title: Chemical delivery system of metaiodobenzylguanidine (MIBG) to the central nervous system.
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.
authors.affiliation: Groupe de Développements Méthodologiques en Tomographie par Emission de Positons, CEA/DSV/I2BM/CI-NAPS UMR6232, Université de Caen Basse Normandie, Caen, France.
authors.forename: Fabienne
authors.initials: F
authors.lastname: Gourand
authors.forename: Guillaume
authors.initials: G
authors.lastname: Mercey
authors.forename: Méziane
authors.initials: M
authors.lastname: Ibazizène
authors.forename: Olivier
authors.initials: O
authors.lastname: Tirel
authors.forename: Joël
authors.initials: J
authors.lastname: Henry
authors.forename: Vincent
authors.initials: V
authors.lastname: Levacher
authors.forename: Cécile
authors.initials: C
authors.lastname: Perrio
authors.forename: Louisa
authors.initials: L
authors.lastname: Barré
mesh_terms: D019797:3-Iodobenzylguanidine / Q000008:administration & dosage*; D000818:Animals; D001812:Blood-Brain Barrier / Q000187:drug effects*; D001921:Brain / Q000187:drug effects* / Q000378:metabolism*; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D008297:Male; D010084:Oxidation-Reduction; D011806:Quinolinium Compounds / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000008:administration & dosage*; D051381:Rats; D017207:Rats, Sprague-Dawley; D021241:Spectrometry, Mass, Electrospray Ionization; D014018:Tissue Distribution
chemical_list: D002250:Carbon Radioisotopes; D004337:Drug Carriers; D011806:Quinolinium Compounds; D019275:Radiopharmaceuticals; D019797:3-Iodobenzylguanidine