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Effect of Structure on Tumor Specificity of Alicyclic -Amino Acids¹

Medical and Health Sciences Division, Oak Ridge Associated Universities,⁴ Oak Ridge, Tennessee 37830

The selective affinity of [carboxyl-¹¹C]-1-aminocyclopentanecarboxylic acid (ACPC) for tumor tissue has led us to study the tumor-localizing characteristics of a series of alicyclic -amino acid analogs of ACPC. The tissue distributions of [¹⁴C]-1-aminocyclopropanecarboxylic acid, 1-aminocyclobutanecarboxylic acid (ACBC), 1-aminocyclohexanecarboxylic acid, 1-amino-2-methylcyclopentanecarboxylic acid, and 1-amino-3-methylcyclopentanecarboxylic acid were compared with that of ACPC in Buffalo rats bearing Morris 5123C hepatomas. ACPC and ACBC were found to have significantly higher tumor-to-nontumor concentration ratios than the other four amino acids. ACBC generally had higher tumor-to-nontumor ratios than did ACPC, significantly so for muscle, kidney, and testis and marginally so for blood. These results suggest that [carboxyl-¹¹C]ACBC may be a better agent than [carboxyl-¹¹C]ACPC for tumor imaging by positron tomography.

¹ This article is based on work supported by NIH Grant CA-14669.

² To whom requests for reprints should be addressed.

³ Student Research Participant.

⁴ Oak Ridge Associated Universities operates under Contract EY-76-C-050033 with the U. S. Department of Energy.

Received 2/17/78. Accepted 5/ 3/78.

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