| Title |
[11C]TASP457, a novel PET ligand for histamine H3 receptors in human brain
|
|---|---|
| Published in |
European Journal of Nuclear Medicine and Molecular Imaging, February 2016
|
| DOI | 10.1007/s00259-016-3332-6 |
| Pubmed ID | |
| Authors |
Yasuyuki Kimura, Chie Seki, Yoko Ikoma, Masanori Ichise, Kazunori Kawamura, Keisuke Takahata, Sho Moriguchi, Tomohisa Nagashima, Tatsuya Ishii, Soichiro Kitamura, Fumitoshi Niwa, Hironobu Endo, Makiko Yamada, Makoto Higuchi, Ming-Rong Zhang, Tetsuya Suhara |
| Abstract |
The 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. Ten 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. [(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. [(11)C]TASP457 is a useful novel PET ligand for the investigation of the density of histamine H3 receptors in human brain. |
X Demographics
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Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 22 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 22 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 6 | 27% |
| Student > Doctoral Student | 2 | 9% |
| Student > Postgraduate | 2 | 9% |
| Student > Bachelor | 1 | 5% |
| Student > Master | 1 | 5% |
| Other | 3 | 14% |
| Unknown | 7 | 32% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 5 | 23% |
| Neuroscience | 4 | 18% |
| Biochemistry, Genetics and Molecular Biology | 1 | 5% |
| Nursing and Health Professions | 1 | 5% |
| Computer Science | 1 | 5% |
| Other | 3 | 14% |
| Unknown | 7 | 32% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 24 February 2016.
All research outputs
#21,153,429
of 23,806,312 outputs
Outputs from European Journal of Nuclear Medicine and Molecular Imaging
#2,610
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Outputs of similar age
#254,504
of 300,406 outputs
Outputs of similar age from European Journal of Nuclear Medicine and Molecular Imaging
#42
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