title: Preparation and biodistribution of 1-((2-methoxyphenyl) piperazine)ferrocenecarboxamide labeled with technetium-99m as a potential brain receptor imaging agent.
abstract: The goal of this study is to develop a novel brain receptor imaging agent. This study reports the synthesis, characterization and the biological evaluation of 1-((2-methoxyphenyl) piperazine)ferrocenecarboxamide labeled with technetium-99 m ((99m)Tc-MP). The (99m)Tc-MP was obtained quickly (radiolabelling time < 5 min), in 90% yield. The (99m)Tc-complex, characterized by HPLC (20-50% ACN of 0 at 5 min then 50% ACN of 5 at 17 min to finally with 50 at 20% ACN of 17 at 20 min), is stable, neutral and lipophilic enough to cross the blood-brain barrier which was confirmed by octanol/water partition coefficient (LogP = 1.82). In vivo biodistribution indicated that this complex had exceptional brain uptake (2.47% ID/g at 5 min and 0.75% ID/g at 60 min). The distribution of the activity at 15 min post-injection in various rat brain regions showed a higher accumulation in the hippocampus area. After blocking with 8-hydroxy-2-(dipropylamino) tetralin, the uptake of hippocampus was decreased significantly from 0.87% ID/g to 0.21% ID/g at 15 min p.i., while the cerebellum had no significant decrease. The new (99m)Tc-cyclopentadienyltricarbonyl technetium complex reported here showed promising biological results, making it an interesting starting point for the development of a new (99m)Tc-complex as brain receptor imaging agent.
authors.affiliation: Radiopharmaceutical Unit, National Centre of Sciences and Nuclear Technology, Sidi Thabet 2020, Tunisia. Electronic address: nadia.malek@gmail.com.
authors.forename: Nadia Malek
authors.initials: NM
authors.lastname: Saied
authors.affiliation: Radiopharmaceutical Unit, National Centre of Sciences and Nuclear Technology, Sidi Thabet 2020, Tunisia.
authors.forename: Najoua
authors.initials: N
authors.lastname: Mejri
authors.affiliation: Radiopharmaceutical Unit, National Centre of Sciences and Nuclear Technology, Sidi Thabet 2020, Tunisia; CNRS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, SPCMIB, UMR 5068, 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France; Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, SPCMIB, UMR 5068, 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France.
authors.forename: Radhia
authors.initials: R
authors.lastname: El Aissi
authors.affiliation: CNRS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, SPCMIB, UMR 5068, 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France; Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, SPCMIB, UMR 5068, 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France.
authors.forename: Eric
authors.initials: E
authors.lastname: Benoist
authors.affiliation: Radiopharmaceutical Unit, National Centre of Sciences and Nuclear Technology, Sidi Thabet 2020, Tunisia.
authors.forename: Mouldi
authors.initials: M
authors.lastname: Saidi
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D006624:Hippocampus / Q000000981:diagnostic imaging* / Q000378:metabolism; D008297:Male; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D010879:Piperazines / Q000138:chemical synthesis / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000032:analysis*; D014018:Tissue Distribution
chemical_list: D015609:Organotechnetium Compounds; D010879:Piperazines; D019275:Radiopharmaceuticals; D011985:Receptors, Serotonin
keywords: (99m)Tc-tricarbonyl complex; 1-(2-methoxyphenyl) piperazine; Radiopharmaceuticals