Evidence map›Paper›PMID 26384292›Full record

ArticleEJNMMI research2015

Further validation to support clinical translation of [(18)F]FTC-146 for imaging sigma-1 receptors.

Bin Shen, Michelle L James, Lauren Andrews, Christopher Lau, Stephanie Chen, Mikael Palner, Zheng Miao, Natasha C Arksey, Adam J Shuhendler, Shawn Scatliffe and 6 more

Registry-linked trialOpen access · goldAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in EJNMMI research, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT03556137 (Use of [18F]FTC-146 PET/MRI in the Diagnosis of Chronic Pain), which is not on this map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
1.5field-weighted citation impact, top 18% 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.

NCT03556137 phase1unknown statusnot on this mapstarted 2018, after this paper: background citation

Use of [18F]FTC-146 PET/MRI in the Diagnosis of Chronic Pain

TypeinterventionalSponsorStanford UniversityRan2018 to 2024Enrolled190ConditionsNeuropathic Pain, Nociceptive Pain, Mixed Pain (Nociceptive and Neuropathic), Spinal PainArms[18F]FTC-146
3 · Its place in the literature

Who cites it

19 citing papers in PubMed, 30 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Article
  6. Up-and-coming Radiotracers for Imaging Pain Generators.Seminars in musculoskeletal radiology · 2023
    Article
  7. Article
  8. Article
  9. Article
  10. Evaluation ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020
    Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Biodistribution and Radiation Dosimetry ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2017
    Article
  16. Article
  17. Chiral resolution of serial potent and selective σBioorganic & medicinal chemistry · 2017
    Article
  18. Article
  19. 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

16 authors at 4 institutions in 1 country.

Bin ShenMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Michelle L JamesMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Lauren AndrewsMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Christopher LauMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Stephanie ChenMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Mikael PalnerMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Zheng MiaoMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Natasha C ArkseyMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Adam J ShuhendlerMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Shawn ScatliffeMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Kota KaneshigeDepartment of Chemistry and Biochemistry, University of California Santa Barbara, Santa Barbara, CA, 93106, USA.
Stanley M ParsonsDepartment of Chemistry and Biochemistry, University of California Santa Barbara, Santa Barbara, CA, 93106, USA.
Christopher R McCurdyDepartment of Medicinal Chemistry and Pharmacology, The University of Mississippi, University, MS, 38677, USA.
Ahmad SalehiDepartment of Neurology and Neurological Sciences, Stanford University, Stanford, CA, 94305, USA.
Sanjiv S GambhirMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA.
Frederick T ChinMolecular Imaging Program at Stanford (MIPS) Department of Radiology Stanford University, Stanford, CA, 94305, USA. chinf@stanford.edu.
Stanford University · USUniversity of California, Santa Barbara · USUniversity of Mississippi · USVA Palo Alto Health Care System · US

Funding

Small Animal ImagingP50CA114747 · NCI · STANFORD UNIVERSITY · PI PAIK, DAVID SEUNGWON · 2005 to 2014
$18.2M
Center of Research Excellence in Natural Products Neuroscience (CORE-NPN)P20GM104932 · NIGMS · UNIVERSITY OF MISSISSIPPI · PI MAJUMDAR, SOUMYAJIT · 2012 to 2016
$10.0M
Novel Pharmacologic Interventions for Drugs of AbuseR01DA023205 · NIDA · UNIVERSITY OF MISSISSIPPI · PI MCCURDY, CHRISTOPHER R · 2007 to 2011
$1.7M
Small animal PET system for molecular imaging of rodents and primatesS10OD018130 · OD · STANFORD UNIVERSITY · PI CHIN, FREDERICK T · 2014 to 2014
$600k
NCI NIH HHS P50 CA114747NIDA NIH HHS R01 DA023205NIGMS NIH HHS P20 GM104932NIH HHS S10 OD018130
6 · The paper itself

Abstract

backgroundThis study aims to further evaluate the specificity and selectivity of [(18)F]FTC-146 and obtain additional data to support its clinical translation.

methodsThe binding of [(19)F]FTC-146 to vesicular acetylcholine transporter (VAChT) was evaluated using [(3)H]vesamicol and PC12(A123.7) cells in an in vitro binding assay. The uptake and kinetics of [(18)F]FTC-146 in S1R-knockout mice (S1R-KO) compared to wild-type (WT) littermates was assessed using dynamic positron emission tomography (PET) imaging. Ex vivo autoradiography and histology were conducted using a separate cohort of S1R-KO/WT mice, and radiation dosimetry was calculated from WT mouse data (extrapolated for human dosing). Toxicity studies in Sprague-Dawley rats were performed with a dose equivalent to 250× the anticipated clinical dose of [(19)F]FTC-146 mass. RESULTS AND DISCUSSION: VAChT binding assay results verified that [(19)F]FTC-146 displays negligible affinity for VAChT (K i = 450 ± 80 nM) compared to S1R. PET images demonstrated significantly higher tracer uptake in WT vs. S1R-KO brain (4.57 ± 1.07 vs. 1.34 ± 0.4 %ID/g at 20-25 min, n = 4, p < 0.05). In S1R-KO mice, it was shown that rapid brain uptake and clearance 10 min post-injection, which are consistent with previous S1R-blocking studies in mice. Three- to fourfold higher tracer uptake was observed in WT relative to S1R-KO mouse brains by ex vivo autoradiography. S1R staining coincided well with the autoradiographic data in all examined brain regions (r (2) = 0.85-0.95). Biodistribution results further demonstrated high [(18)F]FTC-146 accumulation in WT relative to KO mouse brain and provided quantitative information concerning tracer uptake in S1R-rich organs (e.g., heart, lung, pancreas) for WT mice vs. age-matched S1R-KO mice. The maximum allowed dose per scan in humans as extrapolated from mouse dosimetry was 33.19 mCi (1228.03 MBq). No significant toxicity was observed even at a 250X dose of the maximum carrier mass [(19)F]FTC-146 expected to be injected for human studies.

conclusionsTogether, these data indicate that [(18)F]FTC-146 binds specifically to S1Rs and is a highly promising radiotracer ready for clinical translation to investigate S1R-related diseases.

Indexed as

[18F]FTC-146DosimetrySigma-1 receptorSigma-1 receptor knockout miceSmall animal PETToxicologyVesicular acetylcholine transporter

Identifiers

PMID26384292
PMCPMC4573970
OpenAlexW2115796811

What OpenQuestion holds

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Registered trials

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.