ArticleACS medicinal chemistry letters2011
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.
Article in ACS medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 45 citations in OpenAlex.
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- Adenosine-mediated immune responses in inflammatory bowel disease.Frontiers in cell and developmental biology · 2024Review
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- C2-linked alkynyl poly-ethylene glycol(PEG) adenosine conjugates as water-soluble adenosine receptor agonists.Chemical biology & drug design · 2023Article
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- Extracellular adenosine induces hypersecretion of IL-17A by T-helper 17 cells through the adenosine A2a receptor.Brain, behavior, & immunity - health · 2022Article
- Kinetic profiling and functional characterization of 8-phenylxanthine derivatives as ABiochemical pharmacology · 2022Article
- Upregulation of Src Family Tyrosine Kinases in the Rat Striatum by Adenosine AJournal of molecular neuroscience : MN · 2022Article
- Expression of the Adenosine ABiomedicines · 2022Article
- Convergent synthesis of 2-thioether-substituted (RSC advances · 2021Article
- Control of Gut Inflammation by Modulation of Purinergic Signaling.Frontiers in immunology · 2020Review
- Role of Cardiac AFrontiers in pharmacology · 2020Review
- Blood Platelet Adenosine Receptors as Potential Targets for Anti-Platelet Therapy.International journal of molecular sciences · 2019Review
- Dysregulation of Adenosinergic Signaling in Systemic and Organ-Specific Autoimmunity.International journal of molecular sciences · 2019Review
- Activation of adenosine ANeuropharmacology · 2018Article
- Anti-inflammatory effect of a novel locally acting APurinergic signalling · 2018Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Adenosine A2A receptor agonists for the local treatment of inflammatory bowel disease (IBS) were designed and synthesized. Polar groups were introduced to prevent peroral absorption and subsequent systemic, e.g., hypotensive, side effects. 4-(2-{6-Amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-9H-purin-2-ylthio}ethyl)benzenesulfonic acid (7, PSB-0777) was selected for further evaluation in rat ileum/jejunum preparations in ex vivo experiments. Compound 7 significantly improved impaired acetylcholine-induced contractions induced by 2,4,6-trinitrobenzenesulfonic acid and showed synergism with an A2B-selective antagonist. Thus, nonabsorbable, locally active A2A agonists, as a monotherapy or in combination with an A2B antagonist, may be an efficient novel treatment for IBS, preventing the severe systemic side effects of known A2A agonists.
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