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Adenosine receptor

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https://www.readbyqxmd.com/read/28530470/cd73-controls-extracellular-adenosine-generation-in-the-trigeminal-nociceptive-nerves
#1
X Liu, L Ma, S Zhang, Y Ren, R T Dirksen
Purinergic signaling is involved in pain generation and modulation in the nociceptive sensory nervous system. Adenosine triphosphate (ATP) induces pain via activation of ionotropic P2X receptors while adenosine mediates analgesia via activation of metabotropic P1 receptors. These purinergic signaling are determined by ecto-nucleotidases that control ATP degradation and adenosine generation. Using enzymatic histochemistry, we detected ecto-AMPase activity in dental pulp, trigeminal ganglia (TG) neurons, and their nerve fibers...
June 2017: Journal of Dental Research
https://www.readbyqxmd.com/read/28529533/low-expression-of-cd39-and-cd73-genes-in-centenarians-compared-with-octogenarians
#2
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/28529484/targeting-adenosine-receptors-for-the-treatment-of-cardiac-fibrosis
#3
REVIEW
Elizabeth A Vecchio, Paul J White, Lauren T May
Adenosine is a ubiquitous molecule with key regulatory and cytoprotective mechanisms at times of metabolic imbalance in the body. Among a plethora of physiological actions, adenosine has an important role in attenuating ischaemia-reperfusion injury and modulating the ensuing fibrosis and tissue remodeling following myocardial damage. Adenosine exerts these actions through interaction with four adenosine G protein-coupled receptors expressed in the heart. The adenosine A2B receptor (A2BAR) is the most abundant adenosine receptor (AR) in cardiac fibroblasts and is largely responsible for the influence of adenosine on cardiac fibrosis...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28528302/nanomolar-anti-sickling-compounds-identified-by-ligand-based-pharmacophore-approach
#4
Odailson Santos Paz, Milena de Jesus Pinheiro, Renan Fernandes do Espirito Santo, Cristiane Flora Villarreal, Marcelo Santos Castilho
Adenosine receptors are considered as potential targets for drug development against several diseases. The discovery of subtype 2B adenosine receptors role in erythrocyte sickling process proved its importance to neglected diseases such as sickle cell anemia, which affects approximately 29.000 people around the world, but whose treatment is restricted to just one FDA approved drug (hydroxyurea). In order to widen the therapeutic arsenal available to treat sickle cell anemia patients, it is imperative to identify new lead compounds that modify the sickling course and not just its symptoms...
May 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28527108/increased-expression-of-brain-derived-neurotrophic-factor-transcripts-i-and-vi-camp-response-element-binding-and-glucocorticoid-receptor-in-the-cortex-of-patients-with-temporal-lobe-epilepsy
#5
G A Martínez-Levy, L Rocha, F Rodríguez-Pineda, M A Alonso-Vanegas, A Nani, R M Buentello-García, M Briones-Velasco, D San-Juan, J Cienfuegos, C S Cruz-Fuentes
A body of evidence supports a relevant role of brain-derived neurotrophic factor (BDNF) in temporal lobe epilepsy (TLE). Magnetic resonance data reveal that the cerebral atrophy extends to regions that are functionally and anatomically connected with the hippocampus, especially the temporal cortex. We previously reported an increased expression of BDNF messenger for the exon VI in the hippocampus of temporal lobe epilepsy patients compared to an autopsy control group. Altered levels of this particular transcript were also associated with pre-surgical use of certain psychotropic...
May 19, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28526033/effects-of-exenatide-on-cardiac-function-perfusion-and-energetics-in-type-2-diabetic-patients-with-cardiomyopathy-a-randomized-controlled-trial-against-insulin-glargine
#6
Weena J Y Chen, Michaela Diamant, Karin de Boer, Hendrik J Harms, Lourens F H J Robbers, Albert C van Rossum, Mark H H Kramer, Adriaan A Lammertsma, Paul Knaapen
BACKGROUND: Multiple bloodglucose-lowering agents have been linked to cardiovascular events. Preliminary studies showed improvement in left ventricular (LV) function during glucagon-like peptide-1 receptor agonist administration. Underlying mechanisms, however, are unclear. The purpose of this study was to investigate myocardial perfusion and oxidative metabolism in type 2 diabetic (T2DM) patients with LV systolic dysfunction as compared to healthy controls. Furthermore, effects of 26-weeks of exenatide versus insulin glargine administration on cardiac function, perfusion and oxidative metabolism in T2DM patients with LV dysfunction were explored...
May 19, 2017: Cardiovascular Diabetology
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
#7
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
https://www.readbyqxmd.com/read/28515678/soluble-ectodomain-of-neuroligin-1-decreases-synaptic-activity-by-activating-metabotropic-glutamate-receptor-2
#8
Michelle D Gjørlund, Eva M M Carlsen, Andreas B Kønig, Oksana Dmytrieva, Anders V Petersen, Jacob Jacobsen, Vladimir Berezin, Jean-François Perrier, Sylwia Owczarek
Synaptic cell adhesion molecules represent important targets for neuronal activity-dependent proteolysis. Postsynaptic neuroligins (NLs) form trans-synaptic complexes with presynaptic neurexins (NXs). Both NXs and NLs are cleaved from the cell surface by metalloproteases in an activity-dependent manner, releasing a soluble extracellular fragment and membrane-tethered C-terminal fragment. The cleavage of NL1 depresses synaptic transmission, but the mechanism by which this occurs is unknown. Metabotropic glutamate receptor 2 (mGluR2) are located primarily at the periphery of presynaptic terminals, where they inhibit the formation of cyclic adenosine monophosphate (cAMP) and consequently suppress the release of glutamate and decrease synaptic transmission...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28515278/critical-role-of-p2y12-receptor-in-regulation-of-th17-differentiation-and-experimental-autoimmune-encephalomyelitis-pathogenesis
#9
Chaoyan Qin, Jinfeng Zhou, Yuan Gao, Weiming Lai, Cuixia Yang, Yingying Cai, Shuai Chen, Changsheng Du
Adenosine 5'-diphosphate is a key endogenous cell-signaling molecule that can activate P2 purinergic receptor family members. ADP-P2Y signaling is reported to be associated with inflammation, but its function in T cell differentiation and autoimmune diseases pathogenesis is unclear. In this study, we found that the P2Y12 receptor was upregulated in the peripheral immune tissues of experimental autoimmune encephalomyelitis (EAE) mice. Deficiency of P2Y12 led to a reduced peak severity and cumulative disease score in EAE mice, followed by a dramatic reduction of leukocyte infiltration and less extensive demyelination...
May 17, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28515177/do-%C3%AE-3-adrenoceptor-agonists-cause-urinary-bladder-smooth-muscle-relaxation-by-inhibiting-acetylcholine-release
#10
Katerina Okeke, Stavros Gravas, Martin C Michel
The mechanisms leading to improvement of overactive bladder syndrome upon treatment with a β3-adrenoceptor agonist remain controversial. New research points to a role of inhibition of neuronal acetylcholine release. Whether this occurs by a direct effect on prejunctional β3-adrenoceptors or indirectly by formation of adenosine and activation of A1 adenosine receptors is being discussed.
May 17, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28513806/increased-activity-of-vascular-adenosine-deaminase-in-atherosclerosis-and-therapeutic-potential-of-its-inhibition
#11
Barbara Kutryb-Zajac, Lukasz Mateuszuk, Paulina Zukowska, Agnieszka Jasztal, Magdalena A Zabielska, Marta Toczek, Patrycja Jablonska, Agnieszka Zakrzewska, Barbara Sitek, Jan Rogowski, Romuald Lango, Ewa M Slominska, Stefan Chlopicki, Ryszard T Smolenski
Aims: Extracellular nucleotides and adenosine that are formed or degraded by membrane-bound ecto-enzymes could affect atherosclerosis by regulating the inflammation and thrombosis. This study aimed to evaluate a relation between ecto-enzymes that convert extracellular adenosine triphosphate to adenine dinucleotide phosphate, adenosine monophosphate, adenosine, and inosine on the surface of the vessel wall with the severity or progression of experimental and clinical atherosclerosis. Furthermore, we tested whether the inhibition of adenosine deaminase will block the development of experimental atherosclerosis...
November 1, 2016: Cardiovascular Research
https://www.readbyqxmd.com/read/28512854/mogroside-iiie-attenuates-lps-induced-acute-lung-injury-in-mice-partly-through-regulation-of-the-tlr4-mapk-nf-%C3%AE%C2%BAb-axis-via-ampk-activation
#12
Lijun Tao, Fengyan Cao, Gonghao Xu, Haifeng Xie, Mian Zhang, Chaofeng Zhang
Acute lung injury (ALI) often leads to high mortality, and there is as yet no effective drug treatment. The present study aimed to investigate protective effects of mogroside IIIE (MGIIIE, a cucurbitane-type triterpenoid from Siraitia grosvenorii Fruits) in experimental ALI and its underlying mechanism. MGIIIE (1, 10 0r 20 mg/kg) was orally administered for 1 h before a single intratracheal administration of lipopolysaccharide (LPS, 5 mg/kg). MGIIIE treatment dose-dependently suppressed pulmonary oedema, pro-inflammatory mediators (IL-1β, IL-6, TNF-α and HMGB1) release and higher MPO activity in lung tissues induced by LPS challenge...
May 17, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28512397/leukocyte-expression-of-type-1-and-type-2-purinergic-receptors-and-pro-inflammatory-cytokines-during-total-sleep-deprivation-and-or-sleep-extension-in-healthy-subjects
#13
Mounir Chennaoui, Pierrick J Arnal, Catherine Drogou, Damien Leger, Fabien Sauvet, Danielle Gomez-Merino
The purinergic type P1 (adenosine A1 and A2A) receptors and the type P2 (X7) receptor have been suggested to mediate physiological effects of adenosine and adenosine triphosphate on sleep. We aimed to determine gene expression of A1R (receptor), A2AR, and P2RX7 in leukocytes of healthy subjects during total sleep deprivation followed by sleep recovery. Expression of the pro-inflammatory cytokines IL-1β and TNF-α were also determined as they have been characterized as sleep regulatory substances, via P2RX7 activation...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28511553/whole-blood-platelet-aggregation-test-and-prediction-of-hemostatic-difficulty-after-tooth-extraction-in-patients-receiving-antiplatelet-therapy
#14
Yasushi Nagao, Rikuo Masuda, Akane Ando, Mutsumi Nonaka, Akiko Nishimura, Kinuko Goto, Yasubumi Maruoka, Takehiko Iijima
When patients on antiplatelet therapy (APT) require minor invasive surgery, APT is usually continued to limit the risk of thrombosis. However, the possibility of hemostatic difficulties necessitates the monitoring of platelet aggregation to prevent unexpected bleeding. We examined whether whole blood aggregometry as a point-of-care testing (POCT) could be useful as a tool for predicting hemostatic difficulties. Sixty-five patients receiving APT and 15 patients who were not receiving APT were enrolled in the present study; all patients were scheduled to undergo a tooth extraction...
January 1, 2017: Clinical and Applied Thrombosis/hemostasis
https://www.readbyqxmd.com/read/28509867/supporting-the-identification-of-novel-fragment-based-positive-allosteric-modulators-using-a-supervised-molecular-dynamics-approach-a-retrospective-analysis-considering-the-human-a2a-adenosine-receptor-as-a-key-example
#15
Giuseppe Deganutti, Stefano Moro
Structure-driven fragment-based (SDFB) approaches have provided efficient methods for the identification of novel drug candidates. This strategy has been largely applied in discovering several pharmacological ligand classes, including enzyme inhibitors, receptor antagonists and, more recently, also allosteric (positive and negative) modulators. Recently, Siegal and collaborators reported an interesting study, performed on a detergent-solubilized StaR adenosine A2A receptor, describing the existence of both fragment-like negative allosteric modulators (NAMs), and fragment-like positive allosteric modulators (PAMs)...
May 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28508842/a3-adenosine-receptor-agonist-induce-g1-cell-cycle-arrest-via-cyclin-d-and-cyclin-dependent-kinase-4-pathways-in-ovcar-3-and-caov-4-cell-lines
#16
Hamid Reza Joshaghani, Seyyed Mehdi Jafari, Mahmoud Aghaei, Mojtaba Panjehpour, Hamideh Abedi
AIM OF THE STUDY: The cell cycle, a vital process that involves in cells' growth and division, lies at the heart of cancer. It has been shown that IB-MECA, an A3 adenosine receptor agonist inhibits the proliferation of cancer cells by inducing cell cycle arrest in several tumors. In this study, we evaluated the role of IB-MECA inhibition in cell cycle progression in ovarian cancer cells. MATERIALS AND METHODS: Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay in Caov-4 and OVCAR-3...
January 2017: Journal of Cancer Research and Therapeutics
https://www.readbyqxmd.com/read/28508339/induction-of-hibernation-like-hypothermia-by-central-activation-of-the-a1-adenosine-receptor-in-a-non-hibernator-the-rat
#17
Hiroki Shimaoka, Takayuki Kawaguchi, Kahori Morikawa, Yuuki Sano, Kiyotada Naitou, Hiroyuki Nakamori, Takahiko Shiina, Yasutake Shimizu
Central adenosine A1-receptor (A1AR)-mediated signals play a role in the induction of hibernation. We determined whether activation of the central A1AR enables rats to maintain normal sinus rhythm even after their body temperature has decreased to less than 20 °C. Intracerebroventricular injection of an adenosine A1 agonist, N6-cyclohexyladenosine (CHA), followed by cooling decreased the body temperature of rats to less than 20 °C. Normal sinus rhythm was fundamentally maintained during the extreme hypothermia...
May 15, 2017: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/28507584/effects-of-adenosine-receptor-antagonists-in-mptp-mouse-model-of-parkinson-s-disease-mitochondrial-dna-integrity
#18
Soha S Essawy, Mona Kamal Tawfik, Horya Erfan Korayem
INTRODUCTION: In Parkinson's disease (PD), compelling data indicate a functional link between adenosine/dopamine receptors and the progression of the neurodegenerative process. The present study was carried out to evaluate the effect of the non-selective adenosine receptor (ADR) antagonist caffeine, as well as the selective antagonists 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), an ADRsA1 antagonist, and ((E)-1,3-diethyl-8-(3,4-dimethoxystyryl)-7-methyl-3,7-dihydro-1H-purine-2,6-dione) (KW-6002), an ADRsA2A antagonist, on the prevention of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced Parkinsonism in mice...
April 1, 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28507174/elevated-adenosine-induces-placental-dna-hypomethylation-independent-of-a2b-receptor-signaling-in-preeclampsia
#19
Aji Huang, Hongyu Wu, Takayuki Iriyama, Yujin Zhang, Kaiqi Sun, Anren Song, Hong Liu, Zhangzhe Peng, Lili Tang, Minjung Lee, Yun Huang, Xin Ni, Rodney E Kellems, Yang Xia
Preeclampsia is a prevalent pregnancy hypertensive disease with both maternal and fetal morbidity and mortality. Emerging evidence indicates that global placental DNA hypomethylation is observed in patients with preeclampsia and is linked to altered gene expression and disease development. However, the molecular basis underlying placental epigenetic changes in preeclampsia remains unclear. Using 2 independent experimental models of preeclampsia, adenosine deaminase-deficient mice and a pathogenic autoantibody-induced mouse model of preeclampsia, we demonstrate that elevated placental adenosine not only induces hallmark features of preeclampsia but also causes placental DNA hypomethylation...
May 15, 2017: Hypertension
https://www.readbyqxmd.com/read/28505392/beneficial-effects-of-ginger-zingiber-officinale-roscoe-on-obesity-and-metabolic-syndrome-a-review
#20
REVIEW
Jing Wang, Weixin Ke, Rui Bao, Xiaosong Hu, Fang Chen
In recent years, metabolic syndromes (MetSs), including diabetes mellitus, dyslipidemia, and cardiovascular diseases, have become a common health problem in both developed and developing countries. Accumulating data have suggested that traditional herbs might be able to provide a wide range of remedies in prevention and treatment of MetSs. Ginger (Zingiber officinale Roscoe, Zingiberaceae) has been documented to ameliorate hyperlipidemia, hyperglycemia, oxidative stress, and inflammation. These beneficial effects are mediated by transcription factors, such as peroxisome proliferator-activated receptors, adenosine monophosphate-activated protein kinase, and nuclear factor κB...
May 15, 2017: Annals of the New York Academy of Sciences
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