In vivo evaluation in cynomolgus monkey brain and metabolism of [¹⁸F]fluorodeprenyl: a new MAO-B pet radioligand

Nag, Sangram; Varrone, Andrea; Tóth, Miklós; Thiele, Andrea; Kettschau, Georg; Heinrich, Tobias; Lehmann, Lutz; Halldin, Christer (2012). In vivo evaluation in cynomolgus monkey brain and metabolism of [¹⁸F]fluorodeprenyl: a new MAO-B pet radioligand. Synapse, 66(4), pp. 323-30. New York, N.Y.: Wiley-Liss 10.1002/syn.21514

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In this study, we evaluated the in vivo characteristics of a new monoamine oxidase type B (MAO-B) radioligand, [¹⁸F]fluorodeprenyl, by positron emission tomography (PET) in two cynomolgus monkeys. The brain uptake of [¹⁸F]fluorodeprenyl was more than 7% (600% SUV) of the total injected radioactivity and similar to that of [¹¹C]deprenyl, an established MAO-B radioligand. The highest uptake was observed in the striatum, one of the MAO-B-rich regions, with a peak at approximately 2-3 min after injection, followed by lower uptake in the thalamus and the cortex and lowest uptake in the cerebellum. Brain uptake of [¹⁸F]fluorodeprenyl was largely inhibited by preadministration of the MAO-B inhibitor, L-deprenyl, whereas clorgyline, a MAO Type A blocker, had no significant inhibitory effect, thus demonstrating selectivity for MAO-B. [¹⁸F]Fluorodeprenyl showed relatively slow metabolism with the presence of two radiometabolite peaks with similar retention time as the labeled metabolites of [¹¹C]deprenyl. These results suggest that [¹⁸F]fluorodeprenyl is a potential PET radioligand for visualization of MAO-B activity.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Department of Intensive Care, Emergency Medicine and Anaesthesiology (DINA) > Clinic and Policlinic for Anaesthesiology and Pain Therapy

UniBE Contributor:

Lehmann, Lutz Eric

ISSN:

0887-4476

Publisher:

Wiley-Liss

Language:

English

Submitter:

Jeannie Wurz

Date Deposited:

04 Oct 2013 14:19

Last Modified:

23 Jan 2018 12:16

Publisher DOI:

10.1002/syn.21514

PubMed ID:

22124971

Web of Science ID:

000299620200005

URI:

https://boris.unibe.ch/id/eprint/6101 (FactScience: 210997)

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