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Preparation and biological distribution of technetium diphosphonate radiotracers synthesized without stannous ion

Journal Article · · J. Nucl. Med.; (United States)
OSTI ID:6839689

Two HEDP complexes of technetium (either Tc-99 or a mixture of Tc-99 and Tc-99m) have been prepared without the use of stannous ion. The first, Tc(NaBH/sub 4/)-HEDP, is synthesized by reduction of TcO/sub 4//sup -/ with NaBH/sub 4/ in the presence of excess HEDP; this is analogous to the preparation of Tc(Sn)-HEDP in commerical kits wherein Sn(II) functions as the reductant. The second, Tc-HEDP, is prepared by substitution of HEDP onto the pre-formed, pre-reduced, technetium center TcBr/sub 6//sup 2 -/. The HEDP-to-Tc ratio in Tc-HEDP was found to be 1.0 by double-labeling procedures (Tc-99 and (/sup 3/H)HEDP), implying that in solution this material is polymeric or at least dimeric. Preparations of Tc(NaBH/sub 4/)-HEDP and Tc-HEDP with Tc-99m are excellent bone-imaging agents in both rats and dogs. Tissue distribution studies in rats show that uptake of Tc(NaBH/sub 4/)-HEDP and Tc-HEDP by the bone is at least equivalent to that achieved by Tc(Sn)-HEDP prepared in commercial kits with Sn(II) as the reductant. Tin is therefore not necessary for the bone-seeking properties of Tc(Sn)-HEDP, and the in vivo distribution of a given HEDP radiotracer seems to depend primarily on the presence of the HEDP ligand and not on the exact nature of the technetium complex itself. Synthesis of technetium radiotracers by a substitution route, rather than by redox, is practicable; this route has the potential of introducing hitherto unattainable flexibility and subtlety into the preparation of technetium radiotracers.

Research Organization:
Procter and Gamble Co., Cincinnati, OH
OSTI ID:
6839689
Journal Information:
J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 21:9; ISSN JNMEA
Country of Publication:
United States
Language:
English

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