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

Fabienne Gourand (1) , Guillaume Mercey (2) , Méziane Ibazizène (2) , Olivier Tirel (3) , Joël Henry (4) , Vincent Levacher (5) , Cécile Perrio , Louisa Barré (2)

1 CI-NAPS - UMR 6232 - Centre-Imagerie, Neurosciences, et Application aux Pathologies
2 LDM-TEP - Laboratoire de Développements Méthodologiques en Tomographie par Emission de Positons
3 Service d'anesthésie réanimation chirurgicale [Rennes]
4 BOREA - Biologie des Organismes et Ecosystèmes Aquatiques
5 COBRA - Chimie Organique et Bioorganique : Réactivité et Analyse

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.

Domaines: Chimie organique

Fabienne Gourand, Guillaume Mercey, Méziane Ibazizène, Olivier Tirel, Joël Henry, et al.. Chemical delivery system of metaiodobenzylguanidine (MIBG) to the central nervous system.. Journal of Medicinal Chemistry, 2010, 53 (3), pp.1281-1287. ⟨10.1021/jm901550z⟩. ⟨hal-00992135⟩