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Synthesis and Distribution of Tritiated N, N ′‐dibenzoyl‐1,3‐diaminopropan‐2‐ol
Author(s) -
Lambert Didier M.,
Gallez Bernard
Publication year - 1996
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199610)38:10<897::aid-jlcr916>3.0.co;2-d
Subject(s) - chemistry , biodistribution , tritium , diacylglycerol kinase , moiety , chemical synthesis , radiochemistry , specific activity , chloride , distribution (mathematics) , medicinal chemistry , stereochemistry , pharmacology , organic chemistry , in vitro , biochemistry , medicine , mathematical analysis , physics , mathematics , protein kinase c , nuclear physics , enzyme
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.