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Synthesis and Distribution of Tritiated N, N′-dibenzoyl-1,3-diaminopropan-2-ol

✍ Scribed by Didier M. Lambert; Bernard Gallez

Publisher
John Wiley and Sons
Year
1996
Tongue
French
Weight
387 KB
Volume
38
Category
Article
ISSN
0022-2135

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✦ Synopsis

Tritiated N,N'-dibenzoyl-l,3-diaminopropan-2-ol, a compound mimicking a diacylglycerol moiety used as a lipid drug carrier was prepared from N,N'-dibenzoyl-l,3-diaminopropan-2-o1 by isotopic exchange in the presence of rhodium chloride.

Preliminary preparation of the deuterated analog was made in order to assess the position of the substitution. A biodistribution study was carried out in mice after intravenous administration. Five minutes after administration, the level found in the brain was about 9 % of the injected dose per g organ. This value decreases to 1 % 3 hours after administration while in the same time radioactive levels measured in the urine increased. The results are in accordance with the pharmacological evaluation : N,N'-dibenzoyl-1,3-diaminopropan-2-ol exhibits an anticonvulsant activity at 30 minutes in the maximal electroshock seizure test, but was found inactive at 3 hours.

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