The effect of aromatic fluorine substitution in L-DOPA on the in vivo behaviour of [18F]2-, [18F]5- and [18F]6-fluoro-L-DOPA in the human brain

Raman Chirakal; Neil Vasdev; Marie Claude Asselin; Gary J. Schrobilgen; Claude Nahmias

doi:10.1016/S0022-1139(02)00025-8

The effect of aromatic fluorine substitution in L-DOPA on the in vivo behaviour of [¹⁸F]2-, [¹⁸F]5- and [¹⁸F]6-fluoro-L-DOPA in the human brain

Raman Chirakal^*, Neil Vasdev, Marie Claude Asselin, Gary J. Schrobilgen, Claude Nahmias

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

10 Citations (Scopus)

Abstract

Remarkable differences in the human in vivo behaviour of each of the three [¹⁸F]-labelled ring fluorinated isomers of l-dihydroxyphenylalanine (L-DOPA) are presented. Unlike [¹⁸F]2-fluoro-L-DOPA, which did not appear to cross the blood brain barrier, [¹⁸F]5-fluoro-L-DOPA appears to be taken up and cleared from the cerebellum and the striata. In contrast with the 2- and 5-fluoro isomers of L-DOPA, radioactivity derived after injection of [¹⁸F]6-fluoro-L-DOPA is specifically retained in the striata. The present study is the first direct comparison of the time course and distribution of radioactivity in the human brain after intravenous injections of [¹⁸F]2-, [¹⁸F]5- and [¹⁸F]6-fluoro-L-DOPA.

Original language	English
Pages (from-to)	33-39
Number of pages	7
Journal	Journal of Fluorine Chemistry
Volume	115
Issue number	1
DOIs	https://doi.org/10.1016/S0022-1139(02)00025-8
Publication status	Published - 2002
Externally published	Yes

Bibliographical note

Funding Information:
We wish to thank Margo Thompson for her untiring support and Dr. Shigeko Amano for helpful discussions. N.V. and M.C.A. wish to thank the Natural Sciences and Engineering Research Council of Canada for postgraduate scholarships and the Christie Group Ltd. for awarding E.S. Garnett Bursaries in Medical Imaging.

Keywords

Brain uptake
F
Fluoro-L-DOPA
L-DOPA
Positron emission tomography

Access to Document

10.1016/S0022-1139(02)00025-8

Cite this

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title = "The effect of aromatic fluorine substitution in L-DOPA on the in vivo behaviour of [18F]2-, [18F]5- and [18F]6-fluoro-L-DOPA in the human brain",

abstract = "Remarkable differences in the human in vivo behaviour of each of the three [18F]-labelled ring fluorinated isomers of l-dihydroxyphenylalanine (L-DOPA) are presented. Unlike [18F]2-fluoro-L-DOPA, which did not appear to cross the blood brain barrier, [18F]5-fluoro-L-DOPA appears to be taken up and cleared from the cerebellum and the striata. In contrast with the 2- and 5-fluoro isomers of L-DOPA, radioactivity derived after injection of [18F]6-fluoro-L-DOPA is specifically retained in the striata. The present study is the first direct comparison of the time course and distribution of radioactivity in the human brain after intravenous injections of [18F]2-, [18F]5- and [18F]6-fluoro-L-DOPA.",

keywords = "Brain uptake, F, Fluoro-L-DOPA, L-DOPA, Positron emission tomography",

author = "Raman Chirakal and Neil Vasdev and Asselin, {Marie Claude} and Schrobilgen, {Gary J.} and Claude Nahmias",

note = "Funding Information: We wish to thank Margo Thompson for her untiring support and Dr. Shigeko Amano for helpful discussions. N.V. and M.C.A. wish to thank the Natural Sciences and Engineering Research Council of Canada for postgraduate scholarships and the Christie Group Ltd. for awarding E.S. Garnett Bursaries in Medical Imaging. ",

year = "2002",

doi = "10.1016/S0022-1139(02)00025-8",

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pages = "33--39",

journal = "Journal of Fluorine Chemistry",

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AU - Chirakal, Raman

AU - Vasdev, Neil

AU - Asselin, Marie Claude

AU - Schrobilgen, Gary J.

AU - Nahmias, Claude

N1 - Funding Information: We wish to thank Margo Thompson for her untiring support and Dr. Shigeko Amano for helpful discussions. N.V. and M.C.A. wish to thank the Natural Sciences and Engineering Research Council of Canada for postgraduate scholarships and the Christie Group Ltd. for awarding E.S. Garnett Bursaries in Medical Imaging.

PY - 2002

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N2 - Remarkable differences in the human in vivo behaviour of each of the three [18F]-labelled ring fluorinated isomers of l-dihydroxyphenylalanine (L-DOPA) are presented. Unlike [18F]2-fluoro-L-DOPA, which did not appear to cross the blood brain barrier, [18F]5-fluoro-L-DOPA appears to be taken up and cleared from the cerebellum and the striata. In contrast with the 2- and 5-fluoro isomers of L-DOPA, radioactivity derived after injection of [18F]6-fluoro-L-DOPA is specifically retained in the striata. The present study is the first direct comparison of the time course and distribution of radioactivity in the human brain after intravenous injections of [18F]2-, [18F]5- and [18F]6-fluoro-L-DOPA.

AB - Remarkable differences in the human in vivo behaviour of each of the three [18F]-labelled ring fluorinated isomers of l-dihydroxyphenylalanine (L-DOPA) are presented. Unlike [18F]2-fluoro-L-DOPA, which did not appear to cross the blood brain barrier, [18F]5-fluoro-L-DOPA appears to be taken up and cleared from the cerebellum and the striata. In contrast with the 2- and 5-fluoro isomers of L-DOPA, radioactivity derived after injection of [18F]6-fluoro-L-DOPA is specifically retained in the striata. The present study is the first direct comparison of the time course and distribution of radioactivity in the human brain after intravenous injections of [18F]2-, [18F]5- and [18F]6-fluoro-L-DOPA.

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