Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters

Subroto Ghose, Masahiro Fujita, Paul Morrison, George Uhl, Dennis L. Murphy, P. David Mozley, Magnus Schou, Christer Halldin, Robert Innis

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

The aim of this study was to determine the selectivity of (S,S)-2-(α-(2-methoxyphenoxy)benzyl)morpholine (MeNER) binding to norepinephrine transporters (NET). Quantitative autoradiography studies of NET binding were performed in brains of wildtype mice and those of mutant mice lacking one or two alleles of the NET gene. [3H]MeNER binding in the wildtype mouse brains was consistent with previously reported distributions of NET. Highest levels were found in the locus coeruleus, thalamus, hypothalamus, and bed nucleus of stria terminalis. Specific binding in these regions was ∼50% in the heterozygous NET mice and negligible in the NET knockout mice. Binding in the wildtype mouse brains was displaced by the NET ligand, nisoxetine, but not by the serotonin or dopamine transporter blockers, citalopram or GBR 12935. [3H]MeNER displayed much higher affinity for NET than for SERT or DAT in homogenate binding studies. Each of these features supports the binding specificity of this candidate in vivo NET ligand.

Original languageEnglish (US)
Pages (from-to)100-104
Number of pages5
JournalSynapse
Volume56
Issue number2
DOIs
StatePublished - May 2005

Fingerprint

Norepinephrine Plasma Membrane Transport Proteins
nisoxetine
Brain
Ligands
In Vitro Techniques
Septal Nuclei
Serotonin Plasma Membrane Transport Proteins
Citalopram
Dopamine Plasma Membrane Transport Proteins
Locus Coeruleus
Dopamine Antagonists
Autoradiography
Thalamus
Knockout Mice
Hypothalamus
Alleles

Keywords

  • Autoradiography
  • Binding assay
  • Knockout mice
  • NET

ASJC Scopus subject areas

  • Neuroscience(all)
  • Physiology
  • Pharmacology

Cite this

Ghose, S., Fujita, M., Morrison, P., Uhl, G., Murphy, D. L., Mozley, P. D., ... Innis, R. (2005). Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters. Synapse, 56(2), 100-104. https://doi.org/10.1002/syn.20133

Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters. / Ghose, Subroto; Fujita, Masahiro; Morrison, Paul; Uhl, George; Murphy, Dennis L.; Mozley, P. David; Schou, Magnus; Halldin, Christer; Innis, Robert.

In: Synapse, Vol. 56, No. 2, 05.2005, p. 100-104.

Research output: Contribution to journalArticle

Ghose, S, Fujita, M, Morrison, P, Uhl, G, Murphy, DL, Mozley, PD, Schou, M, Halldin, C & Innis, R 2005, 'Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters', Synapse, vol. 56, no. 2, pp. 100-104. https://doi.org/10.1002/syn.20133
Ghose S, Fujita M, Morrison P, Uhl G, Murphy DL, Mozley PD et al. Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters. Synapse. 2005 May;56(2):100-104. https://doi.org/10.1002/syn.20133
Ghose, Subroto ; Fujita, Masahiro ; Morrison, Paul ; Uhl, George ; Murphy, Dennis L. ; Mozley, P. David ; Schou, Magnus ; Halldin, Christer ; Innis, Robert. / Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters. In: Synapse. 2005 ; Vol. 56, No. 2. pp. 100-104.
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