期刊
ACS CHEMICAL NEUROSCIENCE
卷 5, 期 7, 页码 611-615出版社
AMER CHEMICAL SOC
DOI: 10.1021/cn500078e
关键词
[F-18]flourination; nickel-mediated; serotonin receptors; 5HT(2a); MDL100907; PET imaging
资金
- Department of Energy [DE-SC0008430]
- National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health
- NIH
- NIH [T90DA022759/R90DA023427]
- [S10RR017208]
- [S10RR026666]
- [S10RR022976]
- [S10RR019933]
- [S10RR02949S]
- U.S. Department of Energy (DOE) [DE-SC0008430] Funding Source: U.S. Department of Energy (DOE)
Several voids exist in reliable positron emission tomography (PET) radioligands for quantification of the serotonin (5HT) receptor system. Even in cases where 5HT radiotracers exist, challenges remain that have limited the utility of 5HT imaging in clinical research. Herein we address an unmet need in 5HT(2a) imaging using innovative chemistry. We report a scalable and robust synthesis of [F-18]MDL100907, which was enabled by a Ni-mediated oxidative fluorination using [F-18]fluoride. This first demonstration of a Ni-mediated fluorination used for PET imaging required development of a new reaction strategy that ultimately provided high specific activity [F-18]MDL100907. Using the new synthetic strategy and optimized procedure, [F-18]MDL100907 was evaluated against [C-11]MDL100907 for reliability to quantify 5HT(2a), in the nonhuman primate brain and was found to be superior based on a single scan analysis using the same nonhuman primate. The use of this new 5HT(2a) racliotracer will afford clinical neuroscience research the ability to distinguish 5HT(2a) receptor abnormalities binding between healthy subjects and patients even when group differences are small.
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