purinergic p1 receptor antagonists
Summary: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
Cronstein B, Naime D, Ostad E. The antiinflammatory mechanism of methotrexate. Increased adenosine release at inflamed sites diminishes leukocyte accumulation in an in vivo model of inflammation. J Clin Invest. 1993;92:2675-82 pubmed
..These results indicate that methotrexate is a nonsteroidal antiinflammatory agent, the antiphlogistic action of which is due to increased adenosine release at inflamed sites. ..
Falsini M, Squarcialupi L, Catarzi D, Varano F, Betti M, Dal Ben D, et al
. The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A2A Receptor Subtype. J Med Chem. 2017;60:5772-5790 pubmed publisher
..Docking studies at hAR structures were performed to rationalize the observed affinity data. ..
Pell T, Baxter G, Yellon D, Drew G. Renal ischemia preconditions myocardium: role of adenosine receptors and ATP-sensitive potassium channels. Am J Physiol. 1998;275:H1542-7 pubmed
..4%; n = 6) or 5-HD (40.5 +/- 4.2%; n = 6) did not affect infarct-to-risk ratio in sham controls. Thus activation of both adenosine receptors and KATP channels appears to be involved in acute renal preconditioning of the myocardium. ..
Goudis C. Chronic obstructive pulmonary disease and atrial fibrillation: An unknown relationship. J Cardiol. 2017;69:699-705 pubmed publisher
Zhang X, Liu X, Chen L, Wu D, Nie Z, Gao Y, et al
. Caffeine delays oocyte aging and maintains the quality of aged oocytes safely in mouse. Oncotarget. 2017;8:20602-20611 pubmed publisher
..Furthermore, caffeine increased pronucleus formation of aged oocytes and decreased fragmentation after fertilization. These results suggested that caffeine could maintain the quality of aged oocytes safely in mouse. ..
Petrelli R, Scortichini M, Kachler S, Boccella S, Cerchia C, Torquati I, et al
. Exploring the Role of N6-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice ?. J Med Chem. 2017;60:4327-4341 pubmed publisher
..This study demonstrated for the first time the advantages of a single molecule activating two AR pathways both leading to benefit in this acute pain model. ..