Abstract
AbstractN‐benzyloxycarbonyl[14C]‐glycine, a lipophilic derivative of glycine exhibiting anticonvulsant properties, was prepared in one step from [U‐14C] 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.
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