1-氨基环丁烷[11C]羧酸，一种潜在的肿瘤靶向剂。
1-aminocyclobutane[11C]carboxylic acid, a potential tumor-seeking agent.
作者信息
Washburn L C, Sun T T, Byrd B, Hayes R L, Butler T A
出版信息
J Nucl Med. 1979 Oct;20(10):1055-61.
1-Aminocyclobutane[14C]carboxylic acid [C-14) ACBC] was incorporated preferentially by several tumor types in rats and hamsters. The agent was cleared rapidly from rat blood, attaining its maximum tissue concentrations within 30 min after i.v. injection. Carrier ACBC had little effect on the tissue distribution of (C-14) ACBC. This agent showed no affinity for a Staphylococcus aureus abscess in rats. The total excretion was low, 3.6% in 2 hr. (C-11) ACBC was synthesized in amounts up to 415 mCi (55% chemical yield) using our modified Bücherer-Strecker technique. Forty minutes were required for the two-step synthesis and chromatographic purification. ACBC was found to be nontoxic in three animal species. The radiation dose from (C-11) ACBC should be minimal. (C-11) ACBC thus appears to have good potential as a tumor-seeking agent, particularly when used with a positron emission computed tomograph.
1-氨基环丁烷[14C]羧酸[C-14]ACBC在大鼠和仓鼠的几种肿瘤类型中优先被摄取。该药物从大鼠血液中迅速清除，静脉注射后30分钟内达到其最大组织浓度。载体ACBC对[C-14]ACBC的组织分布影响很小。该药物对大鼠的金黄色葡萄球菌脓肿无亲和力。总排泄量较低，2小时内为3.6%。使用我们改良的布赫勒-施特雷克尔技术合成了高达415毫居里（化学产率55%）的[C-11]ACBC。两步合成和色谱纯化需要40分钟。发现ACBC对三种动物无毒。[C-11]ACBC的辐射剂量应最小。因此，[C-11]ACBC作为一种肿瘤寻踪剂似乎具有良好的潜力，特别是与正电子发射计算机断层扫描仪一起使用时。
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