188re(v)-dmsa revisited preparation and biodistribution of a potential radiotherapeutic agent with low kidney uptake

E. Dadachova, J. Chapman

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

Methods of preparation and biodistribution in mice of tin-free 99Tcm(V)-DMSA and 188Re(V)-DMSA, a potential matching pair of radiopharmaceuticals for diagnosis and therapy of certain cancers, are described. Preparation of tin-free 188Re(V)-DMSA (I) is based on reduction with either SO2-releasing compounds like Na2S2O4 (30 mg Na2S2O4, 10 mg DMSA, 1 mg L-ascorbic acid, 37°C, 60 min incubation), Na2S2O5 (as before, 70°C, 15 min incubation), or HBr (0.2 ml 48% HBr, 0.2 ml 7 M HCl, 10 mg DMSA, 1 mg L-ascorbic acid, 70°C, 60 min incubation). I exhibits significantly lower kidney uptake than tin-containing 188Re(V)-DMSA (II) (2–3% and 49% injected dose per gram organ, 1 h post-injection, respectively). HPLC profiles of I and II are similar. DMSA excess in tin-free 188Re(V)-DMSA is not responsible for the low kidney uptake of I. High kidney uptake of II is explained by formation of a mixed 188Re(V)-Sn-DMSA complex in vivo. Age-linked bone uptake in mice dependent on the maturation of the bone is demonstrated for both I and II.

Original languageEnglish (US)
Pages (from-to)173-182
Number of pages10
JournalNuclear Medicine Communications
Volume19
Issue number2
DOIs
StatePublished - Feb 1998
Externally publishedYes

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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