A Novel Potential Positron Emission Tomography Imaging Agent for Vesicular Monoamine Transporter Type 2

In the early 1990s, 9-(+)-11C-dihydrotetrabenazine (9-(+)-11C-DTBZ) was shown to be a useful positron emission tomography (PET) imaging agent for various neurodegenerative disorders. Here, we described the radiosynthesis and evaluation of the 9-(+)-11C-DTBZ analog, 10-(+)-11C-DTBZ, as a vesicular mo...

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Published in:PloS one 2016-09, Vol.11 (9), p.e0161295-e0161295
Main Authors: Huang, Zih-Rou, Tsai, Chia-Ling, Huang, Ya-Yao, Shiue, Chyng-Yann, Tzen, Kai-Yuan, Yen, Ruoh-Fang, Hsin, Ling-Wei
Format: Article
Language:English
Subjects:
Amphetamines
Animals
Biology and Life Sciences
Brain
Brain - diagnostic imaging
Brain - metabolism
Carbon
Carbon Radioisotopes
Cerebellum
Chromatography, High Pressure Liquid
Dopamine
Emissions
Hospitals
Imaging
Insurance claims
Laboratory animals
Male
Medical imaging
Medicine and Health Sciences
Methylation
Molecular Imaging
Monoamine transporter
Neostriatum
Nervous system diseases
Neurodegenerative diseases
Neuroimaging
Nuclear medicine
People and Places
Pharmacy
Physical Sciences
Positron emission
Positron emission tomography
Radiochemistry
Radiopharmaceuticals - chemistry
Rats
Research and Analysis Methods
Sodium hydroxide
Studies
Tetrabenazine - analogs & derivatives
Tetrabenazine - chemistry
Tomography
Vesicular amine transporter
Vesicular Monoamine Transport Proteins - metabolism
Vesicular monoamine transporter 2
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cited_by cdi_FETCH-LOGICAL-c725t-2a6caadd2a5a97219a7a302d9f105835bb5a6d1e018758c7b53394b3c8e673693
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container_issue 9
container_start_page e0161295
container_title PloS one
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creator Huang, Zih-Rou
Tsai, Chia-Ling
Huang, Ya-Yao
Shiue, Chyng-Yann
Tzen, Kai-Yuan
Yen, Ruoh-Fang
Hsin, Ling-Wei
description In the early 1990s, 9-(+)-11C-dihydrotetrabenazine (9-(+)-11C-DTBZ) was shown to be a useful positron emission tomography (PET) imaging agent for various neurodegenerative disorders. Here, we described the radiosynthesis and evaluation of the 9-(+)-11C-DTBZ analog, 10-(+)-11C-DTBZ, as a vesicular monoamine transporter 2 (VMAT2) imaging agent and compare it with 9-(+)-11C-DTBZ. 10-(+)-11C-DTBZ was obtained by 11C-MeI methylation with its 10 hydroxy precursor in the presence of 5 M NaOH. It had a slightly better average radiochemical yield of 35.3 ± 3.6% (decay-corrected to end of synthesis (EOS)) than did 9-(+)-11C-DTBZ (30.5 ± 2.3%). MicroPET studies showed that 10-(+)-11C-DTBZ had a striatum-to-cerebellum ratio of 3.74 ± 0.21 at 40 min post-injection, while the ratio of 9-(+)-11C-DTBZ was 2.50 ± 0.33. This indicated that 10-(+)-11C-DTBZ has a higher specific uptake in VMAT2-rich brain regions, and 10-(+)-11C-DTBZ may be a potential VMAT2 radioligand. Our experiment is the first study of 10-(+)-11C-DTBZ to include dynamic brain distribution in rat brains.
doi_str_mv 10.1371/journal.pone.0161295
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subjects Amphetamines
Animals
Biology and Life Sciences
Brain
Brain - diagnostic imaging
Brain - metabolism
Carbon
Carbon Radioisotopes
Cerebellum
Chromatography, High Pressure Liquid
Dopamine
Emissions
Hospitals
Imaging
Insurance claims
Laboratory animals
Male
Medical imaging
Medicine and Health Sciences
Methylation
Molecular Imaging
Monoamine transporter
Neostriatum
Nervous system diseases
Neurodegenerative diseases
Neuroimaging
Nuclear medicine
People and Places
Pharmacy
Physical Sciences
Positron emission
Positron emission tomography
Radiochemistry
Radiopharmaceuticals - chemistry
Rats
Research and Analysis Methods
Sodium hydroxide
Studies
Tetrabenazine - analogs & derivatives
Tetrabenazine - chemistry
Tomography
Vesicular amine transporter
Vesicular Monoamine Transport Proteins - metabolism
Vesicular monoamine transporter 2
title A Novel Potential Positron Emission Tomography Imaging Agent for Vesicular Monoamine Transporter Type 2
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