Abstract
PD-132301, an inhibitor of sterol O-acyltransferase 1 (SOAT1; also known as acyl-coenzyme A:cholesterol acyltransferase-1, ACAT1), is under clinical investigation for numerous adrenal disorders. Radiolabeled SOAT1 inhibitors could support drug discovery and help diagnose SOAT1-related disorders, such as atherosclerosis. We synthesized two radiolabeled SOAT1 inhibitors, [(11)C]PD-132301 and fluorine analogue [(18)F]1. Rat biodistribution studies were conducted with both agents and, as the most selective tracer, [(11)C]PD-132301 was advanced to preclinical positron emission tomography studies in (atherosclerotic) ApoE(-/-) mice. The uptake of [(11)C]PD-132301 in SOAT1-rich tissue warrants further investigation into the compound as an atherosclerosis and adrenal imaging agent.