Synthesis and body distribution of several iodine-131-labeled central nervous system active drugs

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Abstract
1-(4-Iodo-2,5-dimethoxyphenyl)-2-aminopropane [DOB] (3b), 4-iodo-2,5-dimethoxyphenylethylamine (3a) and 1-(4-iodo-2,5-dimethoxyphenyl)-2-aminobutane (3c) were synthesized with 131I. Labeled iodine monochloride reacts with the appropriately substituted phthalmide at the aromatic 4 position and the phthalic acid group were removed with hydrazine. Body distribution was measured in rats; the most prominent difference between the 3 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 indicated an uptake by the brain similar to that of the bromine analog of 3b (DOB) in humans. [82Br]-DOB may be a potential brain scanning agent for nuclear medicine; 3b may have the advantage over DOB of providing the superior .gamma.-ray imaging properties of 131I or 123I.