当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > N-(6-18F-fluorohexyl)-N-methylpropargylamine: a fluorine-18-labeled monoamine oxidase B inhibitor for potential use in PET studies.

N-(6-18F-fluorohexyl)-N-methylpropargylamine: a fluorine-18-labeled monoamine oxidase B inhibitor for potential use in PET studies.

Abstract：

:We have synthesized N-(6-18F-fluorohexyl)-N-methylpropargylamine (18F-FHMP) as a positron emission tomography (PET) radiotracer for monoamine oxidase B (MAO-B). The radiosynthesis was carried out by a fluorine-for-bromine substitution in 30-40% radiochemical yield in specific activities of 1-2 Ci/micromol. Selectivity for MAO-B was demonstrated by the high affinity of (R)-deprenyl (IC50 = 6.8 nM) and lower affinity of clorgyline (IC50 = 1.2 microM) for the inhibition of 18F-FHMP binding in vitro in rat brain homogenates. In vitro autoradiographic studies in rat brain slices showed localization of 18F-FHMP in regions such as the ependyma of the lateral ventricle, dorsal raphe, area postrema, and other regions such as the cerebellum. The specific binding observed in the autoradiograms was displaced by preincubation with (R)-deprenyl. In in vivo experiments, the uptake of 18F-FHMP in the rat brains was high (0.10-0.20% injected dose/g). The binding of 18F-FHMP in the rat brain correlated with the general distribution of MAO-B and was displaced completely by preadministration of 10 microM (R)-deprenyl. These results suggest that 18F-FHMP is a potential PET radiotracer for MAO-B for use in in vitro and in vivo experiments.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Mukherjee J,Yang ZY,Lew R

doi

10.1016/s0969-8051(98)00061-4

keywords:

subject

Has Abstract

pub_date

1999-01-01 00:00:00

pages

111-6

issue

1

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(98)00061-4

journal_volume

26

pub_type

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