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

Add time:08/27/2019    Source:sciencedirect.com

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 (99mTc-MP). The 99mTc-MP was obtained quickly (radiolabelling time < 5 min), in 90% yield. The 99mTc-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 99mTc-cyclopentadienyltricarbonyl technetium complex reported here showed promising biological results, making it an interesting starting point for the development of a new 99mTc-complex as brain receptor imaging agent.

We also recommend Trading Suppliers and Manufacturers of 1-(2-METHOXYPHENYL)-2-PROPANOL 98 (cas 15541-26-1). Pls Click Website Link as below: cas 15541-26-1 suppliers

Prev:The fate of N1′-methanesulphonyl-N4′-(9-acridinyl) -3′ -methoxy-2′,5′ -cyclohexadiene-1′,4′-diimine (m-aqdi), the primary oxidative metabolite of amsacrine, in transformed chinese hamster fibroblasts☆
Next:Synthesis and evaluation of 1-(cyclopropylmethyl)-4-(4-[11C]methoxyphenyl)-piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile ([11C]CMDC) for PET imaging of metabotropic glutamate receptor 2 in the rat brain)