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. 2010 Feb 11;53(3):1281-7.
doi: 10.1021/jm901550z.

Chemical delivery system of metaiodobenzylguanidine (MIBG) to the central nervous system

Fabienne Gourand  1 , Guillaume Mercey, Méziane Ibazizène, Olivier Tirel, Joël Henry, Vincent Levacher, Cécile Perrio, Louisa Barré
Affiliations

Chemical delivery system of metaiodobenzylguanidine (MIBG) to the central nervous system

Fabienne Gourand et al. J Med Chem. .

Abstract

The aim of the present investigation was to apply a chemical delivery system (CDS) to MIBG (4) with the purpose of delivering this drug to the CNS. Compound 4 has been linked to a 1,4-dihydroquinoline moiety in order to achieve its CNS penetration, and here we report the synthesis to link 4 to the chemical delivery system and the radiosynthesis with carbon-11 of the "CDS-4 entity". After iv injection into rats of the [(11)C]CDS-4, the follow-up study of the radioactivity distribution in blood samples and brain homogenates and the analysis by HPLC and LC-MS/MS have confirmed the release of 4 into the CNS.

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