In vivo evaluation of [123I]-4-iodo-N-(4-(4-(2-methoxyphenyl)-piperazin-1-yl)butyl)-benzamide: a potential sigma receptor ligand for SPECT studies

Staelens, Ludovicus; Oltenfreiter, Ruth; Dumont, Filip; Waterhouse, Rikki N.; Vandenbulcke, Katia; Blanckaert, Peter; Dierckx, Rudi; Slegers, Guido

doi:10.1016/j.nucmedbio.2004.09.007

Cited by 9 publications

(4 citation statements)

References 6 publications

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“…Although it is not known whether B16F1 cells used in our study express sigma receptors, various other tumor cell lines such as PC12, A375 amelanotic melanoma, T47D breast ductal carcimona, SK-N-SH neuroblastoma, and C6 glioma cells highly express sigma receptors. Since these tumor cell lines also show high binding to iodobenzamides, several investigators hypothesized that the binding ability of iodobenzamides to sigma receptors could be exploited to image melanoma and other tumors − . For that reason, John et al synthesized a series of iodobenzamides that showed high sigma receptor binding and displayed varying efficacy to image various tumors , .…”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[¹⁸F]fluorobenzamide ([¹⁸F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

et al. 2009

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In order to develop a PET radiopharmaceutical to image malignant melanoma, we synthesized N-(2-diethylaminoethyl)-4-[18F]fluorobenzamide ([18F]-DAFBA). In vitro studies show a high uptake of [18F]-DAFBA by the B16F1 melanoma cells. No significant binding was seen for DAFBA to the sigma-1 and sigma-2 receptors in vitro. The in vivo biodistribution studies performed in normal ICR mice showed a low uptake in the normal tissues followed by further elimination of radioactivity from these tissues with time. The biodistribution studies performed in C57 mice bearing melanoma tumor xenograft showed a rapid uptake of radioactivity in the tumor that reached a plateau within 30 min post injection. The F-18 uptake in the tumor was 7.00±2.76, 6.57±1.66, and 5.80±0.98 %ID/g at 60, 120, and 180 min, respectively. A steady uptake of radioactivity in the tumor and low uptake in normal tissues resulted in high tumor to normal tissue ratios. For example, at 180 min post-injection, the tumor to tissue ratios were 14.90±6.47, 21.90±4.68, 32.91±6.11, 36.73±5.61, and 6.33±1.9, for the spleen, lungs, muscle, blood, and liver, respectively. The radioactivity rapidly cleared from the blood pool and it decrease from 0.58±0.18 %ID/g at 60 min to 0.13±0.03 %ID/g at 180 min. The F-18 uptake in the bones at 60, 120, and 180 min was 0.91±0.27, 0.57±0.32, and 0.17±0.05 %ID/g, respectively. This low uptake in the bones reflects its in vivo resistance towards de-fluorination. A low residual activity in normal tissues and a high tumor uptake signifies a superior imaging potential of this compound. Owing to these positive traits, [18F]-DAFBA could help delineate tumor and its metastases when used for imaging application. Further in vivo studies are underway to assess potential of [18F]-DAFBA as a promising PET imaging probe.

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Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[¹⁸F]fluorobenzamide ([¹⁸F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

et al. 2009

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“…However, the mechanisms involved in the ability of radioiodine-labelled BZAs to image melanoma were misunderstood at first. Various tumour cell lines with sigma receptors, including PC12, amelanotic A375 melanoma, neuroblastoma SK-N-SH, and C6 glioma cells, demonstrate high affinity for iodoBZAs [28,29]. IodoBZAs also bind to pigmented melanoma, leading to the hypothesis that iodoBZAs bind to sigma receptors [30,31].…”

Section: Discussionmentioning

confidence: 99%

Imaging malignant melanoma with 18F-5-FPN

Feng

Xia

et al. 2015

Eur J Nucl Med Mol Imaging

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“…6,7 The high expression of sigma receptors in tumors suggested that sigma receptors selective ligands could play an important role as biomarkers of tumor diagnosis by SPECT scintigraphy and PET analysis. 8 Significant progress has been made in the development of 11 C-and 18 F-labeled sigma receptors ligands for PET imaging and 123 I-labeled sigma receptors ligands for SPECT imaging, such as benzamides, [9][10][11][12][13] disubstituted piperidines [14][15][16][17][18] and piperazines. 19,20 Compared to 11 C, 18 F and 123 I, 99m Tc is the most common radionuclide in routine nuclear medicine due to its almost ideal physical decay properties (T 1=2 ¼ 6:02 h, E g ¼ 140 keV) and the availability through commercial …”

Section: Introductionmentioning

confidence: 99%

Preparation and biological evaluation of ^99mTcN‐4‐(cyclohexylpiperazin‐1‐yl)‐dithioformate as a potential sigma receptor imaging agent

Lü

Kong

Jia

et al. 2007

Labelled Comp Radiopharmac

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TcN-2 had good tumor uptake (2:12 AE 0:01 %ID=g at 2 h p.i.) and moderate brain uptake (0:27 AE 0:05 %ID=g at 2 h p.i.). After blocking with haloperidol, the uptakes by tumor and brain were lower than control. The results indicated that the complex has specific binding to the s receptors in vivo. Further structural modifications of this complex are needed to obtain 99m Tc-based s receptor imaging agents with high affinity and subtype selectivity.

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In vivo evaluation of [123I]-4-iodo-N-(4-(4-(2-methoxyphenyl)-piperazin-1-yl)butyl)-benzamide: a potential sigma receptor ligand for SPECT studies

Cited by 9 publications

References 6 publications

Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[¹⁸F]fluorobenzamide ([¹⁸F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[¹⁸F]fluorobenzamide ([¹⁸F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

Imaging malignant melanoma with 18F-5-FPN

Preparation and biological evaluation of ^99mTcN‐4‐(cyclohexylpiperazin‐1‐yl)‐dithioformate as a potential sigma receptor imaging agent

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In vivo evaluation of [123I]-4-iodo-N-(4-(4-(2-methoxyphenyl)-piperazin-1-yl)butyl)-benzamide: a potential sigma receptor ligand for SPECT studies

Cited by 9 publications

References 6 publications

Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[18F]fluorobenzamide ([18F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[18F]fluorobenzamide ([18F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

Imaging malignant melanoma with 18F-5-FPN

Preparation and biological evaluation of 99mTcN‐4‐(cyclohexylpiperazin‐1‐yl)‐dithioformate as a potential sigma receptor imaging agent

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Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[¹⁸F]fluorobenzamide ([¹⁸F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[¹⁸F]fluorobenzamide ([¹⁸F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

Preparation and biological evaluation of ^99mTcN‐4‐(cyclohexylpiperazin‐1‐yl)‐dithioformate as a potential sigma receptor imaging agent