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




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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.



Author: Zih-Rou Huang, Chia-Ling Tsai, Ya-Yao Huang, Chyng-Yann Shiue, Kai-Yuan Tzen, Ruoh-Fang Yen, Ling-Wei Hsin

Source: http://plos.srce.hr/



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