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Research ArticleBasic Science Investigations

Preclinical Evaluation of 99mTc(CO)3-Aspartic-N-Monoacetic Acid, a Renal Radiotracer with Pharmacokinetic Properties Comparable to 131I-o-Iodohippurate

Malgorzata Lipowska, Jeffrey Klenc, Luigi G. Marzilli and Andrew T. Taylor
Journal of Nuclear Medicine August 2012, 53 (8) 1277-1283; DOI: https://doi.org/10.2967/jnumed.111.102236
Malgorzata Lipowska
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Jeffrey Klenc
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Luigi G. Marzilli
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Andrew T. Taylor
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  • FIGURE 1.
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    FIGURE 1.

    Structure of NTA and ASMA ligands. Ellipse encloses dangling carboxyl group, and asterisk indicates asymmetric carbon.

  • FIGURE 2.
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    FIGURE 2.

    Preparation of 2 diastereomers of 99mTc(CO)3(l-ASMA).

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    FIGURE 3.

    HPLC of 99mTc(CO)3(l-ASMA): labeling mixture (A), before injection (B), in urine at 15 min after injection (C), and ultraviolet trace (254 nm) of Re(CO)3(l-ASMA) (D). AU = absorbance units.

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    FIGURE 4.

    Biodistribution of 99mTc(CO)3(rac-ASMA) and 131I-OIH in normal rats at 10 min (A) and 60 min (B) after injection and in rats with renal pedicle ligation at 60 min after injection (C), expressed as %ID per organ, blood, and urine.

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    TABLE 1

    Biodistribution (%ID) of 99mTc(CO)3(ASMA) and 131I-OIH in Normal (Group A) and Renal Pedicle–Ligated (Group B) Rats

    ParameterBloodLiverStomachIntestineKidneyUrine% urinary 99mTc/131I
    10 min, group A
     99mTc-rac-ASMA*5.2 ± 1.72.5 ± 0.30.2 ± 0.00.5 ± 0.16.7 ± 1.051.3 ± 6.2106 ± 6
     131I-OIH6.7 ± 1.93.7 ± 0.60.3 ± 0.11.7 ± 0.36.5 ± 0.748.3 ± 4.9
     P0.07110.01780.00410.1104
     99mTc-l-ASMA†4.7 ± 0.93.7 ± 1.20.2 ± 0.00.8 ± 0.24.3 ± 2.251.1 ± 7.3100 ± 3
     131I-OIH5.1 ± 1.02.9 ± 0.30.3 ± 0.11.5 ± 0.34.0 ± 1.850.9 ± 6.0
     P0.07040.45760.07920.9003
    60 min, group A
    99mTc-rac-ASMA‡0.2 ± 0.00.2 ± 0.10.0 ± 0.00.4 ± 0.10.2 ± 0.194.4 ± 1.0106 ± 0
     131I-OIH0.7 ± 0.10.7 ± 0.10.2 ± 0.01.3 ± 0.30.3 ± 0.189.1 ± 0.9
     P0.00020.00500.04130.0008
     99mTc-l-ASMA*0.3 ± 0.10.3 ± 0.00.0 ± 0.00.5 ± 0.20.7 ± 0.395.1 ± 4.1107 ± 2
     131I-OIH0.8 ± 0.10.6 ± 0.20.1 ± 0.11.3 ± 0.30.7 ± 0.388.8 ± 2.7
     P0.00340.00610.00010.0007
    60 min, group B
    99mTc-rac-ASMA*17.9 ± 1.16.2 ± 0.60.7 ± 0.24.4 ± 0.60.6 ± 0.2——
     131I-OIH16.7 ± 1.37.9 ± 0.50.5 ± 0.28.9 ± 2.20.5 ± 0.2—
     P0.01750.03230.0189
    • ↵* Four rats.

    • ↵† Two rats.

    • ↵‡ Three rats.

    • Data are presented as mean ± SD.

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Journal of Nuclear Medicine: 53 (8)
Journal of Nuclear Medicine
Vol. 53, Issue 8
August 1, 2012
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Preclinical Evaluation of 99mTc(CO)3-Aspartic-N-Monoacetic Acid, a Renal Radiotracer with Pharmacokinetic Properties Comparable to 131I-o-Iodohippurate
Malgorzata Lipowska, Jeffrey Klenc, Luigi G. Marzilli, Andrew T. Taylor
Journal of Nuclear Medicine Aug 2012, 53 (8) 1277-1283; DOI: 10.2967/jnumed.111.102236

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Preclinical Evaluation of 99mTc(CO)3-Aspartic-N-Monoacetic Acid, a Renal Radiotracer with Pharmacokinetic Properties Comparable to 131I-o-Iodohippurate
Malgorzata Lipowska, Jeffrey Klenc, Luigi G. Marzilli, Andrew T. Taylor
Journal of Nuclear Medicine Aug 2012, 53 (8) 1277-1283; DOI: 10.2967/jnumed.111.102236
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