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Radiopharmaceuticals for Acutely Damaged Myocardium II: Synthesis and Evaluation of [²⁰³Hg] Hydroxymercurifluoresceins

Harvard Medical School and Northeastern University, Boston, Massachusetts

Correspondence: For reprints contact: Michael A. Davis, Dept. of Radiology, Harvard Medical School, 50 Binney St., Boston, MA 02115.

ABSTRACT

Six [²⁰³Hg] hydroxymercurifluoresceins were prepared by two methods and compared with [³H] fluorescein, [¹³¹I] rose bengal, and [²⁰³Hg] mercuric nitrate, in a rat model for myocardial necrosis, to determine their specificities for damaged myocardium (DM). The nonhalogenated [²⁰³Hg] hydroxymercurifluorescein had the highest ratios of the series for DM/normal heart (51.5 ± 13.5) and DM/blood (22.1 ± 8.1). Halide substituents at the 2' or 4' positions of the fluorescein moiety decreased the tissue selectivity, and bis-hydroxymercuration had no significant effect. The six tracers studied had greater absolute uptake and better target-to-nontarget ratios than [³H] fluorescein, [¹³¹I] rose bengal, or [²⁰³Hg] mercuric nitrate, indicating a cooperative effect between the fluorescein and hydroxymercuri-moieties in the overall sequestration process in damaged tissue.