title: Comparison of the binding of the irreversible monoamine oxidase tracers, [(11)C]clorgyline and [(11)C]l-deprenyl in brain and peripheral organs in humans.
abstract: The monoamine oxidase A and B (MAO A and B) radiotracers [(11)C]clorgyline (CLG) and [(11)C]L-deprenyl (DEP) and their deuterium labeled counterparts (CLG-D and DEP-D) were compared to determine whether their distribution and kinetics in humans are consistent with their physical, chemical and pharmacological properties and the reported ratios of MAO A:MAO B in post-mortem human tissues. Irreversible binding was consistently higher for DEP in brain, heart, kidneys and spleen but not lung where CLG >DEP and not in thyroid where there is no DEP binding. The generally higher DEP binding is consistent with its higher enzyme affinity and larger free fraction in plasma while differences in regional distribution for CLG and DEP in brain, heart, thyroid and lungs are consistent with different relative ratios of MAO A and B in humans.
authors.affiliation: Brookhaven National Laboratory, Chemistry Department, Bldg 555, Upton, NY 11973, USA. fowler@bnl.gov
authors.forename: Joanna S
authors.initials: JS
authors.lastname: Fowler
authors.forename: Jean
authors.initials: J
authors.lastname: Logan
authors.forename: Gene-Jack
authors.initials: GJ
authors.lastname: Wang
authors.forename: Nora D
authors.initials: ND
authors.lastname: Volkow
authors.forename: Frank
authors.initials: F
authors.lastname: Telang
authors.forename: Yu-Shin
authors.initials: YS
authors.lastname: Ding
authors.forename: Colleen
authors.initials: C
authors.lastname: Shea
authors.forename: Victor
authors.initials: V
authors.lastname: Garza
authors.forename: Youwen
authors.initials: Y
authors.lastname: Xu
authors.forename: Zizhong
authors.initials: Z
authors.lastname: Li
authors.forename: David
authors.initials: D
authors.lastname: Alexoff
authors.forename: Paul
authors.initials: P
authors.lastname: Vaska
authors.forename: Richard
authors.initials: R
authors.lastname: Ferrieri
authors.forename: David
authors.initials: D
authors.lastname: Schlyer
authors.forename: Wei
authors.initials: W
authors.lastname: Zhu
authors.forename: S
authors.initials: S
authors.lastname: John Gatley
mesh_terms: D000328:Adult; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics; D003010:Clorgyline / Q000493:pharmacokinetics*; D003903:Deuterium / Q000493:pharmacokinetics; D004789:Enzyme Activation; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000493:pharmacokinetics; D009928:Organ Specificity; D011485:Protein Binding; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D012642:Selegiline / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D002250:Carbon Radioisotopes; D008996:Monoamine Oxidase Inhibitors; D019275:Radiopharmaceuticals; D012642:Selegiline; D003903:Deuterium; D008995:Monoamine Oxidase; D003010:Clorgyline