Advanced Search

Journal Navigation

Journal Home

Subscriptions

Archive

Contact Us

Table of Contents

Click here for more information

Sign In to gain access to subscriptions and/or personal tools.
Journal of Biomolecular Screening
This Article
Right arrow Full Text (PDF)
Right arrow All Versions of this Article:
1087057107299524v1
12/3/378    most recent
Right arrow References
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Right arrow Citation Map
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in Web of Science
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to Saved Citations
Right arrow Download to citation manager
Right arrowRequest Permissions
Right arrow Request Reprints
Right arrow Add to My Marked Citations
Citing Articles
Right arrow Citing Articles via Web of Science (1)
Right arrow Citing Articles via Google Scholar
Right arrow Citing Articles via Scopus
Google Scholar
Right arrow Articles by Haunsø, A.
Right arrow Articles by Buchanan, D.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Haunsø, A.
Right arrow Articles by Buchanan, D.
Right arrowPubmed/NCBI databases
*Compound via MeSH
*Substance via MeSH
Hazardous Substances DB
*TRITIUM
Social Bookmarking
Add to CiteULike   Add to Complore   Add to Connotea   Add to Del.icio.us   Add to Digg   Add to Reddit   Add to Technorati   Add to Twitter  
What's this?

Pharmacological Characterization of a Fluorescent Uptake Assay for the Noradrenaline Transporter

Anders Haunsø

Department of Molecular Pharmacology, Organon Laboratories Ltd., Newhouse, Lanarkshire, Scotland, UK, Department of Molecular Pharmacology Organon Laboratories Ltd. Newhouse, Lanarkshire ML1 5SH Scotland, UK

Dawn Buchanan

Department of Molecular Pharmacology, Organon Laboratories Ltd., Newhouse, Lanarkshire, Scotland, UK, Department of Molecular Pharmacology Organon Laboratories Ltd. Newhouse, Lanarkshire ML1 5SH Scotland, UK

The noradrenaline transporter (NET) is a Na+/Cl— dependent monoamine transporter that mediates rapid clearance of noradrenaline from the synaptic cleft, thereby terminating neuronal signaling. NET is an important target for drug development and is known to be modulated by many psychoactive compounds, including psychostimulants and antidepressants. Here, the authors describe the development and pharmacological characterization of a nonhomogeneous fluorescent NET uptake assay using the compound 4-(4-dimethylaminostyryl)-N-methylpyridinium (ASP+). Data presented show that the pharmacology of both the classic radiolabeled 3H-noradrenaline- and ASP+-based uptake assays are comparable, with an excellent correlation between potency obtained for known modulators of NET (r = 0.95, p < 0.0001). Furthermore, the fluorescent uptake assay is highly reproducible and has sufficiently large Z' values to be amenable for high-throughput screening (HTS). The advantage of this assay is compatibility with both 96- and 384-well formats and lack of radioactivity usage. Thus, the authors conclude that the assay is an inexpensive, viable approach for the identification and pharmacological profiling of small-molecule modulators of the monoamine transporter NET and may be amenable for HTS. (Journal of Biomolecular Screening 2007:378-384)

Key Words: biogenic • monoamine • noradrenaline • norepinephrine • transporter

This version was published on April 1, 2007

Journal of Biomolecular Screening, Vol. 12, No. 3, 378-384 (2007)
DOI: 10.1177/1087057107299524
Add to CiteULike CiteULike   Add to Complore Complore   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us   Add to Digg Digg   Add to Reddit Reddit   Add to Technorati Technorati   Add to Twitter Twitter    What's this?