| Title : N-[18F]fluoroethylpiperidin-4-ylmethyl butyrate: a novel radiotracer for quantifying brain butyrylcholinesterase activity by positron emission tomography - Kikuchi_2004_Bioorg.Med.Chem.Lett_14_1927 |
| Author(s) : Kikuchi T , Zhang MR , Ikota N , Fukushi K , Okamura T , Suzuki K , Arano Y , Irie T |
| Ref : Bioorganic & Medicinal Chemistry Lett , 14 :1927 , 2004 |
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Abstract :
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. |
| PubMedSearch : Kikuchi_2004_Bioorg.Med.Chem.Lett_14_1927 |
| PubMedID: 15050629 |
| Substrate | Methyl-4-piperidinyl-N-butyrate |
Kikuchi T, Zhang MR, Ikota N, Fukushi K, Okamura T, Suzuki K, Arano Y, Irie T (2004)
N-[18F]fluoroethylpiperidin-4-ylmethyl butyrate: a novel radiotracer for quantifying brain butyrylcholinesterase activity by positron emission tomography
Bioorganic & Medicinal Chemistry Lett
14 :1927
Kikuchi T, Zhang MR, Ikota N, Fukushi K, Okamura T, Suzuki K, Arano Y, Irie T (2004)
Bioorganic & Medicinal Chemistry Lett
14 :1927