TITLE

Characterization of voltage-gated sodium-channel blockers by electrical stimulation and fluorescence detection of membrane potential

AUTHOR(S)
Chien-Jung Huang; Harootunian, Alec; Maher, Michael P.; Quan, Catherine; Raj, Christopher D.; McCormack, Ken; Numann, Randal; Negulescu, Paul A.; González, Jesús E
PUB. DATE
April 2006
SOURCE
Nature Biotechnology;Apr2006, Vol. 24 Issue 4, p439
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
Voltage-gated ion channels regulate many physiological functions and are targets for a number of drugs. Patch-clamp electrophysiology is the standard method for measuring channel activity because it fulfils the requirements for voltage control, repetitive stimulation and high temporal resolution, but it is laborious and costly. Here we report an electro-optical technology and automated instrument, called the electrical stimulation voltage ion probe reader (E-VIPR), that measures the activity of voltage-gated ion channels using extracellular electrical field stimulation and voltage-sensitive fluorescent probes. We demonstrate that E-VIPR can sensitively detect drug potency and mechanism of block on the neuronal human type III voltage-gated sodium channel expressed in human embryonic kidney cells. Results are compared with voltage-clamp and show that E-VIPR provides sensitive and information-rich compound blocking activity. Furthermore, we screened ∼400 drugs and observed sodium channel–blocking activity for ∼25% of them, including the antidepressants sertraline (Zoloft) and paroxetine (Paxil).
ACCESSION #
20456293

 

Related Articles

  • Sertraline: A Review of its Use in the Management of Major Depressive Disorder in Elderly Patients. Muijsers, R.B.R.; Plosker, G.L.; Noble, S. // Drugs & Aging;2002, Vol. 19 Issue 5, p377 

    Sertraline is a selective serotonin reuptake inhibitor (SSRI) with well established antidepressant and anxiolytic activity. Results from several well designed trials show that sertraline (50 to 200 mg/day) is effective in the treatment of major depressive disorder in elderly patients (≥60...

  • SSRIs increase risk of postprocedural bleeding.  // Reactions Weekly;6/5/2010, Issue 1304, p5 

    The article discusses a research study on the association between use of selective serotonin reuptake inhibitors (SSRI), specifically sertraline, and increased risk of postprocedural bleeding, published in the May 2010 issue of the journal "Digestive Disease Week."

  • These Two Psych Drugs Should Not Be Taken Together.  // RN;Apr2003, Vol. 66 Issue 4, p96 

    Reports that an additional contraindication has been added to the labeling for sertraline HCl, one of the most widely used selective serotonin reuptake inhibitors.

  • Transfersomes: A Novel Vesicular Carrier for Enhanced Transdermal Delivery of Sertraline: Development, Characterization, and Performance Evaluation. GUPTA, Ankit; AGGARWAL, Geeta; SINGLA, Samita; ARORA, Ritika // Scientia Pharmaceutica;2012, Vol. 80 Issue 4, p1061 

    The aim of the present study was to investigate transfersomes as a transdermal delivery system for the poorly soluble drug, sertraline, in order to overcome the troubles associated with its oral delivery. Different transfersomal formulations were prepared with non-ionic surfactant (span 80),...

  • Drug discrimination studies of the interoceptive cues produced by selective serotonin uptake inhibitors and selective serotonin releasing agents. Marona-Lewicka, Danuta; Nichols, D. E. // Psychopharmacology;1998, Vol. 138 Issue 1, p67 

    Abstract MMAI (5-methoxy-6-methyl-2-aminoindan) is a nonneurotoxic, highly selective neuronal serotonin (5-HT) releasing agent. MMAI and other 5-HT releasing agents produce a robust discriminative cue in drug discrimination (DD) studies. The selective serotonin reuptake inhibitors (SSRIs)...

  • Sertraline-related Bleeding Tendency: Could it be Dose-dependent? Shahrbabki, Mahin Eslami; Shahrbabaki, Amir Eslami // Iranian Journal of Psychiatry & Behavioral Sciences;Autumn2014, Vol. 8 Issue 3, p81 

    Selective serotonin reuptake inhibitors (SSRIs) are reported to be associated with increased bleeding tendency. While findings of recent studies explain a lot about the pathophysiology of this side-effect, there is a general tendency to discontinue SSRIs as harmful medications. We report two...

  • Linezolid interaction.  // Reactions Weekly;5/6/2006, Issue 1100, p15 

    Presents the study "Drug Interactions Between Linezolid and Selective Serotonin Reuptake Inhibitors: Case Report Involving Sertraline and Review of the Literature," which appeared in the February 2006 issue of "Phamacotherapy." Concomitant medications for the patient who developed serotonin...

  • MOOD-LIFTING HEART MEDICINE. Good, Brian // Men's Health;Nov2003, Vol. 18 Issue 9, p46 

    Provides information on a study on the Zoloft antidepressant drug. Link between the drug and heart-attacks; Psychological effect of taking the drug.

  • sertraline.  // Taber's Cyclopedic Medical Dictionary (2009);2009, Issue 21, p2107 

    An encyclopedia entry for "sertraline," which refers to a selective serotonin reuptake inhibitor and antidepressant to treat depression, panic, obsessive-compulsive disorder, and posttraumatic stress disorder, is presented.

Share

Read the Article

Courtesy of THE LIBRARY OF VIRGINIA

Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics