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Molecular Pharmacology Fast Forward
First published on February 28, 2007; DOI: 10.1124/mol.107.035493

0026-895X/07/7105-1206-1208$20.00
Mol Pharmacol 71:1206-1208, 2007

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Perspective

All Aglow about Presynaptic Receptor Regulation of Neurotransmitter Transporters

Randy D. Blakely, and Louis J. DeFelice

Departments of Pharmacology (R.D.B., L.J.D.) and Psychiatry (R.D.B.), and Center for Molecular Neuroscience (R.D.B., L.J.D.), Vanderbilt University School of Medicine, Nashville, Tennessee

Mounting evidence supports the idea that neurotransmitter transporters are subject to many forms of post-translational regulation typically associated with receptors and ion channels, including receptor and kinase-mediated changes in transporter phosphorylation, cell surface trafficking, and/or catalytic activation. Although hints of this regulation can be achieved with traditional radiolabeled substrate flux techniques, higher resolution methods are needed that can localize transporter function in situ as well as permit real-time monitoring of transport function without confounds associated with coincident receptor activation. The elegant study by Bolan et al. (p. 1222) capitalizes on the fluorescent properties of a recently introduced substrate for the dopamine (DA) transporter (DAT), termed 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP+), to illuminate a pertussis toxin-sensitive, extracellular signal-regulated kinase (ERK1/2)-dependent pathway by which presynaptic DA D2 receptors regulate DATs.

Received for publication February 26, 2007.

Accepted for publication February 27, 2007.

Address correspondence to: Dr. Randy D. Blakely, Allan D. Bass Professor of Pharmacology & Psychiatry, Director, Vanderbilt Center for Molecular Neuroscience, Nashville, TN 37232-8548. E-mail: randy.blakely{at}vanderbilt.edu


Related articles in MolPharm:

D2 Receptors Regulate Dopamine Transporter Function via an Extracellular Signal-Regulated Kinases 1 and 2-Dependent and Phosphoinositide 3 Kinase-Independent Mechanism
Elizabeth A. Bolan, Bronwyn Kivell, Vanaja Jaligam, Murat Oz, Lankupalle D. Jayanthi, Yang Han, Namita Sen, Eneki Urizar, Ivone Gomes, Lakshmi A. Devi, Sammanda Ramamoorthy, Jonathan A. Javitch, Agustin Zapata, and Toni S. Shippenberg
MolPharm 2007 71: 1222-1232. [Abstract] [Full Text]  





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