Alveolar Epithelial A2B Adenosine Receptors in Pulmonary Protection during Acute Lung Injury | The Journal of Immunology
A2A adenosine receptor, A2B adenosine receptor, and A3 adenosine receptor (15). Both the A2A adenosine receptor and the A2B ... Inhalational treatment of ALI with the A2B adenosine receptor agonist BAY 60-6583. (A) Experimental set-up: C57/B6 mice matched ... Adenosine can signal through four distinct G protein-coupled adenosine receptors, including the A1 adenosine receptor, ... In addition to A2B adenosine receptor signaling, many studies have implicated the A2A adenosine receptor in attenuating lung ...http://www.jimmunol.org/content/195/4/1815
Medicinal chemistry and pharmacology of A2B adenosine receptors | Pubblicazioni Scientifiche Unicam
Hence, A2B adenosine receptor agonists could be useful in the treatment of cardiac diseases like hypertension or myocardial ... A3/A2B = 360). Among non-xanthine derivs. very promising are substituted purines, in which combination of appropriate ... The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven ... The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven ...https://pubblicazioni.unicam.it/handle/11581/242340
A.sub.2B adenosine receptor antagonists - Patent # 7125993 - PatentGenius
A.sub.2B adenosine receptor antagonists, having the structure of Formula I or Formula II: ##STR00001## by cyclizing a compound ... A.sub.2A and A.sub.2B adenosine receptors are coupled to Gs proteins and thus agonists for A.sub.2A adenosine receptor (such as ... 1 mM EDTA and 10 mM MgCl.sub.2 for CHO-A3) supplemented with 1 Unit/mL adenosine deaminase. The assays were incubated for ... A.sub.1 and A.sub.3 adenosine receptors are coupled to Gi proteins and thus agonists for A.sub.1 adenosine receptor (such as ...http://www.patentgenius.com/patent/7125993.html
Molecules | Free Full-Text | Structural Probing and Molecular Modeling of the A3 Adenosine Receptor: A Focus on Agonist Binding
A2B and A3, which belong to the G protein-coupled receptor (GPCR) superfamily. The human A3AR (hA3AR) subtype is implicated in ... elucidate the binding of agonists to the A3AR and discuss the challenges associated with an accurate prediction of the receptor ... Therefore, hA3AR modulators, and in particular agonists, are sought for their potential application as anti-inflammatory, ... Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, ...http://www.mdpi.com/1420-3049/22/3/449
Federal Register :: Prospective Grant of Start-Up Exclusive Evaluation Option License Agreement: A3 Adenosine...
7. U.S. Provisional Application 62/033,723, filed August 6, 2014, titled "A3 Adenosine Receptor Agonists" [HHS Ref. No. E-210- ... 1. U.S. Patent 8,735,407, issued May 27, 2014, titled "Purine Derivatives As A3 Adenosine Receptor-Selective Agonists" [HHS Ref ... 6. U.S. Provisional Application 61/909,742, filed November 27, 2013, titled "A3 Adenosine Receptor Agonists" [HHS Ref. No. E- ... The subject inventions describe selective A3 Adenosine Receptor (A3AR) agonists, and their in vivo activity reducing or ...https://www.federalregister.gov/documents/2014/12/09/2014-28749/prospective-grant-of-start-up-exclusive-evaluation-option-license-agreement-a3-adenosine-receptor
Advances in drug discovery: Can-Fite moves towards opening Phase 3 study of adenosine A3 receptor agonist, CF101 in rheumatoid...
Can-Fite moves towards opening Phase 3 study of adenosine A3 receptor agonist, CF101 in rheumatoid arthritis ... A3 receptor expression will be determined prior to dosing and correlated with efficacy. Of interest, Can-Fite is developing a ... A3 receptors are over-expressed in rheumatoid arthritis and this correlates with lower disease activity suggesting a possible ... Can-Fite is developing A3 agonist, CF101 for rheumatoid arthritis and psoriasis. ...http://leaddiscovery.blogspot.co.uk/2015/01/can-fite-moves-towards-opening-phase-3.html
A3 adenosine receptors and mitogen-activated protein kinases in lung injury following in vivo reperfusion | Springer for...
Introduction Although activation of A3adenosine receptors attenuates reperfusion lung injury and associated apoptosis, the ... N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. J Med Chem 2005, 48: 1745- ... we compared the effect of the A3 adenosine agonist IB-MECA with the newly synthesized, highly selective A3 adenosine receptor ... Molecular cloning and characterization of an adenosine receptor: the A3adenosine receptor. Proc Natl Acad Sci USA 1992, 89: ...https://rd.springer.com/article/10.1186/cc4893
Adenosine A3 receptor - Wikipedia
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. In a mouse model of ... adenosine receptor". Mol. Pharmacol. 63 (5): 1021-31. doi:10.1124/mol.63.5.1021. PMID 12695530. "Adenosine Receptors: A3". ...https://en.wikipedia.org/wiki/Adenosine_A3_receptor
The Activation Of A3 Adenosine Receptor Inhibits Retinal Ganglion Cell Apoptosis | IOVS | ARVO Journals
The potential neuroprotective effect of the A3 adenosine receptor agonist 2-Cl-IB-MECA was assessed using three different ... Immunohistology confirmed the presence of the A3 adenosine receptor in RGC layer. However, the expression of A3 adenosine ... These results suggest that the A3 adenosine receptor is down regulated in RGC layer by chronic OHT. Moreover, the agonist 2-Cl- ... DARC imaging showed that the A3 adenosine receptor agonist 2-Cl-IB-MECA significantly reduced RGC apoptosis compared to control ...https://iovs.arvojournals.org/article.aspx?articleid=2360861
"Pharmacological and Therapeutic Effects of A3 Adenosine Receptor (A3AR" by Bruce T. Liang
Highly selective A3AR agonists have been synthesized and molecular recognition in the binding site has been characterized. The ... The receptor is overexpressed in inflammatory and cancer cells, while low expression is found in normal cells, rendering the ... Currently, A3AR agonists are being developed for the treatment of inflammatory diseases including rheumatoid arthritis and ... The Gi-coupled A3 adenosine receptor (A3AR) mediates anti-inflammatory, anticancer and anti-ischemic protective effects. ...https://opencommons.uconn.edu/uchcres_articles/159/
CP-532,903 - Wikipedia
CP-532,903 is a selective adenosine A3 subtype receptor agonist. It has antiinflammatory effects and has been shown to reduce ... The A3 adenosine receptor agonist CP-532,903 [N6-(2,5-dichlorobenzyl)-3'-aminoadenosine-5'-N-methylcarboxamide] protects ... Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic ... Activation of the A(3) adenosine receptor suppresses superoxide production and chemotaxis of mouse bone marrow neutrophils. ...https://en.wikipedia.org/wiki/CP-532,903
Meloxicam, an inhibitor of cyclooxygenase-2, increases the level of serum G-CSF and might be usable as an auxiliary means in G...
... pharmacological therapy of the acute radiation disease using a cyclooxygenase-2 inhibitor and an adenosine A3 receptor agonist ... Inhibition of cyclooxygenase-2 promotes the stimulatory action of adenosine A₃ receptor agonist on hematopoiesis in sublethally ... Activation of adenosine A(3) receptors potentiates stimulatory effects of IL-3, SCF, and GM-CSF on mouse granulocyte-macrophage ... Synergistic effect of granulocyte colony-stimulating factor and drugs elevating extracellular adenosine on neutrophil ...https://www.semanticscholar.org/paper/Meloxicam%2C-an-inhibitor-of-cyclooxygenase-2%2C-the-of-Hofer-Posp%C3%AD%C5%A1il/d5d1accab340618172eeda44371979d48db710db
Research Pipeline II: Oral Therapeutics | Springer for Research & Development
IB-MECA, an A3 adenosine receptor agonist prevents bone resorption in rats with adjuvant induced arthritis. Clin Exp Rheumatol ... Antiinflammatory effect of A3 adenosine receptor agonists in murine autoimmune arthritis models. J Rheumatol. 2005;32(3):469-76 ... Tolerability, pharmacokinetics and concentration-dependent hemodynamic effects of oral CF101, an A3 adenosine receptor agonist ... Clinical evidence for utilization of the A3 adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II ...https://rd.springer.com/chapter/10.1007/978-1-4471-4432-8_18
Synthesis, Biological Properties, and Molecular Modeling Investigation of the First Potent, Selective, and Water-Soluble Human...
... and Water-Soluble Human A3 Adenosine Receptor Antagonist ... K B value 3 Adenosine Receptor Antagonist CHO cells hA 3 ... receptors (,10000-fold) ever reported. A Schild analysis of the antagonism by ,b,4 ,/b,of agonist-induced inhibition of cAMP ... adenosine receptor First Potent Schild analysis K i 0.01 nM hA 3 receptor Molecular Modeling Investigation pyrimidine ... A new, highly potent, selective, and water-soluble antagonist of the hA,sub,3,/sub, adenosine receptor was synthesized and ...https://figshare.com/articles/Synthesis_Biological_Properties_and_Molecular_Modeling_Investigation_of_the_First_Potent_Selective_and_Water-Soluble_Human_A_sub_3_sub_Adenosine_Receptor_Antagonist/3681432/1
Can-Fite Reports First Quarter 2018 Financial Results and Provides Clinical Update | Business Wire
Keratinocytes by the A3 Adenosine Receptor Agonist Piclidenoson" (https://www.hindawi.com/journals/jir/aip/2310970/) in the ... and the relationship between outcomes and A3 adenosine receptor expression. The Company anticipates data release to occur in ...https://www.businesswire.com/news/home/20180601005332/en/Can-Fite-Reports-Quarter-2018-Financial-Results-Clinical
Phyllis B. Silver -BIO-PROTOCOL
Inhibition of experimental auto-immune uveitis by the A3 adenosine receptor agonist CF101. Int J Mol Med 28(5): 727-731. ... Spontaneous Ocular Autoimmunity in Mice Expressing a Transgenic T Cell Receptor Specific to Retina: A Tool to Dissect ... Breakdown of immune privilege and spontaneous autoimmunity in mice expressing a transgenic T cell receptor specific for a ... Microbiota-Dependent Activation of an Autoreactive T Cell Receptor Provokes Autoimmunity in an Immunologically Privileged Site. ...https://bio-protocol.org/UserHome.aspx?id=1005276
Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor | Garvan Institute of Medical...
... the endogenous adenosine by increasing the number of adenosine receptors instead of administering an adenosine receptor agonist ... the endogenous adenosine by increasing the number of adenosine receptors instead of administering an adenosine receptor agonist ... A novel adenosine A3 receptor can mediate this protective function. One approach to achieve cardioprotection is to enhance ... A novel adenosine A3 receptor can mediate this protective function. One approach to achieve cardioprotection is to enhance ...https://www.garvan.org.au/research/publications/1164
Superior Control of Blood Glucose in Diabetes Treatment - Patent application
Use of a3 adenosine receptor agonist in osteoarthritis treatment. New patent applications in this class:. ... Novel uses of glp-1 receptor agonists in patients treated with insulin and/or suffering from type 1 diabetes. ...http://www.patentsencyclopedia.com/app/20110183901
IMIDAZOQUINOLINE DERIVATIVES AS ADENOSINE A3 RECEPTOR LIGANDS - Patent application
Purinone derivatives as hm74a agonists. New patent applications in this class:. Date. Title. ... 0160]Human Adenosine A2b Receptor Binding Binding protocol: incubate 20.8 μg of membranes (human A2b adenosine receptors ... 0158]Human Adenosine A2a Receptor Binding Binding protocol: Incubate 7 μg of membranes (human A2a adenosine receptors ... Patent application title: IMIDAZOQUINOLINE DERIVATIVES AS ADENOSINE A3 RECEPTOR LIGANDS. Inventors: Peter ARANYI Laszlo BALAZS ...http://www.patentsencyclopedia.com/app/20080255110
Faculty Publications | West Coast University
... thioadenosines A3 Adenosine Receptor Agonists. Chemical Biology & Drug Design, 75(6), 607-618. DOI: 10.1111/j.1747-0285.2010. ... Recent advances on QSAR-based profiling of agonist and antagonist A3 adenosine receptor ligands. Current Topics in Medicinal ... Desirability-based simultaneous analysis of binding and relative efficacy profiles of A3 adenosine receptor agonists. ... A Prioritization Tool for Dual A2A Adenosine Receptor Antagonists / Monoamine Oxidase B Inhibitors. Current Pharmaceutical ...https://westcoastuniversity.edu/academics/faculty-publications.html
Protocols and Video Articles Authored by Brandon K. Harvey (Translated to Portuguese)
Dec, 2006 , Pubmed ID: 17016854 Adenosine A3 receptor (A3R) agonists have been shown to reduce cardiac and lung injury, but the ... Activation of Adenosine A3 Receptors Reduces Ischemic Brain Injury in Rodents Journal of Neuroscience Research. ... and the long acting GLP-1 receptor agonist exendin-4 (Ex-4) is currently used as an anti-diabetic drug. GLP-1 receptors are ... The protective effect of selective A3R agonist chloro-N(6)-(3-iodo-benzyl)-adenosine-5'-N-methyluronamide (Cl-IB-MECA) was ...https://www.jove.com/author/Brandon+K._Harvey?language=Portuguese
COMPOSITIONS AND METHODS FOR TREATING CONDITIONS ASSOCIATED WITH CERAMIDE BIOSYNTHESIS - Patent application
Use of adenosine a3 receptor agonists for treatment of neuropathic pain. Top Inventors for class "Drug, bio-affecting and body ... opioid receptor such as a μ-opioid receptor, δ-opioid receptor or a κ-opioid receptor. Determining whether the test agent ... μ-opioid receptors, δ-opioid receptors or κ-opioid receptors. In various embodiments, the opioid drug may be morphine. In ... that targets one or more of μ-opioid receptors, δ-opioid receptors or κ-opioid receptors. In various embodiments, the opioid ...http://www.patentsencyclopedia.com/app/20120328602
Publikācijas - Latvijas Organiskās sintēzes institūts
Structure-activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors ... Novel selective melanocortin 4 receptor antagonist induces food intake after peripheral administration. Biochem. Biophys. Res. ...http://www.osi.lv/publikacijas/?op&pg=9&gads=2003
Can-Fite BioPharma - Home Page
The pipeline drugs are synthetic, highly specific agonists and an allosteric modulator, all target the A3 adenosine receptor. ... The company technology platform is based on the finding that the Gi protein coupled A3 adenosine receptor (A3AR) is highly ...http://canfite.com
All Products|Plerixafor,GDC-0980,PF-04691502,AZD2281,Bimatoprost,R788,PCI32765,MG-132,Daptomycin.|Shanghai loulan biological...
IB-MECA is an agonist of the adenosine A3 receptor with EC50 values of 0.11 μM. IC50 value: 0.11 μM (EC50)  Target: ... adenosine A3 receptor in vitro: IB-MECA has been shown to play important roles in cell proliferation and apoptosis in a variety ... that was the reason for the presence of functional A3 adenosine receptor on the cell lines. IB-MECA significantly reduced cell ... fot androgen receptor)  Target: androgen receptor in vitro: RAD140 demonstrates excellent affinity for the androgen receptor ...http://bioll.com/Product.asp?b=&s=&page=128