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Novel 99mTc labeled σ receptor ligand as a potential tumor imaging agent

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Abstract

A novel 99mTc labeled complex, [N-[2-((2-oxo-2-(4-(3-phenylpropyl)piperazin-1-yl)ethyl) (2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato]Technetium(V) oxide (PPPE-MAMA’-99mTcO) ([99m Tc]-2) has been designed and prepared based on the integrated approach. The corresponding rhenium complex (PPPE-MAMA’-ReO)(Re-2) has been prepared and characterized. In vitro competition binding assays show moderate affinity of Re-2 towards σ1 and σ2 receptors with K i values of 8.67 ± 0.07 and 5.71 ± 1.88 μmol, respectively. Planar images obtained at 0.5 h, 4 h, 20 h after i.v. injection indicate the accumulation of [99m Tc]-2 in MCF-7 human breast tumor bearing mice at 20 h. Furthermore, the accumulation of [99m Tc]-2 has been inhibited at 20 h after co-injection of [99m Tc]-2 plus haloperidol (1 mg/kg). Biodistribution studies of [99m Tc]-2 display an in vivo tumor uptake of 0.14% ± 0.01% ID/g at 24 h post i.v. injection with a tumor/muscle ratio of 6.02 ± 0.87. The above results suggest that [99m Tc]-2, derived from a previously published lead compound, retains certain tumor uptake and affinity for σ receptors. [99m Tc]-2 may be used as a basis for further structural modifications to develop tumor imaging agents with high affinity for σ receptors.

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Authors and Affiliations

  1. Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, Department of Chemistry, Beijing Normal University, Beijing, 100875, China

    Fan Caiyun, Jia Hongmei & Liu Boli

  2. Institute of Interdisciplinary Isotope Research, Permoserstr. 15, 04318, Leipzig, Germany

    Deuther-Conrad Winnie, Brust Peter & Steinbach Jörg

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  1. Fan Caiyun
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Correspondence to Liu Boli.

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Fan, C., Jia, H., Deuther-Conrad, W. et al. Novel 99mTc labeled σ receptor ligand as a potential tumor imaging agent. SCI CHINA SER B 49, 169–176 (2006). https://doi.org/10.1007/s11426-006-0169-z

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  • DOI: https://doi.org/10.1007/s11426-006-0169-z

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