and this expression pattern is similar to that of adenosine A2A receptor (ADORA2A). GPR52 has been proposed as a therapeutic target for positive symptoms of schizophrenia, based on observations from pharmacological and transgenic mouse studies. However, the physiological role of GPR52 in dopaminergic functions in the basal ganglia remains unclear. Here, we used GPR52 knockout (KO) mice to examine the role of GPR52 in dopamine receptor-mediated and ADORA2A-mediated locomotor activity and dopamine receptor signaling...
June 2, 2017: Brain Research
https://www.readbyqxmd.com/read/28582704/a-novel-antagonist-of-the-immune-checkpoint-protein-adenosine-a2a-receptor-restores-tumor-infiltrating-lymphocyte-activity-in-the-context-of-the-tumor-microenvironment
#12
Melanie Mediavilla-Varela, Julio Castro, Alberto Chiappori, David Noyes, Dalia C Hernandez, John Stagg, Scott J Antonia
BACKGROUND: Therapeutic strategies targeting immune checkpoint proteins have led to significant responses in patients with various tumor types. The success of these studies has led to the development of various antibodies/inhibitors for the different checkpoint proteins involved in immune evasion of the tumor. Adenosine present in high concentrations in the tumor microenvironment activates the immune checkpoint adenosine A2a receptor (A2aR), leading to the suppression of antitumor responses...
June 2, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28579949/commentary-adenosine-a2a-receptor-blockade-prevents-rotenone-induced-motor-impairment-in-a-rat-model-of-parkinsonism
#13
COMMENT
Marina F de Souza, José M M Bispo, Pollyana C Leal, Auderlan M de Gois, José R Dos Santos
No abstract text is available yet for this article.
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28577977/zonisamide-ameliorates-levodopa-induced-dyskinesia-and-reduces-expression-of-striatal-genes-in-parkinson-model-rats
#14
Mitsuaki Oki, Satoshi Kaneko, Satoshi Morise, Norihiro Takenouchi, Takanori Hashizume, Ayako Tsuge, Masataka Nakamura, Reika Wate, Hirofumi Kusaka
To investigate the difference in results according to the mode of levodopa administration and the effect of zonisamide (ZNS), we analyzed the mRNA expression of dopaminergic and non-dopaminergic receptors in the striatum of Parkinson model rats in relation to the development of levodopa-induced dyskinesia (LID). Unilateral Parkinson model rats were subdivided into 4 groups and treated as follows: no medication (group N), continuous levodopa infusion (group C), intermittent levodopa injection (group I), and intermittent levodopa and ZNS injection (group Z)...
May 31, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28554875/cd39-limits-p2x7-receptor-inflammatory-signaling-and-attenuates-sepsis-induced-liver-injury
#15
Luiz Eduardo Baggio Savio, Paola de Andrade Mello, Vanessa R Figliuolo, Thiago F de Avelar Almeida, Patrícia T Santana, Suellen D S Oliveira, Claudia L M Silva, Linda Feldbrügge, Eva Csizmadia, Richard D Minshall, Maria Serena Longhi, Yan Wu, Simon C Robson, Robson Coutinho-Silva
BACKGROUND & AIMS: The severity of sepsis can be linked to excessive inflammatory responses resulting in hepatic injury with progressive cholestasis. Monocyte/macrophages have been linked to the pathogenesis of cholestasis, cellular injury, and liver failure. P2X7 receptor activation by extracellular ATP (eATP) exacerbates inflammation by augmenting cytokine production; while CD39 scavenges eATP to generate adenosine, thereby limiting P2X7 activation and resulting in A2A receptor stimulation...
May 26, 2017: Journal of Hepatology
https://www.readbyqxmd.com/read/28547175/influence-of-body-mass-index-and-type-of-low-level-exercise-on-the-side-effect-profile-of-regadenoson
#16
Carlos Salgado-Garcia, Amelia Jimenez-Heffernan, Juana Lopez-Martin, Manuela Molina-Mora, Tarik Aroui, Elena Sanchez de Mora, Carlos Ramos-Font, Francisco Rivera de Los Santos, Carlos Ruiz-Frutos
PURPOSE: Regadenoson, an A2A adenosine receptor pharmacologic stress agent for radionuclide myocardial perfusion imaging (MPI), is administered as a single, fixed dose. We studied the side effect profile of regadenoson combined with two types of low-level exercise, according to body mass index (BMI). METHODS: Three hundred and fifty-six patients (46.1% men, mean age 67.7±10.7 years, range 31-90 years) underwent regadenoson stress testing combined with low-level exercise...
May 25, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28540569/altered-purinergic-signaling-in-uridine-adenosine-tetraphosphate-induced-coronary-relaxation-in-swine-with-metabolic-derangement
#17
Zhichao Zhou, Oana Sorop, Vincent J de Beer, Ilkka Heinonen, Caroline Cheng, A H Jan Danser, Dirk J Duncker, Daphne Merkus
We previously demonstrated that uridine adenosine tetraphosphate (Up4A) induces potent and partially endothelium-dependent relaxation in the healthy porcine coronary microvasculature. We subsequently showed that Up4A-induced porcine coronary relaxation was impaired via downregulation of P1 receptors after myocardial infarction. In view of the deleterious effect of metabolic derangement on vascular function, we hypothesized that the coronary vasodilator response to Up4A is impaired in metabolic derangement, and that the involvement of purinergic receptor subtypes and endothelium-derived vasoactive factors (EDVFs) is altered...
May 24, 2017: Purinergic Signalling
https://www.readbyqxmd.com/read/28533515/perivascular-aqp4-dysregulation-in-the-hippocampal-ca1-area-after-traumatic-brain-injury-is-alleviated-by-adenosine-a2a-receptor-inactivation
#18
Zi-Ai Zhao, Ping Li, Shi-Yang Ye, Ya-Lei Ning, Hao Wang, Yan Peng, Nan Yang, Yan Zhao, Zhuo-Hang Zhang, Jiang-Fan Chen, Yuan-Guo Zhou
Traumatic brain injury (TBI) can induce cognitive dysfunction due to the regional accumulation of hyperphosphorylated tau protein (p-tau). However, the factors that cause p-tau to concentrate in specific brain regions remain unclear. Here, we show that AQP4 polarization in the perivascular astrocytic end feet was impaired after TBI, which was most prominent in the ipsilateral brain tissue surrounding the directly impacted region and the contralateral hippocampal CA1 area and was accompanied by increased local p-tau, changes in dendritic spine density and morphology, and upregulation of the adenosine A2A receptor (A2AR)...
May 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28529533/low-expression-of-cd39-and-cd73-genes-in-centenarians-compared-with-octogenarians
#19
Almudena Crooke, Juan Martínez-Henández, Joaquín Martínez-López, Alfonso Cruz-Jentoft, Fernando Huete-Toral, Jesús Pintor
Ageing involves a progressive decline of the body's regulatory systems including immune system. Adenosine regulates immune function by interaction with its receptors, mainly adenosine A2A receptor, present on the surface of immune cells. Furthermore, cellular response to this nucleoside is highly dependent on its extracellular concentration that is regulated by ecto-enzymes such as CD39 and CD73. Therefore, the aim of this study was to investigate the effect of age on adenosine A2A receptor, CD39 and CD73 gene expression...
2017: Immunity & Ageing: I & A
https://www.readbyqxmd.com/read/28517175/comparison-of-the-human-a2a-adenosine-receptor-recognition-by-adenosine-and-inosine-new-insights-from-supervised-molecular-dynamics-simulations
#20
Giuseppe Deganutti, Ajith Welihinda, Stefano Moro
Adenosine deaminase converts adenosine to inosine. Differently by adenosine, modest attention has been dedicated to the physiological roles of inosine. Nevertheless, recent studies demonstrate that inosine has neuroprotective, cardioprotective immunomodulatory, and antidepressive effects. It has been recently reported by Welihinda and collaborators that inosine is a less potent agonist than adenosine at the A2A AR. To better depict the differences in receptor recognition mechanism of both adenosine and inosine, in this work supervised molecular dynamics (SuMD) simulations have been performed and analyzed...
May 18, 2017: ChemMedChem
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