Evidence map›Paper›PMID 28300398›Full record

ArticleJournal of medicinal chemistry2017

Novel Bivalent Ligands Based on the Sumanirole Pharmacophore Reveal Dopamine D

Alessandro Bonifazi, Hideaki Yano, Michael P Ellenberger, Ludovic Muller, Vivek Kumar, Mu-Fa Zou, Ning Sheng Cai, Adrian M Guerrero, Amina S Woods, Lei Shi and 1 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.

0numbers the graph read from it
0cells of the map it votes in
28citing papers in PubMed
2.5field-weighted citation impact, top 10% 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

28 citing papers in PubMed, 52 citations in OpenAlex.

  1. Article
  2. ESG-1-60 and ESG-1-61: Novel dopamine DBritish journal of pharmacology · 2025
    Article
  3. Article
  4. Review
  5. Article
  6. Article
  7. Article
  8. Dopamine DJournal of medicinal chemistry · 2023
    Article
  9. Identification of Novel Dopamine DMolecules (Basel, Switzerland) · 2022
    Article
  10. Review
  11. Review
  12. Article
  13. Potent and Subtype-Selective Dopamine DJournal of medicinal chemistry · 2021
    Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Article
  19. Article
  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

11 authors at 1 institution in 1 country.

Alessandro BonifaziMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Hideaki YanoMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Michael P EllenbergerMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Ludovic MullerStructural Biology Unit, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Vivek KumarMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Mu-Fa ZouMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Ning Sheng CaiMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Adrian M GuerreroMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Amina S WoodsStructural Biology Unit, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Lei ShiMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Amy Hauck NewmanMolecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.ORCID 0000-0001-9065-4072
National Institutes of Health · US

Funding

Structural basis for the functions of dopamine receptors, neurotransmitter transporters, and sigma 1 receptorZIADA000606 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI SHI, LEI · 2015 to 2025
$20.5M
Methodology development to map and quantify imaged molecules in brain tissueZIADA000593 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI WOODS, AMINA · 2013 to 2019
$3.5M
Dopamine D2-like Functionally Selective AgonistsZIADA000609 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI NEWMAN, AMY HAUCK · 2016 to 2020
$2.8M
Demonstration of the specificity of receptor receptor interactionZIADA000594 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI WOODS, AMINA · 2015 to 2020
$1.8M
Intramural NIH HHS Z99 DA999999
6 · The paper itself

Abstract

The development of bivalent ligands has attracted interest as a way to potentially improve the selectivity and/or affinity for a specific receptor subtype. The ability to bind two distinct receptor binding sites simultaneously can allow the selective activation of specific G-protein dependent or β-arrestin-mediated cascade pathways. Herein, we developed an extended SAR study using sumanirole (1) as the primary pharmacophore. We found that substitutions in the N-1- and/or N-5-positions, physiochemical properties of those substituents, and secondary aromatic pharmacophores can enhance agonist efficacy for the cAMP inhibition mediated by G

Indexed as

Benzimidazolesbeta-ArrestinsCyclic AMPDopamine AgonistsGTP-Binding ProteinsHEK293 CellsHumansReceptors, Dopamine D2Structure-Activity RelationshipBenzimidazolesbeta-ArrestinsCyclic AMPDopamine AgonistsGTP-Binding ProteinsReceptors, Dopamine D2U 95666E

Identifiers

PMID28300398
PMCPMC7594663
OpenAlexW2595633258

What OpenQuestion holds

Textmetadata
LicenceTDM
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.