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• W4296570948 abstract "Thiocyanate (SCN-) alters the potency of certain agonists for the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, and dysfunctions in AMPA receptor signaling are considered to underlie a number of neurological diseases. While humans may be exposed to SCN- from the environment, including food sources, a carrier-mediated system transports SCN- from the brain into the blood and is an important regulator of SCN- distribution in the central nervous system. The assessment of this SCN- efflux system in the brain would thus be useful for understanding the mechanisms underlying the neurotoxicity of SCN- and for elucidating the relationship between the efflux system and brain diseases. However, the currently available technique for studying SCN- efflux is severely limited by its invasiveness. Here, we describe the development of a SCN- protracer, 9-pentyl-6-[11C]thiocyanatopurine ([11C]1), to overcome this limitation. [11C]1 was synthesized by the reaction of the iodo-precursor and [11C]SCN- or the reaction of the disulfide precursor with [11C]NH4CN. The protracer [11C]1 entered the brain after intravenous injection into mice and was rapidly metabolized to [11C]SCN-, which was then eliminated from the brain. The efflux of [11C]SCN- was dose-dependently inhibited by perchlorate, a monovalent anion, and the highest dose caused an 82% reduction in the efflux rate. Our findings demonstrate that [11C]1 can be used for the noninvasive and quantitative assessment of the SCN- efflux system in the brain." @default.
• W4296570948 created "2022-09-21" @default.
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• W4296570948 date "2022-08-11" @default.
• W4296570948 modified "2023-09-24" @default.
• W4296570948 title "¹¹C-Labeled Radiotracer for Noninvasive and Quantitative Assessment of the Thiocyanate Efflux System in the Brain" @default.
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• W4296570948 doi "https://doi.org/10.1021/acs.bioconjchem.2c00277" @default.
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