Non‐Xanthine Antagonists for the Adenosine A1 Receptor

  title={Non‐Xanthine Antagonists for the Adenosine A1 Receptor},
  author={Lisa C W Chang and Johannes Brussee and Adriaan P. IJzerman},
  journal={Chemistry \& Biodiversity},
Identification of bioactive metabolites against adenosine A1 receptor using NMR-based metabolomics
The screening of marine sponges crude extracts for their potential to bind the adenosine A1 receptor is reported and the resonances responsible for the separation of high activity samples from the medium and low activity samples were identified as associated to metabolites like halisulfate 1, hal isulfate 3–5, and suvanine (1–5).
New fused pyrroles with rA1/A2A antagonistic activity as potential therapeutics for neurodegenerative disorders.
It is concluded that new 7-azaindole and 7-deazapurine derivatives represent interesting scaffolds for design of A1 and/or A2A AR antagonists.
Development of fluorescent ligands for A1 adenosine receptor and cannabinoid receptors
This paper presents a systematic literature review of single and three letter amino acid codes and their applications in medicine and physiology.
Discovery of 2-aminoimidazole and 2-amino imidazolyl-thiazoles as non-xanthine human adenosine A3 receptor antagonists: SAR and molecular modeling studies.
A receptor-based modeling study was performed to explore the possible binding mode of these novel 2-aminoimidazole and 2-AMinoIMidazolyl-thiazole derivatives into human adenosine A1, A2A and A3 receptor subtypes.
Relevance of in vitro metabolism models for PET radiotracer development
Both quantitative and qualitative aspects of radiotracer metabolism could be reasonably well predicted by microsomal data, and the implementation of in vitro metabolism studies as an integral part of PET radiot Racers development is encouraged.
Biochemical and Pharmacological Role of A1 Adenosine Receptors and Their Modulation as Novel Therapeutic Strategy.
It will become apparent that A1ARs could be implicated in the pharmacological treatment of several pathologies with an important influence on human health.
Identification of adenosine A1 receptor ligands from Morus alba L. stem bark by NMR metabolomics approach
Comprehensive extraction coupled to NMR metabolomics was applied to the identification of active compounds from Morus alba stem bark binding to the adenosine A1 receptor. Orthogonal projection to the


Structure elucidation and total synthesis of new tanshinones isolated from Salvia miltiorrhiza Bunge (Danshen)
Totally 11 new compounds have been isolated from the dried root of Salvia miltiorrhiza Bunge «Danshen» and their structures were elucidated by means of spectrometric methods. The total syntheses of
Compounds from Danshen. Part 7. Regioselective introduction of carbon-3 substituents to 5-alkyl-7-methoxy-2-phenylbenzo[b]furans: synthesis of a novel adenosine A1 receptor ligand and its derivatives
By maintaining the balance between the electronic requirements, the stereochemical restrictions as well as the kinetic and thermodynamic factors, the unprecedented regioselective electrophilic
Mono-α-carbamoylethylthio-substituted pyrazolo[3,4-d]pyrimidines: The position of substitution
Pyrazolo [3,4-d] pyrimidines are a general class of compounds which exhibit adenosine receptor affinity. One particular compound,
Pyrazolopyridines: Effect of structural alterations on activity at adenosine‐ and GABAA‐receptors
Analysis of the interactions indicates that stimulation of [3H]diazepam binding is allosteric and results from binding of the pyrazolopyridine at the GABA site or a subdomain of that site, while inhibition of [ 3H]Ro 15‐1788 binding is competitive and due to binding at the benzodiazepine site.