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Journal of Nuclear Medicine

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OtherBrief Communications

Preclinical Comparison of 111In-Labeled DTPA- or DOTA-Bombesin Analogs for Receptor-Targeted Scintigraphy and Radionuclide Therapy

Wouter A.P. Breeman, Marion de Jong, Jack L. Erion, Joseph E. Bugaj, Ananth Srinivasan, Bert F. Bernard, Dik J. Kwekkeboom, Theo J. Visser and Eric P. Krenning
Journal of Nuclear Medicine December 2002, 43 (12) 1650-1656;
Wouter A.P. Breeman
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Marion de Jong
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Jack L. Erion
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Joseph E. Bugaj
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Ananth Srinivasan
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Bert F. Bernard
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Dik J. Kwekkeboom
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Theo J. Visser
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Eric P. Krenning
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  • FIGURE 1.
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    FIGURE 1.

    Amino acid sequence of GRP and BN analogs. Common C-terminal 7 amino acids in GRP and BN analogs are indicated in boldface type.

  • FIGURE 2.
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    FIGURE 2.

    Specific binding and internalization (dotted) of 111In-labeled BN analogs by GRP receptor-positive CA20948 (A) and AR42J (B) rat pancreatic tumor cells. 5° and 37° = 5°C and 37°C, respectively. Data are expressed as % dose per mg of protein.

  • FIGURE 3.
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    FIGURE 3.

    Tissue distribution of 111In-labeled [DTPA-Pro1,Tyr4]BN, [DOTA-Pro1,Tyr4]BN, [DTPA-ε-Lys3,Tyr4]BN, and [DOTA-ε-Lys3,Tyr4]BN in rats 24 h after administration of radioligand. Nonspecific uptake of radioactivity (striped) was determined by coinjection of GRP receptor-blocking dose of 0.1 mg [Tyr4]BN. Difference between total uptake and nonspecific uptake represents specific binding of radioligand to GRP receptor. Data are expressed as %ID per gram of tissue and presented as means ± SD (n = 3).

  • FIGURE 4.
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    FIGURE 4.

    Tissue-to-blood ratio of 111In-labeled [DTPA-Pro1,Tyr4]BN, [DOTA-Pro1,Tyr4]BN, [DTPA-ε-Lys3,Tyr4]BN, and [DOTA-ε-Lys3,Tyr4]BN in rats 24 h after administration of radioligand. Nonspecific uptake of radioactivity (striped) was determined by coinjection of GRP receptor-blocking dose of 0.1 mg [Tyr4]BN. Data are expressed as ratio of %ID per gram of tissue versus that in blood and presented as means ± SD (n = 3).

  • FIGURE 5.
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    FIGURE 5.

    Distribution of radioactivity in AR42J tumor-bearing rat 24 h after administration of 15 MBq (0.1 μg) [111In-DOTA-Pro1,Tyr4]BN. Note uptake in tumor and physiologic uptake in kidneys.

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Journal of Nuclear Medicine
Vol. 43, Issue 12
December 1, 2002
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Preclinical Comparison of 111In-Labeled DTPA- or DOTA-Bombesin Analogs for Receptor-Targeted Scintigraphy and Radionuclide Therapy
Wouter A.P. Breeman, Marion de Jong, Jack L. Erion, Joseph E. Bugaj, Ananth Srinivasan, Bert F. Bernard, Dik J. Kwekkeboom, Theo J. Visser, Eric P. Krenning
Journal of Nuclear Medicine Dec 2002, 43 (12) 1650-1656;

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Preclinical Comparison of 111In-Labeled DTPA- or DOTA-Bombesin Analogs for Receptor-Targeted Scintigraphy and Radionuclide Therapy
Wouter A.P. Breeman, Marion de Jong, Jack L. Erion, Joseph E. Bugaj, Ananth Srinivasan, Bert F. Bernard, Dik J. Kwekkeboom, Theo J. Visser, Eric P. Krenning
Journal of Nuclear Medicine Dec 2002, 43 (12) 1650-1656;
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