Effect of structure on tumor specificity of alicyclic alpha-amino acids.
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 alpha-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 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.
D000596:Amino Acids / Q000378:metabolism*; D000598:Amino Acids, Cyclic; D000818:Animals; D006528:Carcinoma, Hepatocellular / Q000378:metabolism; D003503:Cyclobutanes / Q000378:metabolism; D003509:Cyclohexanecarboxylic Acids / Q000378:metabolism; D003515:Cycloleucine / Q000031:analogs & derivatives / Q000378:metabolism*; D003521:Cyclopropanes / Q000378:metabolism; D008113:Liver Neoplasms / Q000378:metabolism; D008297:Male; D009369:Neoplasms / Q000000981:diagnostic imaging*; D009374:Neoplasms, Experimental / Q000378:metabolism*; D011877:Radionuclide Imaging; D051381:Rats; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D014057:Tomography, X-Ray Computed
D000596:Amino Acids; D000598:Amino Acids, Cyclic; D003503:Cyclobutanes; D003509:Cyclohexanecarboxylic Acids; D003521:Cyclopropanes; D003515:Cycloleucine; C016987:1-aminocyclobutanecarboxylic acid; C014966:1-aminocyclohexanecarboxylic acid; C016995:1-amino-2-methylcyclopentanecarboxylic acid