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https://www.readbyqxmd.com/read/29485875/discovery-of-novel-adenosine-receptor-antagonists-through-a-combined-structure-and-ligand-based-approach-followed-by-molecular-dynamics-investigation-of-ligand-binding-mode
#1
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 A1 ARs offer exciting opportunities for structure-based drug design. In the first part of the present work, Maybridge HitFinder library of 14400 compounds was utilized to apply a combination of structure-based against the crystal structure of A2A AR and ligand-based methodologies...
April 23, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29480441/a1ar-mediated-renal-protection-against-ischemia-reperfusion-injury-is-dependent-on-hsp27-induction
#2
Bin Xiong, Min Li, Shulin Xiang, Lin Han
PURPOSE: A1 adenosine receptor (AR) activation has been demonstrated to attenuate renal ischemia/reperfusion injury (IRI), but the exact mechanism of this protection remains to be well elucidated. METHODS: Male C57BL/6 mice were used in the present study. Expression of heat shock protein (HSP) 27 and HSF-1 were detected using western blot analysis. An RNA interference with adenovirus vector using short hairpin RNA targeting HSP27 was developed. Together with renal IRI model, indicators of renal function, acute tubular necrosis, inflammation and apoptosis were measured in kidneys after 24-h reperfusion...
February 26, 2018: International Urology and Nephrology
https://www.readbyqxmd.com/read/29473361/-effects-of-electroacupuncture-on-the-expression-of-adenosine-receptors-in-the-heart-tissue-of-myocardial-ischemia-rats
#3
Shengfeng Lu, Yuexia Tang, Yajuan Ding, Meiling Yu, Shuping Fu, Bingmei Zhu
OBJECTIVE: To explore the impact of electroacupuncture (EA) on the protein expression of adenosine receptors in the heart of the rats with myocardial ischemia (MI). METHODS: Thirty healthy male SD rats were divided randomly into a control group ( n =6), a model group ( n =12) and an EA group ( n =12). We ligated the left anterior descending artery (LAD) for MI model in the model group and EA group, and exposed the heart after opening the chest without ligation in the control group...
February 12, 2018: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
https://www.readbyqxmd.com/read/29387112/estrogen-stimulates-adenosine-receptor-expression-subtypes-in-human-breast-cancer-mcf-7-cell-line
#4
Azam Mohamadi, Mahmoud Aghaei, Mojtaba Panjehpour
Estrogen is a steroid hormone that plays a key role in the development and regulation of reproductive system. It has been shown that estrogen is related to breast cancer development through binding to its receptors. In order to uncover the estrogen effects on adenosine receptor expression, estrogen-positive MCF-7 cells were used to treat with agonist and antagonist of estrogen and then the mRNA expression of adenosine receptor subtypes were evaluated. Estrogen-positive MCF-7 cells were treated with various concentrations of 17β estradiol (E2) as an estrogen agonist, and ICI 182,780 as an estrogen antagonist...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29345054/isoflurane-anesthesia-in-aged-mice-and-effects-of-a1-adenosine-receptors-on-cognitive-impairment
#5
Chun-Long Zuo, Chun-Man Wang, Jin Liu, Ting Shen, Jiang-Ping Zhou, Xin-Rui Hao, Yi-Zhao Pan, Hua-Cheng Liu, Qing-Quan Lian, Han Lin
AIMS: Isoflurane may not only accelerate the process of Alzheimer's disease (AD), but increase the risk of incidence of postoperative cognitive dysfunction (POCD). However, the underlying mechanisms remain unknown. This study was designed to investigate whether isoflurane contributed to the POCD occurrence through A1 adenosine receptor (A1AR) in aged mice. METHODS: We assessed cognitive function of mice with Morris water maze (MWM) and then measured expression level of two AD biomarkers (P-tau and Aβ) and a subtype of the NMDA receptor (NR2B) in aged wild-type (WT) and homozygous A1 adenosine receptor (A1AR) knockout (KO) mice at baseline and after they were exposed to isoflurane (1...
January 17, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29117994/role-of-adenosine-1a-receptor-signaling-on-gfr-early-after-the-induction-of-sepsis
#6
Jonathan M Street, Erik H Koritzinsky, Tiffany R Bellomo, Xuzhen Hu, Peter S T Yuen, Robert A Star
Sepsis and acute kidney injury (AKI) synergistically increase morbidity and mortality in the ICU. How sepsis reduces GFR and causes AKI is poorly understood; one proposed mechanism includes tubuloglomerular feedback (TGF). When sodium reabsorption by the proximal tubules is reduced in normal animals, the macula densa senses increased luminal sodium chloride, then adenosine 1a receptor (A1aR) signaling triggers tubuloglomerular feedback, reducing GFR through afferent arteriole vasoconstriction. We measured GFR and systemic hemodynamics early during cecal ligation and puncture-induced sepsis in wild-type and A1aR knockout mice...
November 8, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29097738/pharmacologically-induced-reversible-hypometabolic-state-mitigates-radiation-induced-lethality-in-mice
#7
Subhajit Ghosh, Namita Indracanti, Jayadev Joshi, Jharna Ray, Prem Kumar Indraganti
Therapeutic hypothermia has proven benefits in critical care of a number of diseased states, where inflammation and oxidative stress are the key players. Here, we report that adenosine monophosphate (AMP) triggered hypometabolic state (HMS), 1-3 hours after lethal total body irradiation (TBI) for a duration of 6 hours, rescue mice from radiation-induced lethality and this effect is mediated by the persistent hypothermia. Studies with caffeine and (6)N-cyclohexyladenosine, a non-selective antagonist and a selective agonist of adenosine A1 receptor (A1AR) respectively, indicated the involvement of adenosine receptor (AR) signaling...
November 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28895043/effects-of-long-term-caffeine-consumption-on-the-adenosine-a1-receptor-in-the-rat-brain-an-in-vivo-pet-study-with-18-f-cpfpx
#8
Danje Nabbi-Schroeter, David Elmenhorst, Angela Oskamp, Stefanie Laskowski, Andreas Bauer, Tina Kroll
PURPOSE: Caffeine, a nonselective antagonist of adenosine receptors, is the most popular psychostimulant worldwide. Recently, a protective role of moderate chronic caffeine consumption against neurodegenerative diseases such as Alzheimer's and Parkinson's disease has been discussed. Thus, aim of the present study was an in vivo investigation of effects of long-term caffeine consumption on the adenosine A1 receptor (A1AR) in the rat brain. PROCEDURES: Sixteen adult, male rats underwent five positron emission tomography (PET) scans with the highly selective A1AR radioligand [(18)F]CPFPX in order to determine A1AR availability...
September 11, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28836401/purinergic-receptor-expression-and-potential-association-with-human-embryonic-stem-cell-derived-oligodendrocyte-progenitor-cell-development
#9
Shirin Kashfi, Maryam Peymani, Kamran Ghaedi, Hossein Baharvand, Mohammad Hossein Nasr-Esfahani, Mohammad Javan
OBJECTIVES: Due to recent progress in production of human embryonic stem cell-derived oligodendrocyte progenitor cells (hESC-OPCs) for ameliorating myelin disease such as multiple sclerosis (MS) and the role of purinergic signaling in OPCs development, we avaluated the profile of purinergic receptors expression during development of OPCs from hESC. MATERIALS AND METHODS: In this experimental study, we used reverse transcription and quantitative polymerase chain reaction (RT-qPCR) to obtain more information about potential roles of purinergic receptors during in vitro production of hESC-OPCs...
October 2017: Cell Journal
https://www.readbyqxmd.com/read/28676923/biochemical-and-pharmacological-role-of-a-1-adenosine-receptors-and-their-modulation-as-novel-therapeutic-strategy
#10
Katia Varani, Fabrizio Vincenzi, Stefania Merighi, Stefania Gessi, Pier Andrea Borea
Adenosine, the purine nucleoside, mediates its effects through activation of four G-protein coupled adenosine receptors (ARs) named as A1 , A2A , A2B and A3 . In particular, A1 ARs are distributed through the body, primarily inhibitory in the regulation of adenylyl cyclase activity and able to reduce the cyclic AMP levels. Considerable advances have been made in the pharmacological and molecular characterization of A1 ARs, which had been proposed as targets for the discovery and drug design of antagonists, agonists and allosteric enhancers...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28652388/optimization-of-thermolytic-response-to-a1-adenosine-receptor-agonists-in-rats
#11
Isaac R Bailey, Bernard Laughlin, Lucille A Moore, Lori K Bogren, Zeinab Barati, Kelly L Drew
Cardiac arrest is a leading cause of death in the United States, and, currently, therapeutic hypothermia, now called targeted temperature management (TTM), is the only recent treatment modality proven to increase survival rates and reduce morbidity for this condition. Shivering and subsequent metabolic stress, however, limit application and benefit of TTM. Stimulating central nervous system A1 adenosine receptors (A1AR) inhibits shivering and nonshivering thermogenesis in rats and induces a hibernation-like response in hibernating species...
September 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28548869/neurotransmitter-receptor-availability-in-the-rat-brain-is-constant-in-a-24-hour-period
#12
A Oskamp, F Wedekind, T Kroll, D Elmenhorst, A Bauer
Wakefulness and sleep are fundamental characteristics of the brain. We, therefore, hypothesized that transmitter systems contribute to their regulation and will exhibit circadian alterations. We assessed the concentration of various neurotransmitter receptors and transporters including adenosinergic (A1AR, A2AAR, and ENT1), dopaminergic (D1R, D2R, and DAT), and serotonergic (5-HT2AR) target proteins. Adult male Sprague Dawley rats were used and maintained in a 12 h light: 12 h dark cycle (lights on from 07:00 h to 19:00 h)...
May 26, 2017: Chronobiology International
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
#13
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/28447789/exploring-the-role-of-n-6-substituents-in-potent-dual-acting-5-c-ethyltetrazolyladenosine-derivatives-synthesis-binding-functional-assays-and-antinociceptive-effects-in-mice-%C3%A2
#14
Riccardo Petrelli, Mirko Scortichini, Sonja Kachler, Serena Boccella, Carmen Cerchia, Ilaria Torquati, Fabio Del Bello, Daniela Salvemini, Ettore Novellino, Livio Luongo, Sabatino Maione, Kenneth A Jacobson, Antonio Lavecchia, Karl-Norbert Klotz, Loredana Cappellacci
Structural determinants of affinity of N(6)-substituted-5'-C-(ethyltetrazol-2-yl)adenosine and 2-chloroadenosine derivatives at adenosine receptor (AR) subtypes were studied with binding and molecular modeling. Small N(6)-cycloalkyl and 3-halobenzyl groups furnished potent dual acting A1AR agonists and A3AR antagonists. 4 was the most potent dual acting human (h) A1AR agonist (Ki = 0.45 nM) and A3AR antagonist (Ki = 0.31 nM) and highly selective versus A2A; 11 and 26 were most potent at both h and rat (r) A3AR...
May 25, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28373571/recovery-sleep-after-extended-wakefulness-restores-elevated-a1-adenosine-receptor-availability-in-the-human-brain
#15
David Elmenhorst, Eva-Maria Elmenhorst, Eva Hennecke, Tina Kroll, Andreas Matusch, Daniel Aeschbach, Andreas Bauer
Adenosine and functional A1 adenosine receptor (A1AR) availability are supposed to mediate sleep-wake regulation and cognitive performance. We hypothesized that cerebral A1AR availability after an extended wake period decreases to a well-rested state after recovery sleep. [(18)F]CPFPX positron emission tomography was used to quantify A1AR availability in 15 healthy male adults after 52 h of sleep deprivation and following 14 h of recovery sleep. Data were additionally compared with A1AR values after 8 h of baseline sleep from an earlier dataset...
April 18, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28344125/capadenoson-a-clinically-trialed-partial-adenosine-a-1-receptor-agonist-can-stimulate-adenosine-a-2b-receptor-biased-agonism
#16
Jo-Anne Baltos, Elizabeth A Vecchio, Matthew A Harris, Cheng Xue Qin, Rebecca H Ritchie, Arthur Christopoulos, Paul J White, Lauren T May
The adenosine A2B receptor (A2B AR) has been identified as an important therapeutic target in cardiovascular disease, however in vitro and in vivo targeting has been limited by the paucity of pharmacological tools, particularly potent agonists. Interestingly, 2-((6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)-2-pyridinyl)thio)acetamide (BAY60-6583), a potent and subtype-selective A2B AR agonist, has the same core structure as 2-amino-6-[[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methylsulfanyl]-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitril (capadenoson)...
July 1, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28242442/genetic-biomarkers-of-posttraumatic-epilepsy-a-systematic-review
#17
REVIEW
Devyn Cotter, Andrew Kelso, Aidan Neligan
INTRODUCTION: Posttraumatic epilepsy (PTE) is caused by traumatic brain injury (TBI) and is an important contributor to the overall social and economic burden of epilepsy. Epidemiological studies suggest that there is a genetic contribution to the development of PTE. Identification of clinically useful genetic biomarkers is important for advancements in diagnosis and treatment of PTE. METHODS: A systematic review was performed on the existing literature of genetic biomarkers of posttraumatic epilepsy (PTE)...
March 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/28217962/synthesis-and-pharmacological-evaluation-of-identified-and-putative-metabolites-of-the-a1-adenosine-receptor-antagonist-8-cyclopentyl-3-3-fluoropropyl-1-propylxanthine-cpfpx
#18
Marcus H Holschbach, Dirk Bier, Wiebke Sihver, Annette Schulze, Bernd Neumaier
The A1 adenosine receptor (A1 AR) antagonist [(18) F]8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ([(18) F]CPFPX), used in imaging human brain A1 ARs by positron emission tomography (PET), is stable in the brain, but rapidly undergoes transformation into one major (3-(3-fluoropropyl)-8-(3-oxocyclopenten-1-yl)-1-propylxanthine, M1) and several minor metabolites in blood. This report describes the synthesis of putative metabolites of CPFPX as standards for the identification of those metabolites. Analysis by (radio)HPLC revealed that extracts of human liver microsomes incubated with no-carrier-added (n...
May 22, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28202385/long-term-consequences-of-disrupting-adenosine-signaling-during-embryonic-development
#19
REVIEW
Scott A Rivkees, Christopher C Wendler
There is growing evidence that disruption in the prenatal environment can have long-lasting effects on an individual's health in adulthood. Research on the fetal programming of adult diseases, including cardiovascular disease, focuses on epi-mutations, which alter the normal pattern of epigenetic factors such as DNA methylation, miRNA expression, or chromatin modification, rather than traditional genetic alteration. Thus, understanding how in utero chemical exposures alter epigenetics and lead to adult disease is of considerable public health concern...
June 2017: Molecular Aspects of Medicine
https://www.readbyqxmd.com/read/28034618/adenosine-receptors-regulate-susceptibility-to-noise-induced-neural-injury-in-the-mouse-cochlea-and-hearing-loss
#20
Srdjan M Vlajkovic, Kaushi Ambepitiya, Meagan Barclay, Detlev Boison, Gary D Housley, Peter R Thorne
Our previous studies have shown that the stimulation of A1 adenosine receptors in the inner ear can mitigate the loss of sensory hair cells and hearing loss caused by exposure to traumatic noise. Here, we focus on the role of adenosine receptors (AR) in the development of noise-induced neural injury in the cochlea using A1 AR and A2A AR null mice (A1 AR-/- and A2A AR-/- ). Wildtype (WT) and AR deficient mice were exposed to octave band noise (8-16 kHz, 100 dB SPL) for 2 h to induce cochlear injury and hearing loss...
March 2017: Hearing Research
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