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Investigation of Physicochemical and In-Vivo Behavior of Diastereomeric Iron-59, Gallium-68, and Indium-111-EHPG Trivalent Metal Complexes

Edward Mallinckrodt Institute of Radiology, Washington University Medical School, St. Louis, Missouri
Department of Chemistry, Texas A&M University, College Station, Texas

Correspondence: For reprints contact: Michael J. Welch, Mallinckrodt Institute of Radiology, Washington University Medical School, Division of Radiation Science, Box 8131, 510 S. Kingshighway, St. Louis, MO 63110.

ABSTRACT

EHPG (N, N'-ethylenebis-[2-(o-hydroxyphenyl)glycine]) trivalent metal complexes show diagnostic potential both in radiopharmaceutical applications (gallium-68, indium-111) and as MRI contrast agents (iron). Although several publications report similar behavior of iron, gallium and indium complexes, we observe significant differences between EHPG complexes of these metals both in physicochemical and in vivo analyses. In addition, stereospecific behavior has been observed for the two diastereomers of EHPG when complexed with each metal. Complexes of Fe[⁵⁹Fe], ⁶⁸Ga, and ¹¹¹In with meso, racemic, and unseparated EHPG have been evaluated. Relative lipophilicity has been measured with HPLC. Blood clearance and liver uptake have been correlated with pM values, stability constants and metal ion reduction potentials.

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