Evidence map›Paper›PMID 16366590›Full record

ArticleJournal of medicinal chemistry2005

Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.

Kenneth A Jacobson, Zhan-Guo Gao, Susanna Tchilibon, Heng T Duong, Bhalchandra V Joshi, Dmitry Sonin, Bruce T Liang

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
–field-weighted citation impact
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

19 citing papers in PubMed.

  1. An updated review of enantioselective syntheses and biological actions of carbanucleosides.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
    Review
  2. Review
  3. Potent and Selective Human 5-HTJournal of medicinal chemistry · 2024
    Article
  4. Structure activity relationships of 5-HTEuropean journal of medicinal chemistry · 2023
    Article
  5. Article
  6. Review
  7. Review
  8. Design and in Vivo Characterization of AJournal of medicinal chemistry · 2019
    Article
  9. Review
  10. Article
  11. AMedicinal research reviews · 2018
    Review
  12. Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Article
  19. NUCLEOSIDE PRODRUGS OF ACollection of Czechoslovak chemical communications · 2006
    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

7 authors.

Kenneth A JacobsonNational Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA. kajacobs@helix.nih.gov
Zhan-Guo Gao
Susanna Tchilibon
Heng T Duong
Bhalchandra V Joshi
Dmitry Sonin
Bruce T Liang

Funding

Drugs that Act at Adenosine ReceptorsZ01DK031117 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 1991 to 2008
$854k
FUNCTIONALIZED CONGENERS OF BIOACTIVE COMPOUNDSZ01DK031115 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 1991 to 2008
$577k
Computer Modeling of G Protein-Coupled ReceptorsZ01DK031126 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2007 to 2008
$577k
Intramural NIH HHS Z01 DK031115Intramural NIH HHS Z01 DK031117Intramural NIH HHS Z01 DK031126NHLBI NIH HHS R01 HL482325
6 · The paper itself

Abstract

Ring-constrained adenosine analogues have been designed to act as dual agonists at tissue-protective A(1) and A(3) adenosine receptors (ARs). 9-Ribosides transformed into the ring-constrained (N)-methanocarba-2-chloro-5'-uronamides consistently lost affinity at A(1)/A(2A)ARs and gained at A(3)AR. Among 9-riboside derivatives, only N(6)-cyclopentyl and 7-norbornyl moieties were extrapolated for mixed A(1)/A(3) selectivity and rat/human A(3)AR equipotency. Consequently, 2 was balanced in affinity and potency at A(1)/A(3)ARs as envisioned and dramatically protected in an intact heart model of global ischemia and reperfusion.

Indexed as

Adenosine A1 Receptor AgonistsAdenosine A3 Receptor AgonistsAdenosineAdenosine A2 Receptor AgonistsAnimalsCardiotonic AgentsCHO CellsCricetinaeDrug DesignHumansMiceMyocardial InfarctionReceptor, Adenosine A1Receptor, Adenosine A2AReceptor, Adenosine A3Reperfusion InjuryAdenosineAdenosine A1 Receptor AgonistsAdenosine A2 Receptor AgonistsAdenosine A3 Receptor AgonistsCardiotonic AgentsReceptor, Adenosine A1Receptor, Adenosine A2AReceptor, Adenosine A3

Identifiers

PMID16366590
PMCPMC2597460

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.