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Synthesis and distribution of N-benzyloxycarbonyl-[14C]-glycine, a lipophilic derivative of glycine

✍ Scribed by Dr. Didier M. Lambert; Bernard Gallez; Jacques H. Poupaert


Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
392 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis


N-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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