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Preliminary studies of 99mTc-BnAO and its analogues: synthesis, radiolabeling and in vitro cell uptake.

Abstract：

INTRODUCTION:(99m)Tc-BnAO is one of the nonnitroimidazole hypoxia markers with the highest citation and could be potentially useful in both oncology and other clinical applications. However, it appears inferior in vitro due to lower absolute accumulation and smaller anoxic/normoxic uptake ratio. It is possible that the analogues of (99m)Tc-BnAO have higher hypoxia selectivity after the ligand of (99m)Tc-BnAO is modified. METHODS:2,2'-(1,4-Diaminobutane)bis(2-methyl-3-butanone) dioxime (BnAO or HL91) and three novel analogues were synthesized and radiolabeled with technetium-99m. The cellular uptake of the radiolabeled complexes was determined in murine sarcoma S180 cell lines under anoxic and normoxic conditions. RESULTS:(99m)Tc-BnAO and its three novel analogues continuously accumulated in anoxic cells but not in normoxic ones, while the analogues showed earlier hypoxia selectivity and greater anoxic/normoxic differential. CONCLUSIONS:The analogues are superior to (99m)Tc-BnAO in terms of in vitro hypoxia selectivity and are viable candidates for further development as new nonnitroimidazole hypoxia markers in the future.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Sun X,Chu T,Wang X

doi

10.1016/j.nucmedbio.2009.09.003

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

117-23

issue

2

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(09)00241-8

journal_volume

37

pub_type

杂志文章

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