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

Jonathan McConathy, Michael J. Owens, Clinton D. Kilts, Eugene J. Malveaux, John R. Votaw, Charles Nemeroff, Mark M. Goodman

Research output: Contribution to journalArticle

5 Citations (Scopus)

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, [ 11C]3-BrPA, were investigated in rat biodistribution and nonhuman primate PET studies. Despite high in vitro affinity for the human NET, the uptake of [11C]3-BrPA in the brain and the heart was not displaceable with pharmacological doses of NET antagonists.

Original languageEnglish
Pages (from-to)593-605
Number of pages13
JournalNuclear Medicine and Biology
Volume32
Issue number6
DOIs
StatePublished - Aug 1 2005
Externally publishedYes

Fingerprint

Norepinephrine Plasma Membrane Transport Proteins
Primates
Central Nervous System
Pharmacology
Drug Therapy
Brain
In Vitro Techniques

Keywords

  • Carbon-11
  • Monoamine transporter ligands
  • Norepinephrine transporter
  • Phenylindanamine
  • Positron emission tomography

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging

Cite this

Synthesis and biological evaluation of trans-3-phenyl-1-indanamines as potential norepinephrine transporter imaging agents. / McConathy, Jonathan; Owens, Michael J.; Kilts, Clinton D.; Malveaux, Eugene J.; Votaw, John R.; Nemeroff, Charles; Goodman, Mark M.

In: Nuclear Medicine and Biology, Vol. 32, No. 6, 01.08.2005, p. 593-605.

Research output: Contribution to journalArticle

McConathy, Jonathan ; Owens, Michael J. ; Kilts, Clinton D. ; Malveaux, Eugene J. ; Votaw, John R. ; Nemeroff, Charles ; Goodman, Mark M. / Synthesis and biological evaluation of trans-3-phenyl-1-indanamines as potential norepinephrine transporter imaging agents. In: Nuclear Medicine and Biology. 2005 ; Vol. 32, No. 6. pp. 593-605.
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