• Because of the effects of adenosine on AV node-dependent SVTs, adenosine is considered a class V antiarrhythmic agent. (wikipedia.org)
  • The regional hemodynamic effects of adenosine A2A and A2B selective agonists were investigated in conscious rats. (bvsalud.org)
  • This is being contested, and it is now considered a relative contraindication (however, selective adenosine antagonists are being investigated for use in treatment of asthma) Adenosine is an endogenous purine nucleoside that modulates many physiological processes. (wikipedia.org)
  • Pharmacological studies have shown that KW-6356 is a potent and selective ligand for the A2A receptor (the -log of inhibition constant = 9.93 ± 0.01 for human receptor) with a very low dissociation rate from the receptor (the dissociation kinetic rate constant = 0.016 ± 0.006 minute-1 for human receptor). (bvsalud.org)
  • SIGNIFICANCE STATEMENT: KW-6356 is a potent and selective adenosine A2A receptor antagonist/inverse agonist and exhibits insurmountable antagonism, whereas istradefylline, a first-generation adenosine A2A receptor antagonist, exhibits surmountable antagonism. (bvsalud.org)
  • Taken together, these data indicate that A2A and A2B receptors are regionally selective in their regulation of vascular tone. (bvsalud.org)
  • Methylxanthines act as competitive antagonists of adenosine and can blunt its pharmacological effects. (wikipedia.org)
  • In this study, we investigated the in vitro pharmacological profile of KW-6356 as an A2A receptor antagonist/inverse agonist and the mode of antagonism and compared them with istradefylline. (bvsalud.org)
  • Structural studies of adenosine A2A receptor in complex with KW-6356 and istradefylline explain the characteristic differences in the pharmacological properties of KW-6356 and istradefylline. (bvsalud.org)
  • Adenosine is used as an adjunct to thallium (TI 201) or technetium (Tc99m) myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
  • Istradefylline is a first-generation A2A receptor antagonist approved for use as adjunct treatment to levodopa/decarboxylase inhibitor in adult PD patients experiencing "OFF" episodes. (bvsalud.org)
  • These results suggest that the development of A2B receptor agonists to induce vasodilatation in the kidney may provide a good therapeutic approach for the treatment of acute kidney injury. (bvsalud.org)
  • In addition, atrial tachycardia can sometimes be terminated with adenosine. (wikipedia.org)
  • In addition, we determined cocrystal structures of A2A receptor in complex with KW-6356 and istradefylline to explore the structural basis of the antagonistic properties of KW-6356. (bvsalud.org)
  • Recent studies have built upon decades of evidence that adenosine, a purine nucleoside that can act as a neuromodulator, is involved in pain transmission and sensitization. (mdpi.com)
  • Adenosine is one of the four nucleoside building blocks of RNA (and its derivative deoxyadenosine is a building block of DNA), which are essential for all life on earth. (wikipedia.org)
  • This is being contested, and it is now considered a relative contraindication (however, selective adenosine antagonists are being investigated for use in treatment of asthma) Adenosine is an endogenous purine nucleoside that modulates many physiological processes. (wikipedia.org)
  • The endogenous levels of the purine nucleoside, adenosine, increase significantly following cardiovascular events. (frontiersin.org)
  • The purine nucleoside adenosine was first identified in 1929 when Drury and Szent-Gyorgyi successfully extracted a rhythm-influencing adenylic substance from the mammalian heart and other tissues ( Drury and Szent-Gyorgyi, 1929 ). (frontiersin.org)
  • Overall, this study suggests that the novel dual A2AAR/A3AR nucleoside antagonists would be promising drug candidates for immune-oncology. (bvsalud.org)
  • Only in 1972, Geoff Burnstock (born: May 10, 1929, died: June 2, 2020) coined the term purinergic signalling referring to the extracellular effects of adenosine 5′-triphosphate (ATP). (frontiersin.org)
  • Following Burnstock's pioneering work on the role of ATP-sensitive P2 purinoceptors, its metabolite adenosine soon became recognized as an extracellular signalling molecule through the activation of plasma membrane-bound P1 receptors family that are expressed in every organ systems in the body. (frontiersin.org)
  • Based on hA2AAR structures, a hydrophobic C8-heteroaromatic ring in 5'-truncated adenosine analogues occupies the subpocket tightly, converting hA2AAR agonists into antagonists while maintaining affinity toward hA3AR. (bvsalud.org)
  • In reality, there is a continuum between estrogen receptor agonist and estrogen receptor antagonist activity and some compounds behave as estrogen receptor agonists in some tissues but estrogen receptor antagonists in others. (justia.com)
  • N)-Methanocarba adenosine derivatives were structurally modified to target 5-HT2B serotonin receptors as antagonists, predominantly containing branched N6-alkyl groups. (bvsalud.org)
  • Adenosine exerts cardioprotective, neuromodulatory, and immunosuppressive effects by activating plasma membrane-bound P1 receptors that are widely expressed in the cardiovascular system. (frontiersin.org)
  • Compounds 43, 45 and 48 were functional 5-HT2BR (KB 2-3 nM) and 5-HT2CR (KB 79-328 nM) antagonists in a Gq-mediated calcium flux assay, with 5-HT2BR functional selectivity ranging from 45- (48) to 113-fold (43). (bvsalud.org)
  • The compounds of the invention bind to the ERβ receptor and may therefore useful in treating ERβ mediated diseases for example the compounds of this invention may be useful in the treatment of pain, chronic inflammatory disorders, autoimmune diseases, CNS disorders, metabolic disorders or appetite disorders. (justia.com)
  • Adenosine (symbol A) is an organic compound that occurs widely in nature in the form of diverse derivatives. (wikipedia.org)
  • Its derivatives include the energy carriers adenosine mono-, di-, and triphosphate, also known as AMP/ADP/ATP. (wikipedia.org)
  • More recently, however, there was the discovery of second subtype of estrogen receptor, termed estrogen receptor beta (ERβ or ER beta). (justia.com)
  • The discovery of this second subtype of estrogen receptor significantly increased the biological complexity of estrogen signalling. (justia.com)
  • Currently, ARS has been interested in the contribution of glial cells and neuroinflammation to retinal neurodegeneration, and the identification of therapeutic strategies for retinal diseases targeting neuroprotection and neuroinflammation control. (cienciavitae.pt)
  • PMID- 5097523 TI - Cell size distribution in brain suspensions and in fractions enriched with neuronal and glial cells. (nih.gov)
  • Clinical evidence and rodent studies have suggested that adenosine signaling also plays a critical role in migraine headache. (mdpi.com)
  • Methylxanthines (e.g. caffeine found in coffee, theophylline found in tea, or theobromine found in chocolate) have a purine structure and bind to some of the same receptors as adenosine. (wikipedia.org)
  • Caffeine has a three-dimensional structure similar to that of adenosine," which allows it to bind and block its receptors. (wikipedia.org)
  • Upon binding ligand, these receptors dimerize and can activate gene transcription either by directly binding to specific sequences on DNA known as response elements or by interacting with transcription factors (such as API) which in turn bind directly to specific DNA sequences. (justia.com)
  • Adenosine is used as an adjunct to thallium (TI 201) or technetium (Tc99m) myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
  • Estrogen receptors are ligand-activated transcription factors and belong to the nuclear hormone receptor subfamily. (justia.com)
  • Adenosine is used as an intravenous medication for some cardiac arrhythmias. (wikipedia.org)
  • Because of the effects of adenosine on AV node-dependent SVTs, adenosine is considered a class V antiarrhythmic agent. (wikipedia.org)
  • The dose is often decreased in patients on dipyridamole (Persantine) and diazepam (Valium) because adenosine potentiates the effects of these drugs. (wikipedia.org)
  • Here, we provide a comprehensive and up-to-date critical review about the main therapeutic advantages of tuning adenosine signalling pathways in HFpEF, without discounting their side effects and how these can be seized. (frontiersin.org)
  • In our previous work, we showed that the terpenes geraniol, linalool, ß-pinene, α- humulene, and ß-caryophyllene produced cannabimimetic behavioral effects via multiple receptor targets. (bvsalud.org)
  • The precise reason why the same compound can have cell-specific effects has not been elucidated, but the differences in receptor conformation and/or in the milieu of coregulatory proteins have been suggested. (justia.com)
  • PMID- 5097518 TI - Effects of -amanitin on mouse and rat liver cell nuclei. (nih.gov)
  • ARS is a Biochemist with a PhD in Cell Biology (2008), with part of the experimental work performed at Penn State College of Medicine (USA) and Institute for Neurosciences and Amsterdam Medical Center (The Netherlands). (cienciavitae.pt)
  • The hA2AAR-5d X-ray structure revealed that C8-heteroaromatic rings prevented receptor activation-associated conformational changes. (bvsalud.org)
  • Structural SAR features and docking studies supported different binding modes at A2AAR and A3AR, elucidating pharmacophores for receptor activation and selectivity. (bvsalud.org)
  • She is member of the editorial board of Cell Biology, Journal of Ophthalmology and Scientific Reports. (cienciavitae.pt)
  • PMID- 5097527 TI - [Morphological problems resulting from a biochemical study of various fractions of chromatin extracts from the cell nucleus of mouse liver]. (nih.gov)