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adenosine a2a receptor

Mabrouka Salem, Alain Tremblay, Julie Pelletier, Bernard Robaye, Jean Sévigny
In this study, we investigated the role of extracellular nucleotides in chemokine (KC, MIP-2, MCP-1, and CXCL10) expression and secretion by murine primary intestinal epithelial cells (IECs) with a focus on P2Y6 receptors. qRT-PCR experiments showed that P2Y6 was the dominant nucleotide receptor expressed in mouse IEC. In addition, the P2Y6 ligand UDP induced expression and secretion of CXCL10. For the other studies, we took advantage of mice deficient in P2Y6 ( P2ry6 -/- ). Similar expression levels of P2Y1 , P2Y2 , P2X2, P2X4, and A2A were detected in P2ry6 -/- and WT IEC...
2018: Frontiers in Pharmacology
Hyun-Kyung Do, Joong-Hoon Lee, Jae-Young Lim
OBJECTIVE: Polydeoxyribonucleotide as adenosine receptor (A2A ) agonist has been used in plastic surgery and dermatology related to its regenerative property. The aim of this pilot study is to evaluate the safety and efficacy of polydeoxynucleotide injection in patients with rotator cuff tears by a variety of outcomes including pain, disability, physical performance test, and ultrasonography (US). METHODS: Seventeen patients (9 men, 8 women, age: 57.9 ± 9.1) with partial-thickness tear of supraspinatus tendon were evaluated in a prospective, open-label, and pre-and-post study...
March 14, 2018: Physician and Sportsmedicine
Angel Guerrero
In the last 20 years, an increasing interest of medicinal chemists on the development of potent and selective agonists and antagonists of adenosine receptors has been noticed due to the large impact they have shown in a variety of important biological processes and diseases. Among these, it should be mentioned vasodilation, inflammation, cancer, wound healing, ischemia reperfusion injury, Parkinson disease, infectious diseases, and other CNS disorders. In this review, I will provide an update of the structures of the A2A agonists known, their selectivity versus other adenosine receptors, and their latest therapeutic applications...
March 12, 2018: Current Medicinal Chemistry
Wei Bai, Ping Li, Ya-Lei Ning, Yan Peng, Ren-Ping Xiong, Nan Yang, Xing Chen, Yuan-Guo Zhou
Glutamate transporters (EAATs) on cerebral vascular endothelial cells play an important role in maintaining glutamate homeostasis in the brain. The dysfunction of endothelial EAATs is an important reason for the dramatically elevated brain glutamate levels after brain injury, such as traumatic brain injury (TBI). The adenosine A2A receptor (A2A R) plays an important role in regulating the brain glutamate level after brain injury; however, researchers have not clearly determined whether this role was related to its ability to regulate endothelial EAATs...
March 8, 2018: Biochemical and Biophysical Research Communications
Marco Betti, Daniela Catarzi, Flavia Varano, Matteo Falsini, Katia Varani, Fabrizio Vincenzi, Diego Dal Ben, Catia Lambertucci, Vittoria Colotta
A new series of amino-3,5-dicyanopyridines (3-28) as analogues of the adenosine hA2B receptor agonist BAY60-6583 (compound 1) was synthesized. All the compounds that interact with the hA2B adenosine receptor display EC50 values in the range 9-350 nM behaving as partial agonists, with the only exception being the 2-{[4-(4-acetamidophenyl)-6-amino-3,5-dicyanopyridin-2-yl]thio}acetamide (8) which shows a full agonist profile. Moreover, the 2-[(1H-imidazol-2-yl)methylthio)]-6-amino-4-(4-cyclopropylmethoxy-phenyl)pyridine-3,5-dicarbonitrile (15) turns out to be 3-fold more active than 1 although less selective...
March 6, 2018: European Journal of Medicinal Chemistry
Maryam Akhtari, Seyed Jalal Zargar, Mahdi Mahmoudi, Mahdi Vojdanian, Alireza Rezaeimanesh, Ahmadreza Jamshidi
Macrophages play an important role in the ankylosing spondylitis (AS) auto-inflammatory responses and fibrocartilage destruction. Adenosine is a key modulator of inflammatory conditions. The various effects of adenosine are mediated by its interaction with adenosine receptors (AR). In this study, we investigated the mRNA expression of A1 , A2A , A2B , and A3 adenosine receptors, ectonucleoside triphosphate diphosphohydrolase-1 (CD39), and ecto-5'-nucleotidase (CD73) in the monocyte-derived macrophages from AS patients in comparison to healthy controls...
March 9, 2018: Clinical Rheumatology
Yan Xia, Xiliang Zheng, Erkang Wang, Dongfeng Li, Ruibin Hou, Jin Wang
Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, termed A1 , A2A , A2B and A3 , which belong to the G-protein-coupled receptor superfamily. The human A3 AR (hA3 AR) subtype is implicated in several cytoprotective functions. Therefore, hA3 AR modulators, and in particular agonists, are sought for their potential application as anti-inflammatory, anti-cancer and cardioprotective agents. Here, we prepared novel adenosine derivatives with indole moiety as hA3 AR ligands...
February 2018: Royal Society Open Science
Astrid Nehlig
Most individuals adjust their caffeine intake according to the objective and subjective effects induced by the methylxanthine. However, to reach the desired effects, the quantity of caffeine consumed varies largely among individuals. It has been known for decades that the metabolism, clearance, and pharmacokinetics of caffeine is affected by many factors such as age, sex and hormones, liver disease, obesity, smoking, and diet. Caffeine also interacts with many medications. All these factors will be reviewed in the present document and discussed in light of the most recent data concerning the genetic variability affecting caffeine levels and effects at the pharmacokinetic and pharmacodynamic levels that both critically drive the level of caffeine consumption...
April 2018: Pharmacological Reviews
Wen Huang, Shunjie Bai, Xuzheng Zuo, Weiju Tang, Pengfei Chen, Xiuying Chen, Gong Wang, Haoxiang Wang, Peng Xie
Microglial activation-mediated inflammatory damage to oligodendrocytes is a key step in the etiology of ischemic white matter lesions. The adenosine A1 receptor (A1R) and adenosine A2a receptor (A2aR) have been reported to regulate the activation of microglia, however, the underlying mechanisms remain elusive. Thus, the present study used a microglia/oligodendrocyte co‑culture model exposed to low glucose/hypoxia, and treated with agonists/antagonists of A1R and A2aR to investigate the role of A1R and A2aR...
March 7, 2018: International Journal of Molecular Medicine
Peng-Zhi Chen, Wen-Juan He, Zhi-Ru Zhu, Guo-Ji E, Gang Xu, De-Wei Chen, Yu-Qi Gao
Hypobaric hypoxia (HH) at high altitudes leads to a wide range of cognitive impairments which can handicap human normal activities and performances. However, the underlying mechanism is still unclear. Adenosine A2A receptors (A2A Rs) of the brain are pivotal to synaptic plasticity and cognition. Besides, insult-induced up-regulation of A2A R regulates neuroinflammation and therefore induces brain damages in various neuropathological processes. The present study was designed to determine whether A2A R-mediate neuroinflammation involves in cognitive impairments under acute HH...
February 28, 2018: Behavioural Brain Research
Safa Bouabid, Fu-Ming Zhou
The indirect pathway striatal medium spiny projection neurons (iMSNs) are critical to motor and cognitive brain functions. These neurons express a high level of cAMP-increasing adenosine A2a receptors (A2aRs). However, the potential effects of cAMP production on iMSN spiking activity have not been established, and recording identified iMSNs in freely moving animals is challenging. Here we show that in the transgenic mice expressing cAMP-producing G protein Gs -coupled designer receptor exclusively activated by designer drug (Gs-DREADD) in iMSNs, the baseline spike firing in MSNs is normal, indicating DREADD expression does not affect the normal physiology of these neurons...
March 3, 2018: Journal of Neurochemistry
Livio Luongo, Daniela Salvemini
No abstract text is available yet for this article.
February 27, 2018: Brain, Behavior, and Immunity
Estefanía Moreno, Júlia Canet, Eduard Gracia, Carme Lluís, Josefa Mallol, Enric I Canela, Antoni Cortés, Vicent Casadó
Adenosine is an endogenous purine nucleoside that acts in all living systems as a homeostatic network regulator through many pathways, which are adenosine receptor (AR)-dependent and -independent. From a metabolic point of view, adenosine deaminase (ADA) is an essential protein in the regulation of the total intracellular and extracellular adenosine in a tissue. In addition to its cytosolic localization, ADA is also expressed as an ecto-enzyme on the surface of different cells. Dipeptidyl peptidase IV (CD26) and some ARs act as binding proteins for extracellular ADA in humans...
2018: Frontiers in Pharmacology
Shu-Qing Chen, Ze-Shi Wang, Yi-Xiao Ma, Wei Zhang, Jian-Liang Lu, Yue-Rong Liang, Xin-Qiang Zheng
As the population ages, neurodegenerative diseases such as Parkinson's disease (PD) and Alzheimer's disease (AD) impose a heavy burden on society and families. The pathogeneses of PD and AD are complex. There are no radical cures for the diseases, and existing therapeutic agents for PD and AD have diverse side effects. Tea contains many bioactive components such as polyphenols, theanine, caffeine, and theaflavins. Some investigations of epidemiology have demonstrated that drinking tea can decrease the risk of PD and AD...
February 25, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Gemma Navarro, Arnau Cordomí, Marc Brugarolas, Estefanía Moreno, David Aguinaga, Laura Pérez-Benito, Sergi Ferre, Antoni Cortés, Vicent Casadó, Josefa Mallol, Enric I Canela, Carme Lluís, Leonardo Pardo, Peter J McCormick, Rafael Franco
BACKGROUND: G-protein-coupled receptor (GPCR) heteromeric complexes have distinct properties from homomeric GPCRs, giving rise to new receptor functionalities. Adenosine receptors (A1 R or A2A R) can form A1 R-A2A R heteromers (A1 -A2A Het), and their activation leads to canonical G-protein-dependent (adenylate cyclase mediated) and -independent (β-arrestin mediated) signaling. Adenosine has different affinities for A1 R and A2A R, allowing the heteromeric receptor to detect its concentration by integrating the downstream Gi - and Gs -dependent signals...
February 28, 2018: BMC Biology
Kei-Ichi Nakashima, Keiichiro Iwao, Toshihiro Inoue, Akira Haga, Takayuki Tsutsumi, Miyuki Inoue Mochita, Tomokazu Fujimoto, Hidenobu Tanihara
Among candidate neuroprotective agents, adenosine is thought to be a possible treatment for central nervous system disorders. Adenosine elicits biological effects through four G protein-coupled receptors (A1 , A2A , A2B , and A3 ). The A2A and A2B receptors stimulate adenylyl cyclase (AC) and increase cyclic adenosine monophosphate (cAMP) levels, whereas A1 and A3 receptors inhibit AC and decrease cAMP levels. Several studies have investigated the effects of adenosine receptors (AdoRs) in glaucoma, because modulation of A1 , A2A , or A3 receptor regulates intraocular pressure...
February 24, 2018: Experimental Eye Research
Panagiotis Lagarias, Eleni Vrontaki, George Lambrinidis, Dimitrios Stamatis, Marino Convertino, Gabriella Ortore, Thomas Mavromoustakos, Karl-Norbert Klotz, Antonios Kolocouris
An intense effort is made by pharmaceutical and academic research laboratories to identify and develop selective antagonists for each adenosine receptor (AR) subtype as potential clinical candidates for "soft" treatment of various diseases. Crystal structures of subtypes A2A and A1ARs offer exciting opportunities for structure-based drug design. In the first part of the present work, Maybridge HitFinderTM library of 14400 compounds was utilized to apply a combination of structure-based against the crystal structure of A2AAR and ligand-based methodologies...
February 27, 2018: Journal of Chemical Information and Modeling
Jie Lv
Neural progenitor cells (NPCs) play a key role not only in the maintenance of the adult central nervous system (CNS) but also in the ability to recover from injury and disease. In this study, we established a 96-well-based screening system to screen small molecules modulating the proliferation of NPCs. A compound library composed of 1280 compounds was screened. We found that the A1 adenosine receptor agonist cyclopentyladenosine (CPA) and the A2a adenosine receptor agonist CGS-21680 increased proliferation of NPCs...
February 21, 2018: Brain Research
Chithra Devi Palani, Lalitha Ramanathapuram, Aroonwan Lam-Ubol, Zoya B Kurago
Patient treatment for oral squamous cell carcinoma (OSCC) not associated with Human papillomavirus remains problematic. OSCC microenvironment is typically inflamed and colonized by microorganisms, providing ligands for toll-like receptors (TLR). In immune cells TLR2 and TLR4 activate NF-kB and extracellular signal regulated kinase (ERK)1/2 pathways, leading to upregulation of inhibitory adenosine receptors A2a and A2b, and reduction in stimulatory A1 and A3. How TLR and adenosine receptors function in SCC cells is not understood...
January 23, 2018: Oncotarget
Brian C Shonesy, Walker P Parrish, Hala K Haddad, Jason R Stephenson, Rita Báldi, Rebecca J Bluett, Christian R Marks, Samuel W Centanni, Oakleigh M Folkes, Keeley Spiess, Shana M Augustin, Ken Mackie, David M Lovinger, Danny G Winder, Sachin Patel, Roger J Colbran
BACKGROUND: Endocannabinoid signaling plays an important role in regulating synaptic transmission in the striatum, a brain region implicated as a central node of dysfunction in autism spectrum disorder. Deficits in signaling mediated by the endocannabinoid 2-arachidonoylglycerol (2-AG) have been reported in mouse models of autism spectrum disorder, but a causal role for striatal 2-AG deficiency in phenotypes relevant to autism spectrum disorder has not been explored. METHODS: Using conditional knockout mice, we examined the electrophysiological, biochemical, and behavioral effects of 2-AG deficiency by deleting its primary synthetic enzyme, diacylglycerol lipase α (DGLα), from dopamine D1 receptor-expressing or adenosine A2a receptor-expressing medium spiny neurons (MSNs) to determine the role of 2-AG signaling in striatal direct or indirect pathways, respectively...
December 28, 2017: Biological Psychiatry
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