Comparison of Three 18F‐Labeled Butyrophenone Neuroleptic Drugs in the Baboon Using Positron Emission Tomography

• DOI: 10.1111/j.1471-4159.1985.tb12891.x
• Publication Date: 2006-12-13T12:10:35Z
• Authors: Carroll D. Arnett; Chyng‐Yann Shiue; Alfred P. Wolf; Joanna S. Fowler; Jean Logan; Masazumi Watanabe
• Keywords: Spiperone; Butyrophenone; Desmethyl

Abstract: The butyrophenone neuroleptics spiroperidol, benperidol, and haloperidol were radiolabeled with fluorine‐18 studied in baboon brain using positron emission transaxial tomography (PETT). Pretreatment of the a high pharmacological dose (+)‐butaclamol reduced specifically bound component radioactivity distribution striatum to approximately found cerebellum. Comparative studies kinetics over 4‐h period indicated that either [ 18 F]spiroperidol or F]benperidol may be suitable for specific labeling neuroleptic receptors. In an 8‐h study F]spiroperidol, striatal did not decline, suggesting spiroperidol has very slow dissociation rate it binds irreversibly these receptors vivo. F]Haloperidol vivo PETT studies, because relatively nonspecific faster from receptor. Analysis F plasma after injection rapid metabolism polar acidic metabolites, only 40% total being present as unchanged drug 30 min. metabolic stability radioactively labeled compound rat greater than 95% remains 4 h.