Evidence map›Paper›PMID 16380972›Full record

ReviewMedicinal research reviews2006

Progress in the pursuit of therapeutic adenosine receptor antagonists.

Stefano Moro, Zhan-Guo Gao, Kenneth A Jacobson, Giampiero Spalluto

Open access · greenAbstract readReview
In one paragraph

Review in Medicinal research reviews, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.

0numbers the graph read from it
0cells of the map it votes in
49citing papers in PubMed
4.3field-weighted citation impact, top 5% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

49 citing papers in PubMed, 151 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. Article
  5. Article
  6. The role of adenosine AInflammation research : official journal of the European Histamine Research Society ... [et al.] · 2022
    Review
  7. Article
  8. Article
  9. Article
  10. Article
  11. Conjugable AEuropean journal of medicinal chemistry · 2020
    Article
  12. Agonists activate different ANaunyn-Schmiedeberg's archives of pharmacology · 2019
    Article
  13. Chemical Probes for the Adenosine Receptors.Pharmaceuticals (Basel, Switzerland) · 2019
    Review
  14. Article
  15. Article
  16. Review
  17. Fluorinated Adenosine AInternational journal of medicinal chemistry · 2017
    Article
  18. Article
  19. Review
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

4 authors at 4 institutions in 2 countries.

Stefano MoroMolecular Modeling Section, Dipartimento di Scienze Farmaceutiche, Università di Padova, Via Marzolo 5, I-35131 Padova, Italy. stefano.moro@unipd.it
Zhan-Guo Gao
Kenneth A Jacobson
Giampiero Spalluto
National Institute of Diabetes and Digestive and Kidney Diseases · USNational Institutes of Health · USUniversity of Padua · ITUniversity of Trieste · IT

Funding

Development Of Drugs Acting At Adenosine ReceptorsZIADK031117 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$10.4M
Drugs that Act at Adenosine ReceptorsZ01DK031117 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 1991 to 2008
$854k
Intramural NIH HHS Z01 DK031117Intramural NIH HHS ZIA DK031117
6 · The paper itself

Abstract

Ever since the discovery of the hypotensive and bradycardiac effects of adenosine, adenosine receptors continue to represent promising drug targets. First, this is due to the fact that the receptors are expressed in a large variety of tissues. In particular, the actions of adenosine (or methylxanthine antagonists) in the central nervous system, in the circulation, on immune cells, and on other tissues can be beneficial in certain disorders. Second, there exists a large number of ligands, which have been generated by introducing several modifications in the structure of the lead compounds (adenosine and methylxanthine), some of them highly specific. Four adenosine receptor subtypes (A1, A2A, A2B, and A3) have been cloned and pharmacologically characterized, all of which are G protein-coupled receptors. Adenosine receptors can be distinguished according to their preferred mechanism of signal transduction: A1 and A3 receptors interact with pertussis toxin-sensitive G proteins of the Gi and Go family; the canonical signaling mechanism of the A2A and of the A2B receptors is stimulation of adenylyl cyclase via Gs proteins. In addition to the coupling to adenylyl cyclase, all four subtypes may positively couple to phospholipase C via different G protein subunits. The development of new ligands, in particular, potent and selective antagonists, for all subtypes of adenosine receptors has so far been directed by traditional medicinal chemistry. The availability of genetic information promises to facilitate understanding of the drug-receptor interaction leading to the rational design of a potentially therapeutically important class of drugs. Moreover, molecular modeling may further rationalize observed interactions between the receptors and their ligands. In this review, we will summarize the most relevant progress in developing new therapeutic adenosine receptor antagonists.

Indexed as

Purinergic P1 Receptor AntagonistsAdenosine A1 Receptor AntagonistsAdenosine A2 Receptor AntagonistsAdenosine A3 Receptor AntagonistsAmino Acid SequenceAnimalsFlavonoidsHeterocyclic CompoundsHumansQuantitative Structure-Activity RelationshipQuinazolinesReceptor, Adenosine A2BTriazolesXanthines1,3-dipropyl-8-cyclopentylxanthineAdenosine A1 Receptor AntagonistsAdenosine A2 Receptor AntagonistsAdenosine A3 Receptor AntagonistsFlavonoidsHeterocyclic CompoundsPurinergic P1 Receptor AntagonistsQuinazolinesReceptor, Adenosine A2BTriazolesXanthines

Identifiers

PMID16380972
PMCPMC9194718
OpenAlexW2122624834

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.