Chemical delivery system of metaiodobenzylguanidine (MIBG) to the central nervous system.
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.
Gourand
Fabienne
F
Groupe de Développements Méthodologiques en Tomographie par Emission de Positons, CEA/DSV/I2BM/CI-NAPS UMR6232, Université de Caen Basse Normandie, Caen, France.
Mercey
Guillaume
G
Ibazizène
Méziane
M
Tirel
Olivier
O
Henry
Joël
J
Levacher
Vincent
V
Perrio
Cécile
C
Barré
Louisa
L
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
D002250:Carbon Radioisotopes; D004337:Drug Carriers; D011806:Quinolinium Compounds; D019275:Radiopharmaceuticals; D019797:3-Iodobenzylguanidine