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adenosine receptors

N C Gareis, E Angeli, E Huber, N R Salvetti, F M Rodríguez, H H Ortega, G J Hein, F Rey
High-producing dairy cows frequently suffer metabolic alterations that cause different diseases, which could decrease the reproductive efficiency of the herd. Among these reproductive disorders, cystic ovarian disease (COD) has been related to alterations in metabolites and hormonal factors such as insulin, adiponectin and leptin. The aim of this study was to determine the protein expression of adiponectin and some of its downstream targets in ovarian follicles of control cows and cows with clinical diagnosis of COD...
August 7, 2018: Theriogenology
Peyvand Amini, Rachel Wilson, William Koeblitz, Junye Wang, Huiqing Tan, Lijuan Yi, Zachary Stanfield, Andrea Romani, Charles Malemud, Sam Mesiano
Progesterone (P4) acting through the P4 receptor (PR) isoforms, PR-A and PR-B, promotes uterine quiescence for most of pregnancy, in part, by inhibiting the response of myometrial cells to pro-labor inflammatory stimuli. This anti-inflammatory effect is inhibited by phosphorylation of PR-A at serine-344 and -345 (pSer344/345 -PRA). Activation of the cyclic adenosine monophosphate (cAMP) signaling pathway also promotes uterine quiescence and myometrial relaxation. This study examined the cross-talk between P4/PR and cAMP signaling to exert anti-inflammatory actions and control pSer344/345 -PRA generation in myometrial cells...
August 14, 2018: Molecular and Cellular Endocrinology
Sun-Hye Choi, Hyeon-Joong Kim, Hee-Jung Cho, Sang-Deuk Park, Na-Eun Lee, Sung-Hee Hwang, Ik-Hyun Cho, Hongik Hwang, Hyewhon Rhim, Hyoung-Chun Kim, Seung-Yeol Nah
Astrocytes are a unique brain cell-storing glycogen and express lysophosphatidic acid (LPA) receptors. Gintonin is a ginseng-derived exogenous G protein-coupled LPA receptor ligand. Accumulating evidence shows that astrocytes serve as an energy supplier to neurons through astrocytic glycogenolysis under physiological and pathophysiological conditions. However, little is known about the relationships between LPA receptors and astrocytic glycogenolysis or about the roles of LPA receptors in hypoxia and re-oxygenation stresses...
August 16, 2018: Molecular Neurobiology
J H Azambuja, N E Gelsleichter, L R Beckenkamp, I C Iser, M C Fernandes, F Figueiró, A M O Battastini, J N Scholl, F H de Oliveira, R M Spanevello, Jean Sévigny, M R Wink, M A Stefani, H F Teixeira, Elizandra Braganhol
Glioblastoma is the worst and most common primary brain tumor. Here, we demonstrated the role of CD73, an enzyme responsible for adenosine (ADO) production, in glioblastoma progression. ADO increased glioma cell viability via A1 receptor sensitization. CD73 downregulation decreased glioma cell migration and invasion by reducing metalloproteinase-2 and vimentin expression and reduced cell proliferation by 40%, which was related to necrosis and sub-G1 phase blockage of cell cycle. Those effects also involved the stimulation of Akt/NF-kB pathways...
August 16, 2018: Molecular Neurobiology
Anida Hasanovic, Isabelle Mus-Veteau
One of the crucial challenges in the clinical management of cancer is resistance to chemotherapeutics. Multidrug resistance (MDR) has been intensively studied, and one of the most prominent mechanisms underlying MDR is overexpression of adenosine triphosphate (ATP)-binding cassette (ABC) transporters. Despite research efforts to develop compounds that inhibit the efflux activity of ABC transporters and thereby increase classical chemotherapy efficacy, to date, the Food and Drug Administration (FDA) has not approved the use of any ABC transporter inhibitors due to toxicity issues...
August 14, 2018: Cells
Hiba Zaidan, Gokul Ramaswami, Michal Barak, Jin B Li, Inna Gaisler-Salomon
Adenosine to inosine RNA editing is an epigenetic process that entails site-specific modifications in double-stranded RNA molecules, catalyzed by adenosine deaminases acting on RNA (ADARs). Using the multiplex microfluidic PCR and deep sequencing technique, we recently showed that exposing adolescent female rats to chronic unpredictable stress before reproduction affects editing in the prefrontal cortex and amygdala of their newborn offspring, particularly at the serotonin receptor 5-HT2c (encoded by Htr2c) ...
April 2018: Environmental Epigenetics
Michał Załuski, Katarzyna Stanuch, Tadeusz Karcz, Sonja Hinz, Gniewomir Latacz, Ewa Szymańska, Jakub Schabikowski, Agata Doroż-Płonka, Jadwiga Handzlik, Anna Drabczyńska, Christa E Müller, Katarzyna Kieć-Kononowicz
A library of 27 novel amide derivatives of annelated xanthines was designed and synthesized. The new compounds represent 1,3-dipropyl- and 1,3-dibutyl-pyrimido[2,1- f ]purinedione-9-ethylphenoxy derivatives including a CH2 CONH linker between the (CH2 )2 -amino group and the phenoxy moiety. A synthetic strategy to obtain the final products was developed involving solvent-free microwave irradiation. The new compounds were evaluated for their adenosine receptor (AR) affinities. The most potent derivatives contained a terminal tertiary amino function...
June 1, 2018: MedChemComm
Amit N Pandya, Arshi B Baraiya, Hitesh B Jalani, Dhaivat Pandya, Jitendra C Kaila, Sonja Kachler, Veronica Salmaso, Stefano Moro, Karl-Norbert Klotz, Kamala K Vasu
A small-molecule combinatorial library of 24 compounds with 2-aminoimidazole and 2-aminoimidazolyl-thiazole derivatives was synthesized using a 2-chloro trityl resin. The generated compound library was tested against all the human adenosine receptors subtypes. The 2-aminoimidazole derivatives ( 6a-6l ) showed weak to moderate affinity towards the human adenosine receptors. Further modification to 2-aminoimidazolyl-thiazole derivatives ( 12a-12l ) resulted in an improvement of affinity at adenosine A1 , A2A and A3 receptor subtypes...
April 1, 2018: MedChemComm
Barbara Cosimelli, Giovanni Greco, Sonia Laneri, Ettore Novellino, Antonia Sacchi, Simona Collina, Daniela Rossi, Sandro Cosconati, Elisabetta Barresi, Sabrina Taliani, Maria Letizia Trincavelli, Claudia Martini
Three A3 adenosine receptor (AR) antagonists ( 1-3 ) selected from 4-acylamino-6-alkyloxy-2-alkylthiopyrimidines previously investigated by us were modified by inserting a methyl group on their ether or thioether side chains. These compounds gave us the chance to evaluate whether their higher lipophilicity, reduced conformational freedom and chirality might improve the potency towards the A3 AR. Racemic mixtures of 1-3 were resolved using chiral HPLC methods and the absolute configurations of the enantiomers were assigned by chiroptical spectroscopy and density functional theory calculations...
January 1, 2018: MedChemComm
Jie Sun, Ming Zhang, Kun Chen, Beidong Chen, Yanyang Zhao, Huan Gong, Xin Zhao, Ruomei Qi, Eur J Pharmacol
Resveratrol has many beneficial biological actions, including cardiovascular protection and antithrombotic effects. Whether resveratrol inhibits oxidized low-density lipoprotein (ox-LDL)-induced Toll-like receptor 4 (TLR4) expression in activated platelets remains unclear. The present study investigated the effects of resveratrol on the TLR4-mediated inflammatory response in ox-LDL-activated platelets. The results showed that resveratrol suppressed TLR4 expression in ox-LDL- and lipopolysaccharide (LPS)-activated platelets...
August 11, 2018: European Journal of Pharmacology
Fernando Dobrachinski, Rogério R Gerbatin, Gláubia Sartori, Ronaldo M Golombieski, Alfredo Antoniazzi, Cristina W Nogueira, Luiz F Royes, Michele R Fighera, Lisiane O Porciúncula, Rodrigo A Cunha, Félix A A Soares
Traumatic brain injury (TBI) is a leading cause of disability worldwide, triggering chronic neurodegeneration underlying cognitive and mood disorder still without therapeutic prospects. Based on our previous observations that guanosine (GUO) attenuates short-term neurochemical alterations caused by TBI, this study investigated the effects of chronical GUO treatment in behavioral, molecular, and morphological disturbances 21 days after trauma. Rats subject to TBI displayed mood (anxiety-like) and memory dysfunction...
August 13, 2018: Molecular Neurobiology
Iman Azimi, Alice H Bong, Greta X H Poo, Kaela Armitage, Dawn Lok, Sarah J Roberts-Thomson, Gregory R Monteith
Store-operated Ca2+ entry is a pathway that is remodelled in a variety of cancers, and altered expression of the components of store-operated Ca2+ entry is a feature of breast cancer cells of the basal molecular subtype. Studies of store-operated Ca2+ entry in breast cancer cells have used non-specific pharmacological inhibitors, complete depletion of intracellular Ca2+ stores and have mostly focused on MDA-MB-231 cells (a basal B breast cancer cell line). These studies compared the effects of the selective store-operated Ca2+ entry inhibitors Synta66 and YM58483 (also known as BTP2) on global cytosolic free Ca2+ ([Ca2+ ]CYT ) changes induced by physiological stimuli in a different breast cancer basal cell line model, MDA-MB-468...
August 13, 2018: Cellular and Molecular Life Sciences: CMLS
Minna Lahesmaa, Vesa Oikonen, Semi Helin, Pauliina Luoto, Mueez U Din, Alexander Pfeifer, Pirjo Nuutila, Kirsi A Virtanen
PURPOSE: Brown adipose tissue (BAT) has emerged as a potential target to combat obesity and diabetes, but novel strategies to activate BAT are needed. Adenosine and A2A receptor (A2AR) agonism activate BAT in rodents, and endogenous adenosine is released locally in BAT as a by-product of noradrenaline, but physiological data from humans is lacking. The purpose of this pilot study was to investigate the effects of exogenous adenosine on human BAT perfusion, and to determine the density of A2ARs in human BAT in vivo for the first time, using PET/CT imaging...
August 13, 2018: European Journal of Nuclear Medicine and Molecular Imaging
Jianmei Gao, Shuang Liu, Fan Xu, Yuangui Liu, Chun Lv, Yan Deng, Jingshan Shi, Qihai Gong
Oxidative stress-induced neuronal cell damage is a crucial factor in the pathogenesis of mitochondria-associated neurological diseases. Therefore, elimination of overproduction of mitochondrial reactive oxygen species (mtROS) may be a potential strategy for prevention and treatment of neurological diseases. In the present study, the neuroprotective effects of trilobatin (TLB), a novel small molecule monomer derived from Lithocarpus polystachyus Rehd, and its underlying mechanisms were investigated in vitro using hydrogen peroxide (H2 O2 )-induced oxidative stress model in a neuron-like PC12 cell...
2018: Frontiers in Molecular Neuroscience
Marcel Lindemann, Sonja Hinz, Winnie Deuther-Conrad, Vigneshwaran Namasivayam, Sladjana Dukic-Stefanovic, Rodrigo Teodoro, Magali Toussaint, Mathias Kranz, Cathleen Juhl, Jörg Steinbach, Peter Brust, Christa E Müller, Barbara Wenzel
On the basis of a pyrazine core structure, three new adenosine A2B receptor ligands (7a-c) were synthesized containing a 2-fluoropyridine moiety suitable for 18 F-labeling. Compound 7a was docked into a homology model of the A2B receptor based on X-ray structures of the related A2A receptor, and its interactions with the adenosine binding site were rationalized. Binding affinity data were determined at the four human adenosine receptor subtypes. Despite a rather low selectivity regarding the A1 receptor, 7a was radiolabeled as the most suitable candidate (Ki (A2B ) = 4...
July 29, 2018: Bioorganic & Medicinal Chemistry
Jigisha A Patel, Lei Shen, Susan M Hall, Chabha Benyahia, Xavier Norel, Robin J McAnulty, Shahin Moledina, Adam M Silverstein, Brendan J Whittle, Lucie H Clapp
Prostacyclins are extensively used to treat pulmonary arterial hypertension (PAH), a life-threatening disease involving the progressive thickening of small pulmonary arteries. Although these agents are considered to act therapeutically via the prostanoid IP receptor, treprostinil is the only prostacyclin mimetic that potently binds to the prostanoid EP₂ receptor, the role of which is unknown in PAH. We hypothesised that EP₂ receptors contribute to the anti-proliferative effects of treprostinil in human pulmonary arterial smooth muscle cells (PASMCs), contrasting with selexipag, a non-prostanoid selective IP agonist...
August 12, 2018: International Journal of Molecular Sciences
Akie Inami, Hiroshi Kiyono, Yosuke Kurashima
Extracellular nucleotides, such as adenosine triphosphate (ATP), are released from host cells including nerve termini, immune cells, injured or dead cells, and the commensal bacteria that reside in the gut lumen. Extracellular ATP interacts with the host through purinergic receptors, and promotes intercellular and bacteria-host communication to maintain the tissue homeostasis. However, the release of massive concentrations of ATP into extracellular compartments initiates acute and chronic inflammatory responses through the activation of immunocompetent cells (e...
August 12, 2018: International Journal of Molecular Sciences
Michael Mousseau, Nicole E Burma, Kwan Yeop Lee, Heather Leduc-Pessah, Charlie H T Kwok, Allison R Reid, Melissa O'Brien, Boriss Sagalajev, Jo Anne Stratton, Natalya Patrick, Patrick L Stemkowski, Jeff Biernaskie, Gerald W Zamponi, Paul Salo, Jason J McDougall, Steven A Prescott, John R Matyas, Tuan Trang
Chronic joint pain such as mechanical allodynia is the most debilitating symptom of arthritis, yet effective therapies are lacking. We identify the pannexin-1 (Panx1) channel as a therapeutic target for alleviating mechanical allodynia, a cardinal sign of arthritis. In rats, joint pain caused by intra-articular injection of monosodium iodoacetate (MIA) was associated with spinal adenosine 5'-triphosphate (ATP) release and a microglia-specific up-regulation of P2X7 receptors (P2X7Rs). Blockade of P2X7R or ablation of spinal microglia prevented and reversed mechanical allodynia...
August 2018: Science Advances
Xiliang Du, Taiyu Shen, Heyuan Wang, Xia Qin, Dongmei Xing, Qianqian Ye, Zhen Shi, Zhiyuan Fang, Yiwei Zhu, Yuchen Yang, Zhicheng Peng, Chenxu Zhao, Bin Lv, Xiaobing Li, Guowen Liu, Xinwei Li
The inevitable deficiency in nutrients and energy at the onset of lactation requires an optimal adaptation of the hepatic metabolism to overcome metabolic stress. Fatty liver is one of the main health disorders after parturition. Therefore, to investigate changes in hepatic lipid metabolic status and mitochondria in dairy cows with mild fatty liver, liver and blood samples were collected from healthy cows (n = 15) and cows with mild fatty liver (n = 15). To determine the effects of palmitic acids (PA), one of the major component of fatty acids, on lipid metabolism and mitochondria in vitro, calf hepatocytes were isolated from healthy calves and treated with various concentrations of PA (0, 50, 100, and 200 μM)...
August 9, 2018: Journal of Dairy Science
Agbonlahor Okhuarobo, Ighodaro Igbe, Abdulmajid Yahaya, Zakariya Sule
Background The aim of the study was to determine the effect of caffeine on alcohol consumption with or without deprivation and alcohol-induced conditioned place preference. Methods In the present study, we examined the effects of caffeine (2.5, 5 and 10 mg/kg) on alcohol consumption in Wistar rats with or without periods of deprivation in an unlimited-access, two-bottle, free choice drinking procedure after a stable baseline alcohol consumption was established. Conditioned place preference (CPP) was established by intraperitoneal injections of alcohol (2 g/kg) in a 12-day conditioning schedule in mice...
August 13, 2018: Journal of Basic and Clinical Physiology and Pharmacology
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