Zopiclone (ZPC) was labeled with 131I by using the halogen exchange method. Temperature and reaction time effects to labeling yields were studied. Infrared, nuclear magnetic resonance, and gas chromatography-mass spectroscopy spectra were undertaken to identify chemical structure. High performance liquid chromatography (HPLC) was performed to determine purity of cold zopiclone. Biodistribution studies were performed on rabbits and rats. 131IZPC was administered intravenously to rabbits. Static images were taken by a Sophy DX Gamma Camera. 131IZPC was also administered intraperitoneally to rats. Activities were counted in a NaI(Tl) scintillation detector for several organs (liver, brain, spleen, lung, blood, fat) after rats were decapitated on different times. Biodistribution profiles were obtained depending on the time.