D. Lambert, B. Gallez, Jacques Poupaert
Apr 1, 1995
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Influential Citations
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
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.