Synthesis and biological evaluation of [11C]talopram and [ 11C]talsupram

Candidate PET ligands for the norepinephrine transporter

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

Research output: Contribution to journalArticle

35 Citations (Scopus)

Abstract

PET and SPECT ligands for the norepinephrine transporter (NET) will be important tools for studying the physiology, pathophysiology and pharmacology of the CNS noradrenergic system in vivo. A series of candidate NET ligands were synthesized and characterized in terms of their affinity for human monoamine transporters. The two most promising compounds, talopram and talsupram, were radiolabeled with carbon-11 and evaluated through biodistribution studies in rats and PET imaging studies in a rhesus monkey. Although both compounds displayed high affinity and selectivity for the human NET in vitro, these compounds did not enter the CNS in adequate amounts to be used in PET imaging studies.

Original languageEnglish
Pages (from-to)705-718
Number of pages14
JournalNuclear Medicine and Biology
Volume31
Issue number6
DOIs
StatePublished - Aug 1 2004
Externally publishedYes

Fingerprint

Norepinephrine Plasma Membrane Transport Proteins
Ligands
Single-Photon Emission-Computed Tomography
Macaca mulatta
Carbon
Pharmacology
talopram
talsupram

Keywords

  • Carbon-11
  • Monoamine transporter ligands
  • Norepinephrine transporter
  • Positron emission tomography
  • Talopram
  • Talsupram

ASJC Scopus subject areas

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

Cite this

Synthesis and biological evaluation of [11C]talopram and [ 11C]talsupram : Candidate PET ligands for the norepinephrine transporter. / McConathy, Jonathan; Owens, Michael J.; Kilts, Clinton D.; Malveaux, Eugene J.; Camp, Vernon M.; Votaw, John R.; Nemeroff, Charles; Goodman, Mark M.

In: Nuclear Medicine and Biology, Vol. 31, No. 6, 01.08.2004, p. 705-718.

Research output: Contribution to journalArticle

McConathy, Jonathan ; Owens, Michael J. ; Kilts, Clinton D. ; Malveaux, Eugene J. ; Camp, Vernon M. ; Votaw, John R. ; Nemeroff, Charles ; Goodman, Mark M. / Synthesis and biological evaluation of [11C]talopram and [ 11C]talsupram : Candidate PET ligands for the norepinephrine transporter. In: Nuclear Medicine and Biology. 2004 ; Vol. 31, No. 6. pp. 705-718.
@article{e258881aa16845dc9f1f293a172f3921,
title = "Synthesis and biological evaluation of [11C]talopram and [ 11C]talsupram: Candidate PET ligands for the norepinephrine transporter",
abstract = "PET and SPECT ligands for the norepinephrine transporter (NET) will be important tools for studying the physiology, pathophysiology and pharmacology of the CNS noradrenergic system in vivo. A series of candidate NET ligands were synthesized and characterized in terms of their affinity for human monoamine transporters. The two most promising compounds, talopram and talsupram, were radiolabeled with carbon-11 and evaluated through biodistribution studies in rats and PET imaging studies in a rhesus monkey. Although both compounds displayed high affinity and selectivity for the human NET in vitro, these compounds did not enter the CNS in adequate amounts to be used in PET imaging studies.",
keywords = "Carbon-11, Monoamine transporter ligands, Norepinephrine transporter, Positron emission tomography, Talopram, Talsupram",
author = "Jonathan McConathy and Owens, {Michael J.} and Kilts, {Clinton D.} and Malveaux, {Eugene J.} and Camp, {Vernon M.} and Votaw, {John R.} and Charles Nemeroff and Goodman, {Mark M.}",
year = "2004",
month = "8",
day = "1",
doi = "10.1016/j.nucmedbio.2003.05.001",
language = "English",
volume = "31",
pages = "705--718",
journal = "Nuclear Medicine and Biology",
issn = "0969-8051",
publisher = "Elsevier Inc.",
number = "6",

}

TY - JOUR

T1 - Synthesis and biological evaluation of [11C]talopram and [ 11C]talsupram

T2 - Candidate PET ligands for the norepinephrine transporter

AU - McConathy, Jonathan

AU - Owens, Michael J.

AU - Kilts, Clinton D.

AU - Malveaux, Eugene J.

AU - Camp, Vernon M.

AU - Votaw, John R.

AU - Nemeroff, Charles

AU - Goodman, Mark M.

PY - 2004/8/1

Y1 - 2004/8/1

N2 - PET and SPECT ligands for the norepinephrine transporter (NET) will be important tools for studying the physiology, pathophysiology and pharmacology of the CNS noradrenergic system in vivo. A series of candidate NET ligands were synthesized and characterized in terms of their affinity for human monoamine transporters. The two most promising compounds, talopram and talsupram, were radiolabeled with carbon-11 and evaluated through biodistribution studies in rats and PET imaging studies in a rhesus monkey. Although both compounds displayed high affinity and selectivity for the human NET in vitro, these compounds did not enter the CNS in adequate amounts to be used in PET imaging studies.

AB - PET and SPECT ligands for the norepinephrine transporter (NET) will be important tools for studying the physiology, pathophysiology and pharmacology of the CNS noradrenergic system in vivo. A series of candidate NET ligands were synthesized and characterized in terms of their affinity for human monoamine transporters. The two most promising compounds, talopram and talsupram, were radiolabeled with carbon-11 and evaluated through biodistribution studies in rats and PET imaging studies in a rhesus monkey. Although both compounds displayed high affinity and selectivity for the human NET in vitro, these compounds did not enter the CNS in adequate amounts to be used in PET imaging studies.

KW - Carbon-11

KW - Monoamine transporter ligands

KW - Norepinephrine transporter

KW - Positron emission tomography

KW - Talopram

KW - Talsupram

UR - http://www.scopus.com/inward/record.url?scp=3042789525&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=3042789525&partnerID=8YFLogxK

U2 - 10.1016/j.nucmedbio.2003.05.001

DO - 10.1016/j.nucmedbio.2003.05.001

M3 - Article

VL - 31

SP - 705

EP - 718

JO - Nuclear Medicine and Biology

JF - Nuclear Medicine and Biology

SN - 0969-8051

IS - 6

ER -