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Synthesis and body distribution of several iodine-313 labeled centrally acting drugs. [1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane; 4-iodo-2,5-dimethoxyphenylethylamine; rats, dogs]

Journal Article · · J. Med. Chem.; (United States)
DOI:https://doi.org/10.1021/jm00222a001· OSTI ID:6550068
1-(4-Iodo-2,5-dimethoxyphenyl)-2-aminopropane (3b), 4-iodo-2,5-dimethoxyphenylethylamine (3a), and 1-(4-iodo-2,5-dimethoxyphenyl)-2-aminobutane (3c) have been synthesized with /sup 131/I. Labeled iodine monochloride reacts with the appropriately substituted phthalimide at the aromatic 4 position, and the phthalic acid group is removed with hydrazine. Body distribution was measured in rats; the most prominent different between the three compounds was a much greater concentration in the lung with 3b than with 3a or 3c. ..gamma..-Ray scintigraphs of 3a-c in rats and of 3b in a dog indicate an uptake by the brain similar to that of the bromine analogue of 3b (DOB) in humans. (/sup 82/Br)-DOB has been suggested as a potential brain scanning agent for nuclear medicine; 3b would have the advantage over DOB of providing the superior ..gamma..-ray imaging properties of /sup 131/I or /sup 123/I.
Research Organization:
Univ. of California, Berkeley
OSTI ID:
6550068
Journal Information:
J. Med. Chem.; (United States), Journal Name: J. Med. Chem.; (United States) Vol. 20:12; ISSN JMCMA
Country of Publication:
United States
Language:
English