title: Synthesis and biological evaluation of trans-3-phenyl-1-indanamines as potential norepinephrine transporter imaging agents.
abstract: The development of radioligands suitable for studying the central nervous system (CNS) norepinephrine transporter (NET) in vivo will provide important new tools for examining the pathophysiology and pharmacotherapy of a variety of neuropsychiatric disorders including major depression. Towards this end, a series of trans-3-phenyl-1-indanamine derivatives were prepared and evaluated in vitro. The biological properties of the most promising compound, [(11)C]3-BrPA, were investigated in rat biodistribution and nonhuman primate PET studies. Despite high in vitro affinity for the human NET, the uptake of [(11)C]3-BrPA in the brain and the heart was not displaceable with pharmacological doses of NET antagonists.
authors: Department of Psychiatry and Behavioral Sciences, Emory University, Atlanta, GA 30322, USA.
authors: Jonathan
authors: J
authors: McConathy
authors: Michael J
authors: MJ
authors: Owens
authors: Clinton D
authors: CD
authors: Kilts
authors: Eugene J
authors: EJ
authors: Malveaux
authors: John R
authors: JR
authors: Votaw
authors: Charles B
authors: CB
authors: Nemeroff
authors: Mark M
authors: MM
authors: Goodman
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism; D006801:Humans; D007189:Indans / Q000138:chemical synthesis*; D008024:Ligands; D008253:Macaca mulatta; D008297:Male; D008657:Metabolic Clearance Rate; D009638:Norepinephrine / Q000378:metabolism; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012701:Serotonin / Q000378:metabolism; D050486:Serotonin Plasma Membrane Transport Proteins / Q000378:metabolism*; D013045:Species Specificity; D014055:Tomography, Emission-Computed / Q000379:methods
chemical_list: D007189:Indans; D008024:Ligands; D019275:Radiopharmaceuticals; C493230:SLC6A4 protein, human; D050486:Serotonin Plasma Membrane Transport Proteins; D012701:Serotonin; D004298:Dopamine; D009638:Norepinephrine