| Autor: |
Kikuchi T; Department of Medical Imaging, National Institute of Radiological Sciences, Chiba 263-8555, Japan., Zhang MR, Ikota N, Fukushi K, Okamura T, Suzuki K, Arano Y, Irie T |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Apr 19; Vol. 14 (8), pp. 1927-30. |
| DOI: |
10.1016/j.bmcl.2004.01.080 |
| Abstrakt: |
In Alzheimer's disease, cerebral cortical butyrylcholinesterase (BChE) activity is reported to be elevated. Our aim was to develop a novel (18)F-labeled tracer for quantifying cerebral BChE activity by positron emission tomography. With in vitro screening of N-[(14)C]ethylpiperidin-3- and 4-ylmethyl esters, N-[(14)C]ethylpiperidin-4-ylmethyl butyrate was selected as a lead for (18)F-labeling, affording N-[(18)F]fluoroethylpiperidin-4-ylmethyl butyrate. The (18)F-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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
Full Text from ScienceDirect