Synthesis and biological evaluation of trans-3-phenyl-1-indanamines as potential norepinephrine transporter imaging agents.

Academic Article

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.
  • Published In

    Keywords

  • Animals, Brain, Dopamine, Humans, Indans, Ligands, Macaca mulatta, Male, Metabolic Clearance Rate, Norepinephrine, Protein Binding, Radiopharmaceuticals, Rats, Rats, Sprague-Dawley, Serotonin, Serotonin Plasma Membrane Transport Proteins, Species Specificity, Tomography, Emission-Computed
  • Digital Object Identifier (doi)

    Author List

  • McConathy J; Owens MJ; Kilts CD; Malveaux EJ; Votaw JR; Nemeroff CB; Goodman MM
  • Start Page

  • 593
  • End Page

  • 605
  • Volume

  • 32
  • Issue

  • 6