Evidence map›Paper›PMID 30450619›Full record

ReviewMedicinal research reviews2019

Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging.

Vladimir Shalgunov, Aren van Waarde, Jan Booij, Martin C Michel, Rudi A J O Dierckx, Philip H Elsinga

Open access · hybridAbstract readReview
In one paragraph

Review in Medicinal research reviews, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed, 1 pooled it
1.6field-weighted citation impact, top 16% 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

17 citing papers in PubMed, 1 synthesis or guideline pooled it, 24 citations in OpenAlex.

  1. Pooled it
  2. Estimation of Dopamine DACS chemical neuroscience · 2025
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    Article
  5. Discovery of Highly Potent Adenosine AACS chemical neuroscience · 2021
    Article
  6. Article
  7. Opposite alterations of 5-HTTranslational psychiatry · 2021
    Article
  8. First-in-Human Assessment ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021
    Article
  9. Biomedicines · 2021
    Review
  10. A Single Dose of Psilocybin Increases Synaptic Density and Decreases 5-HTInternational journal of molecular sciences · 2021
    Article
  11. Review
  12. Kinetic Modeling and Test-Retest Reproducibility ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020
    Article
  13. Article
  14. Article
  15. Review
  16. Design, synthesis and evaluation ofNuclear medicine and biology · 2019
    Article
  17. 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

6 authors at 3 institutions in 3 countries.

Vladimir ShalgunovDepartment of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands.ORCID 0000-0001-8956-1207
Aren van WaardeDepartment of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands.ORCID 0000-0003-1183-1603
Jan BooijDepartment of Radiology and Nuclear Medicine, Amsterdam University Medical Centers, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands.
Martin C MichelDepartment of Pharmacology, Johannes Gutenberg University, Mainz, Germany.
Rudi A J O DierckxDepartment of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands.
Philip H ElsingaDepartment of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands.
University Medical Center Groningen · NLAmsterdam UMC Location University of Amsterdam · NLJohannes Gutenberg University Mainz · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The concept of the high-affinity state postulates that a certain subset of G-protein-coupled receptors is primarily responsible for receptor signaling in the living brain. Assessing the abundance of this subset is thus potentially highly relevant for studies concerning the responses of neurotransmission to pharmacological or physiological stimuli and the dysregulation of neurotransmission in neurological or psychiatric disorders. The high-affinity state is preferentially recognized by agonists in vitro. For this reason, agonist tracers have been developed as tools for the noninvasive imaging of the high-affinity state with positron emission tomography (PET). This review provides an overview of agonist tracers that have been developed for PET imaging of the brain, and the experimental paradigms that have been developed for the estimation of the relative abundance of receptors configured in the high-affinity state. Agonist tracers appear to be more sensitive to endogenous neurotransmitter challenge than antagonists, as was originally expected. However, other expectations regarding agonist tracers have not been fulfilled. Potential reasons for difficulties in detecting the high-affinity state in vivo are discussed.

Indexed as

Positron-Emission TomographyAnimalsCentral Nervous SystemEndocytosisHumansRadiopharmaceuticalsReceptors, G-Protein-CoupledSignal TransductionRadiopharmaceuticalsReceptors, G-Protein-Coupledagonist high-affinity stateexperimental designG-protein-coupled receptorshuman brainneurotransmitterspositron emission tomography

Identifiers

PMID30450619
PMCPMC6587759
OpenAlexW2901058579

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.