Evidence map›Paper›PMID 26902370›Full record

Trial reportEuropean journal of nuclear medicine and molecular imaging2016

[(11)C]TASP457, a novel PET ligand for histamine H3 receptors in human brain.

Yasuyuki Kimura, Chie Seki, Yoko Ikoma, Masanori Ichise, Kazunori Kawamura, Keisuke Takahata, Sho Moriguchi, Tomohisa Nagashima, Tatsuya Ishii, Soichiro Kitamura and 6 more

Abstract readClinical Trial
PubMed Publisher
In one paragraph

Trial report in European journal of nuclear medicine and molecular imaging, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.2field-weighted citation impact, top 22% 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

7 citing papers in PubMed, 17 citations in OpenAlex.

  1. Development and Preclinical Characterization of [Journal of medicinal chemistry · 2025
    Article
  2. Pharmacokinetic Modeling of [Molecular pharmaceutics · 2022
    Article
  3. Pharmacokinetic and pharmacodynamic assessment of histamine HEuropean journal of nuclear medicine and molecular imaging · 2022
    Article
  4. Imaging Histamine H3 Receptors with Positron Emission Tomography.Current topics in behavioral neurosciences · 2022
    Review
  5. Review
  6. Histamine HEJNMMI research · 2018
    Article
  7. News and views on in-vivo imaging of neurotransmission using PET and MRI.The quarterly journal of nuclear medicine and molecular imaging : official publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR), [and] Section of the Society of... · 2017
    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 2 institutions in 1 country.

Yasuyuki KimuraMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan. y-kimura@nirs.go.jp.
Chie SekiMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Yoko IkomaMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Masanori IchiseMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan. ichisem@nirs.go.jp.
Kazunori KawamuraMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Keisuke TakahataMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Sho MoriguchiMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Tomohisa NagashimaMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Tatsuya IshiiMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Soichiro KitamuraMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Fumitoshi NiwaMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Hironobu EndoMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Makiko YamadaMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Makoto HiguchiMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Ming-Rong ZhangMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Tetsuya SuharaMolecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Chiba, Japan.
Chiba Hospital · JPChiba Prefectural Institute of Public Health · JP

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeThe histamine H3 receptors are presynaptic neuroreceptors that inhibit the release of histamine and other neurotransmitters. The receptors are considered a drug target for sleep disorders and neuropsychiatric disorders with cognitive decline. We developed a novel PET ligand for the H3 receptors, [(11)C]TASP0410457 ([(11)C]TASP457), with high affinity, selectivity and favorable kinetic properties in the monkey, and evaluated its kinetics and radiation safety profile for quantifying the H3 receptors in human brain.

methodsTen healthy men were scanned for 120 min with a PET scanner for brain quantification and three healthy men were scanned for radiation dosimetry after injection of 386 ± 6.2 MBq and 190 ± 7.5 MBq of [(11)C]TASP457, respectively. For brain quantification, arterial blood sampling and metabolite analysis were performed using high-performance liquid chromatography. Distribution volumes (V T) in brain regions were determined by compartment and graphical analyses using the Logan plot and Ichise multilinear analysis (MA1). For dosimetry, radiation absorbed doses were estimated using the Medical Internal Radiation Dose scheme.

results[(11)C]TASP457 PET showed high uptake (standardized uptake values in the range of about 3 - 6) in the brain and fast washout in cortical regions and slow washout in the pallidum. The two-tissue compartment model and graphical analyses estimated V T with excellent identification using 60-min scan data (about 16 mL/cm(3) in the pallidum, 9 - 14 in the basal ganglia, 6 - 9 in cortical regions, and 5 in the pons), which represents the known distribution of histamine H3 receptors. For parametric imaging, MA1 is recommended because of minimal underestimation with small intersubject variability. The organs with the highest radiation doses were the pancreas, kidneys, and liver. The effective dose delivered by [(11)C]TASP457 was 6.9 μSv/MBq.

conclusion[(11)C]TASP457 is a useful novel PET ligand for the investigation of the density of histamine H3 receptors in human brain.

Indexed as

AdultBiological TransportBrainCarbon RadioisotopesHealthy VolunteersHumansKineticsLigandsMalePositron-Emission TomographyRadiometryReceptors, Histamine H3Carbon RadioisotopesLigandsReceptors, Histamine H3[11C]TASP0410457[11C]TASP457DosimetryHistamine H3 receptorsPET quantification

Identifiers

PMID26902370
OpenAlexW2278756750

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.