ARTICLE AUTHOR: Lambert-DM; Gallez-B; Poupaert-JH

REPRINT AUTHOR: Lambert, DM; UNIV CATHOLIQUE LOUVAIN; DEPT PHARMACEUT SCI, CHIM PHARMACEUT LAB, AVE E MOUNIER 7340; B-1200 BRUSSELS; BELGIUM

SOURCE: JOURNAL-OF-LABELLED-COMPOUNDS-AND-RADIOPHARMACEUTICALS. APR 1995; 36 (4) : 397-406

ABSTRACT:

N-benzyloxycarbonyl[C-14]-glycine, a lipophilic derivative of glycine exhibiting anticonvulsant properties, was prepared in one step from [U-C-14] glycine and benzyl chloroformate in alkali medium. A comparative study of biodistribution was carried on mice between this compound and the parent amino-acid after intravenous administration. Dimethylsulfoxide was used as injection vehicle for N-benzyloxycarbonylglycine. The influence of this injection vehicle was studied comparing glycine injected in a saline solution and glycine co-administered with dimethylsulfoxide. No significant difference was found between these two treatments. Compared to glycine, N-benzyloxycarbonylglycine reached quickly the central nervous system and exhibited an enhanced brain penetration index, 13-fold superior to the parent aminoacid value.