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Chemical Delivery System of Metaiodobenzylguanidine (MIBG) to the Central Nervous System

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journal contribution
posted on 11.02.2010, 00:00 by Fabienne Gourand, Guillaume Mercey, Méziane Ibazizène, Olivier Tirel, Joël Henry, Vincent Levacher, Cécile Perrio, Louisa Barré
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 [11C]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.