ARTICLE AUTHOR: Lambert-DM; Gallez-B

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

SOURCE: JOURNAL-OF-LABELLED-COMPOUNDS-AND-RADIOPHARMACEUTICALS. OCT 1996; 38 (10) : 897-905

ABSTRACT:

Tritiated N,N'-dibenzoyl-1,3-diaminopropan-2-ol, a compound mimicking a diacylglycerol moiety used as a lipid drug carrier was prepared from N,N'-dibenzoyl-1,3-diaminopropan-2-ol 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.