Labeled Choline and Phosphorylcholine: Body Distribution and Brain Autoradiography: Concise Communication

Following intravenous injection of labeled choline or phosphorylcholine in rats and mice, the brain uptake as percent injected dose was less than 0.2% with 6-12% going to kidney and 3-6% to liver. A study of [14C]choline autoradiography in a stump-tailed macaque demonstrated a five- to sixfold greater uptake in gray matter than in white matter. Dynamic positron imaging of [11C]choline in a rhesus monkey demonstrated rapid brain uptake followed by rapid washout, with heavy late uptake in muscle. The use of labeled choline and choline analogs as imaging agents in human studies is constrained by the low brain uptake relative to extracerebral tissues.