Synthesis and in vivo evaluation of [(11)C]CGP62349, a new GABA(B) receptor antagonist.

Abstract:

:This paper describes the radiosynthesis of [(11)C]CGP62349, a potential ligand to assess GABA(B) receptors in vivo. (11)C was introduced by O-methylation of the corresponding des-methyl precursor, namely CGP67780. The final product was obtained with a reliable method in good yield. The radioligand was tested in monkey, revealing negligible blood-brain barrier penetration and brain uptake, thus prompting us to search for a new target structure with a better lipophilicity.

journal_name

Nucl Med Biol

authors

Todde S,Moresco RM,Fröstl W,Stampf P,Matarrese M,Carpinelli A,Magni F,Galli Kienle M,Fazio F

doi

10.1016/s0969-8051(00)00124-4

keywords:

subject

Has Abstract

pub_date

2000-08-01 00:00:00

pages

565-9

issue

6

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(00)00124-4

journal_volume

27

pub_type

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