N-[ 18F]fluoroethylpiperidin-4-ylmethyl butyrate: a novel radiotracer for quantifying brain butyrylcholinesterase activity by positron emission tomography

In Alzheimer's disease, cerebral cortical butyrylcholinesterase (BChE) activity is reported to be elevated. Our aim was to develop a novel 18F-labeled tracer for quantifying cerebral BChE activity by positron emission tomography. With in vitro screening of N-[ 14C]ethylpiperidin-3- and 4-ylmeth...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-04, Vol.14 (8), p.1927-1930
Hauptverfasser:	Kikuchi, Tatsuya, Zhang, Ming-Rong, Ikota, Nobuo, Fukushi, Kiyoshi, Okamura, Toshimitsu, Suzuki, Kazutoshi, Arano, Yasushi, Irie, Toshiaki
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - analysis Acetylcholinesterase - metabolism Biological and medical sciences Brain - diagnostic imaging Brain - enzymology Butyrates - chemical synthesis Butyrates - chemistry Butyrylcholinesterase - analysis Butyrylcholinesterase - metabolism Contrast media. Radiopharmaceuticals Fluorine Radioisotopes Humans Hydrolysis Medical sciences Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Positron emission tomography Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - chemistry Substrate Specificity Tomography, Emission-Computed - methods
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Zusammenfassung:	In Alzheimer's disease, cerebral cortical butyrylcholinesterase (BChE) activity is reported to be elevated. Our aim was to develop a novel 18F-labeled tracer for quantifying cerebral BChE activity by positron emission tomography. With in vitro screening of N-[ 14C]ethylpiperidin-3- and 4-ylmethyl esters, N-[ 14C]ethylpiperidin-4-ylmethyl butyrate was selected as a lead for 18F-labeling, affording N-[ 18F]fluoroethylpiperidin-4-ylmethyl butyrate. The 18F-labeled butyrate showed the required properties for in vivo BChE measurement, that is, the lipophilic nature of the authentic ester, high specificity to BChE, a moderate hydrolysis rate, and the hydrophilic nature of the metabolite. Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.01.080