Iodohippurate Sodium 131I (OIH) Clearance in Mice Bioassay of Radiopharmaceuticals

Konikowski, T.; Tp, Hayhie; Hj, Glenn; Le, Farr

doi:10.3181/00379727-137-35785

Cited by 2 publications

(1 citation statement)

References 6 publications

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“…Many of the charges come from the chelating agent, and chelator selection is a critical component of probe design 47 48 . Some chelated metals have very low non-specific interactions like indium-DTPA while others have higher plasma protein binding and overall lipophilic properties like Tc-99m-DTPA 28 49 . More hydrophilic chelators have been designed, but here again these do not completely correlate with physicochemical properties 50 , making predictions from structure alone challenging.…”

Section: Discussionmentioning

confidence: 99%

Mechanistic and quantitative insight into cell surface targeted molecular imaging agent design

Zhang

Bhatnagar

Deschenes

et al. 2016

Sci Rep

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Molecular imaging agent design involves simultaneously optimizing multiple probe properties. While several desired characteristics are straightforward, including high affinity and low non-specific background signal, in practice there are quantitative trade-offs between these properties. These include plasma clearance, where fast clearance lowers background signal but can reduce target uptake, and binding, where high affinity compounds sometimes suffer from lower stability or increased non-specific interactions. Further complicating probe development, many of the optimal parameters vary depending on both target tissue and imaging agent properties, making empirical approaches or previous experience difficult to translate. Here, we focus on low molecular weight compounds targeting extracellular receptors, which have some of the highest contrast values for imaging agents. We use a mechanistic approach to provide a quantitative framework for weighing trade-offs between molecules. Our results show that specific target uptake is well-described by quantitative simulations for a variety of targeting agents, whereas non-specific background signal is more difficult to predict. Two in vitro experimental methods for estimating background signal in vivo are compared – non-specific cellular uptake and plasma protein binding. Together, these data provide a quantitative method to guide probe design and focus animal work for more cost-effective and time-efficient development of molecular imaging agents.

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Section: Discussionmentioning

confidence: 99%

Mechanistic and quantitative insight into cell surface targeted molecular imaging agent design

Zhang

Bhatnagar

Deschenes

et al. 2016

Sci Rep

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Ru-labeled ruthenocenoyl-glycine: comparison of clearance with hippuran

1985

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Ruthenocenoyl-glycine (ruppuran) is a metallocene analog of iodo-labeled hippuran. After injection of 103Ru-labeled ruppuran and ruthenocenoyl-1,1'-diglycine in rabbits, measurement with external detectors revealed a very rapid accumulation in the kidneys followed by rapid excretion of the 103Ru activity. By measurement of the radioactivity concentration in plasma and urine samples collected 1-60 min after IV injection, the plasma clearance was calculated and compared with the clearance of 125I-labeled hippuran injected simultaneously. The clearance of ruppuran and ruthenocenoyl-diglycine in rabbits was found to be somewhat higher than that of hippuran. Extrapolating to man (1.73 m3), plasma clearance with both ruthenocene derivatives was approximately 500-600 ml/min. Biochemical data as well as the nuclear properties of 97Ru indicate the usefulness of 97Ru-labeled ruthenocenoyl-glycine as a radiopharmaceutical for kidney function studies.

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Iodohippurate Sodium 131I (OIH) Clearance in Mice Bioassay of Radiopharmaceuticals

Cited by 2 publications

References 6 publications

Mechanistic and quantitative insight into cell surface targeted molecular imaging agent design

Mechanistic and quantitative insight into cell surface targeted molecular imaging agent design

Ru-labeled ruthenocenoyl-glycine: comparison of clearance with hippuran

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