1-aminocyclobutane[11C]carboxylic acid, a potential tumor-seeking agent

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.