title: PET radioligands for the vesicular transporters for monoamines and acetylcholine.
abstract: The vesicular transporters for the monoamine and acetylcholine have been successfully targeted for the development of radioligands for human brain imaging. The vesicular monoamine transporter type 2 ligands are based on the structure of tetrabenazine, a known clinically used drug. In contrast, the radioligands for vesicular acetylcholine transporter are based on vesamicol, a toxic xenobiotic. The similarities and differences in the development of these two classes of radioligands are discussed.
authors.affiliation: Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, Ann Arbor, MI, USA.
authors.forename: Michael R
authors.initials: MR
authors.lastname: Kilbourn
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D002250:Carbon Radioisotopes / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D008024:Ligands; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D050494:Vesicular Acetylcholine Transport Proteins / Q000378:metabolism*; D050493:Vesicular Monoamine Transport Proteins / Q000378:metabolism*
chemical_list: D002250:Carbon Radioisotopes; D005462:Fluorine Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D050494:Vesicular Acetylcholine Transport Proteins; D050493:Vesicular Monoamine Transport Proteins
keywords: brain; carbon-11; fluorine-18; transporter; vesicular