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用于急性受损心肌的放射性药物。II:[203汞]羟基汞荧光素的合成与评价。

Radiopharmaceuticals for acutely damaged myocardium. II: Synthesis and evaluation of [203Hg] hydroxymercurifluoresceins.

作者信息

Hanson R N, Davis M A, Holman B L

出版信息

J Nucl Med. 1977 Aug;18(8):803-8.

PMID:874169
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 tissues.

摘要

通过两种方法制备了六种[203Hg]羟基汞荧光素,并在大鼠心肌坏死模型中与[3H]荧光素、[131I]孟加拉玫瑰红和[203Hg]硝酸汞进行比较,以确定它们对受损心肌(DM)的特异性。非卤代[203Hg]羟基汞荧光素在该系列中DM/正常心脏的比值最高(51.5±13.5),DM/血液的比值也最高(22.1±8.1)。荧光素部分2'或4'位的卤代取代基降低了组织选择性,双羟基汞化没有显著影响。所研究的六种示踪剂比[3H]荧光素、[131I]孟加拉玫瑰红或[203Hg]硝酸汞具有更高的绝对摄取量和更好的靶标与非靶标比值,表明在受损组织的整体螯合过程中,荧光素和羟基汞部分之间存在协同作用。

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J Nucl Med. 1977 Aug;18(8):803-8.
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