Skip to Content
MilliporeSigma
  • Preparation and biodistribution of 1-((2-methoxyphenyl) piperazine)ferrocenecarboxamide labeled with technetium-99m as a potential brain receptor imaging agent.

Preparation and biodistribution of 1-((2-methoxyphenyl) piperazine)ferrocenecarboxamide labeled with technetium-99m as a potential brain receptor imaging agent.

European journal of medicinal chemistry (2015-05-21)
Nadia Malek Saied, Najoua Mejri, Radhia El Aissi, Eric Benoist, Mouldi Saidi
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Oxalyl chloride solution, 2.0 M in methylene chloride
Sigma-Aldrich
Oxalyl chloride, reagent grade, 98%
Sigma-Aldrich
Oxalyl chloride, ReagentPlus®, ≥99%
Sigma-Aldrich
Hexane, for residue analysis, JIS 5000
Sigma-Aldrich
Hexane, suitable for HPLC
Sigma-Aldrich
Ethyl acetate, suitable for HPLC
Sigma-Aldrich
Hexane, HPLC Plus, for HPLC, GC, and residue analysis, ≥95%
Sigma-Aldrich
Hexane, ≥96.0%, suitable for residual phthalate analysis
Sigma-Aldrich
Ethyl acetate, JIS 300, ≥99.5%, for residue analysis
Sigma-Aldrich
Ethyl acetate, JIS special grade, ≥99.5%
Sigma-Aldrich
Hexane, JIS 300, ≥96.0%, for residue analysis
Sigma-Aldrich
Ethyl acetate, SAJ first grade, ≥99.0%
Sigma-Aldrich
Hexane, SAJ first grade, ≥95.0%
Sigma-Aldrich
Ethyl acetate, ReagentPlus®, ≥99.8%
Sigma-Aldrich
Sodium iodide, 99.999% trace metals basis
Sigma-Aldrich
Hexane, anhydrous, 95%
Sigma-Aldrich
Ethyl acetate, ACS reagent, ≥99.5%
Sigma-Aldrich
Sodium iodide, ≥99.99% trace metals basis
Sigma-Aldrich
Ethyl acetate, anhydrous, 99.8%
Sigma-Aldrich
Ethyl acetate, ≥99%, FCC, FG
Sigma-Aldrich
Sodium iodide, AnhydroBeads, −10 mesh, 99.999% trace metals basis
Sigma-Aldrich
Ethyl acetate, natural, ≥99%, FCC, FG
Sigma-Aldrich
Hexane, JIS special grade, ≥96.0%
Sigma-Aldrich
Ethyl acetate, JIS 1000, ≥99.5%, for residue analysis
Sigma-Aldrich
Hexane, JIS 1000, ≥96.0%, for residue analysis
Sigma-Aldrich
1-(2-Methoxyphenyl)piperazine, 98%
Sigma-Aldrich
Ethyl acetate
Sigma-Aldrich
Ethyl acetate
Sigma-Aldrich
Sodium iodide, anhydrous, free-flowing, Redi-Dri, ReagentPlus®, ≥99%