Evidence map›Paper›PMID 32969645›Full record

ArticleACS chemical neuroscience2020

Evidence for a Stereoselective Mechanism for Bitopic Activity by Extended-Length Antagonists of the D

Amy E Moritz, Alessandro Bonifazi, Adrian M Guerrero, Vivek Kumar, R Benjamin Free, J Robert Lane, Ravi Kumar Verma, Lei Shi, Amy Hauck Newman, David R Sibley

Abstract read
In one paragraph

Article in ACS chemical neuroscience, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing 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

14 citing papers in PubMed.

  1. The structure of the dopamine DScience advances · 2026
    Article
  2. Article
  3. Article
  4. Review
  5. Article
  6. Article
  7. Allosteric modulation of dopamine DPharmacological reports : PR · 2022
    Article
  8. Article
  9. Article
  10. Article
  11. Article
  12. Article
  13. Article
  14. Review
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

10 authors.

Amy E MoritzMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.
Alessandro BonifaziMedicinal Chemistry Section, Molecular Targets and Medication Discovery Branch, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.ORCID 0000-0002-7306-0114
Adrian M GuerreroMedicinal Chemistry Section, Molecular Targets and Medication Discovery Branch, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Vivek KumarMedicinal Chemistry Section, Molecular Targets and Medication Discovery Branch, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.
R Benjamin FreeMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.ORCID 0000-0002-2428-0487
J Robert LaneCentre of Membrane Protein and Receptors, Universities of Birmingham and Nottingham, Nottingham, United Kingdom.ORCID 0000-0002-7361-7875
Ravi Kumar VermaComputational Chemistry and Molecular Biophysics Unit, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Lei ShiComputational Chemistry and Molecular Biophysics Unit, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Amy Hauck NewmanMedicinal Chemistry Section, Molecular Targets and Medication 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
David R SibleyMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.ORCID 0000-0002-0624-962X

Funding

Molecular And Pharmacological Studies Of Dopamine ReceptorsZIANS002263 · NINDS · NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE · PI SIBLEY, DAVID · 2009 to 2025
$37.4M
Novel Dopamine D3 Receptor Ligands ZIADA000424 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI NEWMAN, AMY HAUCK · 2009 to 2025
$25.9M
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
Molecular &Pharmacological Studies Of Dopamine ReceptorZ01NS002263 · NINDS · NEUROLOGICAL DISORDERS AND STROKE · PI SIBLEY, DAVID R. · 1985 to 2008
$3.1M
NOVEL DOPAMINE D3 RECEPTOR LIGANDSZ01DA000424 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI NEWMAN, AMY HAUCK · 1999 to 2008
$1.8M
Intramural NIH HHS Z01 DA000424Intramural NIH HHS Z01 NS002263Intramural NIH HHS ZIA DA000424Intramural NIH HHS ZIA DA000606Intramural NIH HHS ZIA NS002263
6 · The paper itself

Abstract

The D3 dopamine receptor (D3R) has been suggested as a drug target for the treatment of a number of neuropsychiatric disorders, including substance use disorders (SUD). Many D3R-selective antagonists are bivalent in nature in that they engage two distinct sites on the receptor-a primary pharmacophore binds to the orthosteric site, where dopamine binds, whereas a secondary pharmacophore interacts with a unique secondary binding pocket (SBP). When engagement of the secondary pocket exerts allosteric activity, the compound is said to be bitopic. We recently reported the synthesis and characterization of two bitopic antagonists of the D3R, (±)-VK04-87 and (±)-VK05-95, which incorporated a racemic

Indexed as

Receptors, Dopamine D2Receptors, Dopamine D3Molecular ConformationMolecular Dynamics SimulationStructure-Activity RelationshipReceptors, Dopamine D2Receptors, Dopamine D3bitopicD3 receptorDopaminenegative allosteric modulatornoncompetitive antagoniststereoselectivity

Identifiers

PMID32969645
PMCPMC8262072

What OpenQuestion holds

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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.