Pyrroxamide, a nonionic nitroxyl spin label contrast agent for magnetic resonance imaging. Mutagenesis and cell survival.
Pyrroxamide, a nonionic nitroxyl spin label contrast agent for magnetic resonance imaging. Mutagenesis and cell survival.
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Pyrroxamide，一种用于磁共振成像的非离子硝酰基自旋标记造影剂。
DOI：
10.1097/00004424-198808000-00013
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发表时间：
1988
影响因子：
6.7
通讯作者：
Deen,D
中科院分区：
文献类型：
--
作者：
Gordon,DG;Brasch,RC;Ogan,MD;Deen,D
Pyrroxamide [N-(1-羟甲基-2, 3, 二羟丙基)-2, 2, 5, 5-四甲基吡咯烷-1-氧基-3-甲酰胺] 是一种新测试的非离子单体硝酰基化合物，在低至 10-3 M 的剂量下已证明可有效增强 MRI 对比度。使用电池在 10-9 至 10-2 M 的浓度下测试了 Pyrroxamide 及其羟胺代谢衍生物使用哺乳动物中国仓鼠卵巢细胞进行细胞毒性和诱变测定。在存在和不存在肝微粒体代谢激活混合物（S-9 mix）的情况下，检查了次黄嘌呤鸟嘌呤磷酸核糖转移酶（HGPRT）和Na+/K+ ATP酶基因座的基因座特异性突变诱导。还研究了细胞存活和姐妹染色单体交换的诱导。所有测试均得出阴性结果，表明吡咯酰胺和羟胺衍生物在测试剂量下均无细胞毒性和无致突变性。
Pyrroxamide [N-(1-hydroxymethyl-2, 3, dihydroxypropyl)-2, 2, 5, 5-tetramethyl pyrrolidine-l-oxyl-3-carboxyamide] is a newly tested nonionic monomeric nitroxyl compound with demonstrated effectiveness for MRI contrast enhancement at doses as low as 10-3 M. Pyrroxamide and its hydroxylamine metabolic derivative were tested in concentrations from 10-9 to 10-2 M with a battery of cytotoxic and mutagenic assays using mammalian Chinese hamster ovary cells. Loci-specific mutation induction was examined at the hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and the Na+/K+ ATPase loci, both in the presence and absence of a liver microsomal metabolic activating mixture (S-9 mix). Cell survival and induction of sister chromatid exchanges also were studied. All tests yielded negative results indicating that pyrroxamide and and hydroxylamine derivative were both noncytotoxic and nonmutagenic at the doses tested.