ArticleJournal of medicinal chemistry2002
Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.
Article in Journal of medicinal chemistry, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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Who cites it
19 citing papers in PubMed, 69 citations in OpenAlex.
- Discovery of a novel 4-pyridyl SLC-0111 analog targeting tumor-associated carbonic anhydrase isoform IX through tail-based design approach with potent anticancer activity.Frontiers in chemistry · 2025Article
- Potent and selective ARSC medicinal chemistry · 2021Article
- Conjugable AEuropean journal of medicinal chemistry · 2020Article
- AMedicinal research reviews · 2018Review
- Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility.Journal of medicinal chemistry · 2011Article
- Pyrazolo derivatives as potent adenosine receptor antagonists: an overview on the structure-activity relationships.International journal of medicinal chemistry · 2011Review
- Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process.Bioorganic & medicinal chemistry · 2010Article
- Medicinal chemistry of the A3 adenosine receptor: agonists, antagonists, and receptor engineering.Handbook of experimental pharmacology · 2009Review
- Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry letters · 2008Article
- Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: Effect of the N-5 bond type on the affinity and selectivity at the four adenosine receptor subtypes.Purinergic signalling · 2008Article
- Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: A complete structure-activity profile.Purinergic signalling · 2007Article
- Invited Lectures : Overviews Purinergic signalling: past, present and future.Purinergic signalling · 2006Article
- Progress in the pursuit of therapeutic adenosine receptor antagonists.Medicinal research reviews · 2006Review
- A3 adenosine receptor antagonists delay irreversible synaptic failure caused by oxygen and glucose deprivation in the rat CA1 hippocampus in vitro.British journal of pharmacology · 2006Article
- Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.Bioorganic & medicinal chemistry letters · 2006Article
- Techniques: Recent developments in computer-aided engineering of GPCR ligands using the human adenosine A3 receptor as an example.Trends in pharmacological sciences · 2005Review
- Demystifying the three dimensional structure of G protein-coupled receptors (GPCRs) with the aid of molecular modeling.Chemical communications (Cambridge, England) · 2003Review
- N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.Biochemical pharmacology · 2003Article
- Chapter 13. AAnnual reports in medicinal chemistryArticle
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
A new, highly potent, selective, and water-soluble antagonist of the hA(3) adenosine receptor was synthesized and tested in binding and functional assays. Compound 4 (5-[[(4-pyridyl)amino]carbonyl]amino-8-methyl-2-(2-furyl)-pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine hydrochloride) displayed high water solubility (15 mM) and the highest affinity (K(i) = 0.01 nM) and selectivity for the hA(3) versus A(1), A(2A), and A(2B) receptors (>10000-fold) ever reported. A Schild analysis of the antagonism by 4 of agonist-induced inhibition of cAMP production in CHO cells expressing the hA(3) receptor indicated a K(B) value of 0.20 nM.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.