title: Synthesis and biological evaluation of 2beta,3alpha-(substituted phenyl)nortropanes as potential norepinephrine transporter imaging agents.
abstract: A series of 2beta,3alpha-(substituted phenyl)nortropanes was synthesized and evaluated in vitro for human monoamine transporters. All compounds studied in this series exhibited nanomolar potency for the norepinephrine transporter (NET). Radiolabeling and nonhuman primate microPET brain imaging studies were performed with the most promising compound, [(11)C]1, to determine its utility as a NET imaging agent. Despite high in vitro affinity for the human NET, the high uptake of [(11)C]1 in the caudate and putamen excludes its use as an in vivo PET imaging agent for the NET.
authors: Department of Radiology, Division of Radiological Sciences, Emory University, 1364 Clifton Road, Atlanta, GA 30322, USA.
authors: Fanxing
authors: F
authors: Zeng
authors: Jeffrey S
authors: JS
authors: Stehouwer
authors: Nachwa
authors: N
authors: Jarkas
authors: Ronald J
authors: RJ
authors: Voll
authors: Larry
authors: L
authors: Williams
authors: Vernon M
authors: VM
authors: Camp
authors: John R
authors: JR
authors: Votaw
authors: Michael J
authors: MJ
authors: Owens
authors: Clinton D
authors: CD
authors: Kilts
authors: Charles B
authors: CB
authors: Nemeroff
authors: Mark M
authors: MM
authors: Goodman
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging; D001923:Brain Chemistry; D002250:Carbon Radioisotopes / Q000032:analysis / Q000737:chemistry / Q000378:metabolism; D003952:Diagnostic Imaging; D006801:Humans; D008253:Macaca mulatta; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000032:analysis*; D009662:Nortropanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography
chemical_list: D002250:Carbon Radioisotopes; D050484:Norepinephrine Plasma Membrane Transport Proteins; D009662:Nortropanes