Advanced Search

Journal Navigation

Journal Home

Subscriptions

Archive

Contact Us

Table of Contents

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:
1087057106289891v1
11/6/688    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 HighWire
Right arrow Citing Articles via Web of Science (3)
Right arrow Citing Articles via Google Scholar
Right arrow Citing Articles via Scopus
Google Scholar
Right arrow Articles by Navarro, H. A.
Right arrow Articles by Lewin, A. H.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Navarro, H. A.
Right arrow Articles by Lewin, A. H.
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?

A Rapid Functional Assay for the Human Trace Amine-Associated Receptor 1 Based on the Mobilization of Internal Calcium

Hernán A. Navarro

Center for Organic and Medicinal Chemistry, RTI International, Research Triangle Park, North Carolina

Brian P. Gilmour

Center for Organic and Medicinal Chemistry, RTI International, Research Triangle Park, North Carolina

Anita H. Lewin

Center for Organic and Medicinal Chemistry, RTI International, Research Triangle Park, North Carolina

The molecular targets for trace amines (TAs) such as p-tyramine and ß-phenylethylamine have been recently discovered and have been shown to comprise a family of G-protein-coupled receptors based on DNA sequence homologies. These have been termed trace amine-associated receptors (TAARs) because TAs do not activate all of the identified receptors. Because TA may be involved in modulating a variety of behaviors including mood, cognition, and addiction, it is of interest to discover novel ligands for TAARs to probe the role TAs play in brain function. Pharmacophore development for the Gs-coupled human TAAR1 (hTAAR1) would be aided by a rapid functional assay amenable to screening libraries of compounds. Accordingly, the authors used RD-HGA16 CHO-1 cells from Molecular Devices, which stably express the promiscuous Gq, G{alpha}16, to create a cell line stably expressing hTAAR1, thereby coupling receptor activation to the mobilization of internal calcium. They used this cell line to develop a homogenous fluorometric imaging plate reader-based assay using the Calcium 3 fluorescent dye. The EC50 and Emax data obtained for known TAs are in close agreement with previous work using transient hTAAR1 expression systems or a chimeric receptor. These data indicate that the hTAAR1 retains its reported pharmacological characteristics when coupled to G{alpha}16.

Key Words: human • trace amine • calcium mobilization • G{alpha}16

This version was published on September 1, 2006

Journal of Biomolecular Screening, Vol. 11, No. 6, 688-693 (2006)
DOI: 10.1177/1087057106289891
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?


This article has been cited by other articles:


Home page
 Mol. Pharmacol.Home page
T. D. Sotnikova, M. G. Caron, and R. R. Gainetdinov
Trace Amine-Associated Receptors as Emerging Therapeutic Targets
Mol. Pharmacol., August 1, 2009; 76(2): 229 - 235.
[Abstract] [Full Text] [PDF]

Home page
 Pharmacol. Rev.Home page
J. J. Maguire, W. A. E. Parker, S. M. Foord, T. I. Bonner, R. R. Neubig, and A. P. Davenport
International Union of Pharmacology. LXXII. Recommendations for Trace Amine Receptor Nomenclature
Pharmacol. Rev., March 1, 2009; 61(1): 1 - 8.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
Z. Xie, S. V. Westmoreland, M. E. Bahn, G.-L. Chen, H. Yang, E. J. Vallender, W.-D. Yao, B. K. Madras, and G. M. Miller
Rhesus Monkey Trace Amine-Associated Receptor 1 Signaling: Enhancement by Monoamine Transporters and Attenuation by the D2 Autoreceptor in Vitro
J. Pharmacol. Exp. Ther., April 1, 2007; 321(1): 116 - 127.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
D. B. Wainscott, S. P. Little, T. Yin, Y. Tu, V. P. Rocco, J. X. He, and D. L. Nelson
Pharmacologic Characterization of the Cloned Human Trace Amine-Associated Receptor1 (TAAR1) and Evidence for Species Differences with the Rat TAAR1
J. Pharmacol. Exp. Ther., January 1, 2007; 320(1): 475 - 485.
[Abstract] [Full Text] [PDF]