An iodinated catecholamine congener for brain imaging and metabolic studies.

The iodinated O-methylated catecholamine congener, 4-iodo-2,5-dimethoxyphenylisopropylamine (4-I-DPIA), has potential as a new agent for imaging and metabolic studies of the brain and lung. The organ distribution and brain uptake of radioiodine-labeled 4-I-DPIA were studied in the dog and monkey by whole-body scanning, gamma-camera scintigraphy, and organ assay. The brain takes up 2% of the injected dose, with a half-time of 8 sec in the monkey, and the lung takes up 11.8%. An unusual finding was a concentration in the retina, five times that in any other CNS tissue. 4-I-DPIA may have potential in the imaging of normal brain tissues and thereby delineating nonfunctional areas damaged by infarction, trauma, or malignancy, and may also be useful in metabolic studies of catecholamine function. Adequate radioactivity can theoretically be administered with a quantity of 4-I-DPIA 1/10,000 of the pharmacologically active levels. The agent may also find application in lung imaging because of the high pulmonary uptake.