scholarly journals Development and Characterization of Novel Derivatives of the Antiepileptic Drug Lacosamide That Exhibit Far Greater Enhancement in Slow Inactivation of Voltage-Gated Sodium Channels

2010 ◽  
Vol 2 (2) ◽  
pp. 90-106 ◽  
Author(s):  
Yuying Wang ◽  
Ki Duk Park ◽  
Christophe Salomé ◽  
Sarah M. Wilson ◽  
James P. Stables ◽  
...  
Keyword(s):  
Antiepileptic Drug ◽  
Sodium Channels ◽  
Slow Inactivation ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels ◽  
Derivatives Of

Molecular characterization of voltage-gated sodium channels in human gliomas

Neuroreport ◽  
2002 ◽  
Vol 13 (18) ◽  
pp. 2493-2498 ◽  
Author(s):  
Michael Schrey ◽  
Carolina Codina ◽  
Robert Kraft ◽  
Christian Beetz ◽  
Rolf Kalff ◽  
...  
Keyword(s):  
Molecular Characterization ◽  
Sodium Channels ◽  
Human Gliomas ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

scholarly journals Purification and Characterization of JZTx-14, a Potent Antagonist of Mammalian and Prokaryotic Voltage-Gated Sodium Channels

Toxins ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 408 ◽  
Author(s):  
Jie Zhang ◽  
Dongfang Tang ◽  
Shuangyu Liu ◽  
Haoliang Hu ◽  
Songping Liang ◽  
...  
Keyword(s):  
Sodium Channels ◽  
Resting State ◽  
Purification And Characterization ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels ◽  
Steady State Inactivation ◽  
Ic50 Values ◽  
Gating Modifier ◽  
Potent Antagonist

Exploring the interaction of ligands with voltage-gated sodium channels (NaVs) has advanced our understanding of their pharmacology. Herein, we report the purification and characterization of a novel non-selective mammalian and bacterial NaVs toxin, JZTx-14, from the venom of the spider Chilobrachys jingzhao. This toxin potently inhibited the peak currents of mammalian NaV1.2–1.8 channels and the bacterial NaChBac channel with low IC50 values (<1 µM), and it mainly inhibited the fast inactivation of the NaV1.9 channel. Analysis of NaV1.5/NaV1.9 chimeric channel showed that the NaV1.5 domain II S3–4 loop is involved in toxin association. Kinetics data obtained from studying toxin–NaV1.2 channel interaction showed that JZTx-14 was a gating modifier that possibly trapped the channel in resting state; however, it differed from site 4 toxin HNTx-III by irreversibly blocking NaV currents and showing state-independent binding with the channel. JZTx-14 might stably bind to a conserved toxin pocket deep within the NaV1.2–1.8 domain II voltage sensor regardless of channel conformation change, and its effect on NaVs requires the toxin to trap the S3–4 loop in its resting state. For the NaChBac channel, JZTx-14 positively shifted its conductance-voltage (G–V) and steady-state inactivation relationships. An alanine scan analysis of the NaChBac S3–4 loop revealed that the 108th phenylalanine (F108) was the key residue determining the JZTx-14–NaChBac interaction. In summary, this study provided JZTx-14 with potent but promiscuous inhibitory activity on both the ancestor bacterial NaVs and the highly evolved descendant mammalian NaVs, and it is a useful probe to understand the pharmacology of NaVs.

scholarly journals Functional and Molecular Characterization of Voltage-Gated Sodium Channels in Uteri from Nonpregnant Rats1

2007 ◽  
Vol 77 (5) ◽  
pp. 855-863 ◽  
Author(s):  
Marian Seda ◽  
Francisco M. Pinto ◽  
Susan Wray ◽  
Cristina G. Cintado ◽  
Pedro Noheda ◽  
...  
Keyword(s):  
Molecular Characterization ◽  
Sodium Channels ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

The Investigational Anticonvulsant Lacosamide Selectively Enhances Slow Inactivation of Voltage-Gated Sodium Channels

2007 ◽  
Vol 73 (1) ◽  
pp. 157-169 ◽  
Author(s):  
Adam C. Errington ◽  
Thomas Stöhr ◽  
Cara Heers ◽  
George Lees
Keyword(s):  
Sodium Channels ◽  
Slow Inactivation ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

scholarly journals Lidocaine reduces the transition to slow inactivation in Na v 1.7 voltage‐gated sodium channels

2011 ◽  
Vol 164 (2b) ◽  
pp. 719-730 ◽  
Author(s):  
Patrick L Sheets ◽  
Brian W Jarecki ◽  
Theodore R Cummins
Keyword(s):  
Sodium Channels ◽  
Slow Inactivation ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

Species selective resistance of cardiac muscle voltage gated sodium channels: Characterization of brevetoxin and ciguatoxin binding sites in rats and fish

Toxicon ◽  
2006 ◽  
Vol 48 (6) ◽  
pp. 702-712 ◽  
Author(s):  
Marie-Yasmine Bottein Dechraoui ◽  
Jeremy J. Wacksman ◽  
John S. Ramsdell
Keyword(s):  
Cardiac Muscle ◽  
Sodium Channels ◽  
Binding Sites ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

Expression and Biophysical Characterization of Voltage-Gated Sodium Channels in Axons and Growth Cones of the Regenerating Optic Nerve

2010 ◽  
Vol 51 (3) ◽  
pp. 1789 ◽  
Author(s):  
Andreas Feigenspan ◽  
Karin Dedek ◽  
Katrin Schlich ◽  
Reto Weiler ◽  
Solon Thanos
Keyword(s):  
Optic Nerve ◽  
Sodium Channels ◽  
Growth Cones ◽  
Biophysical Characterization ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

scholarly journals Biophysical Characterization Of Duloxetine Activity On Voltage-gated Sodium Channels Involved In Pain Transmission

2009 ◽  
Vol 96 (3) ◽  
pp. 252a ◽  
Author(s):  
Jean-francois Rolland ◽  
David Madge ◽  
John Ford ◽  
Marc Rogers
Keyword(s):  
Sodium Channels ◽  
Biophysical Characterization ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels ◽  
Pain Transmission

scholarly journals Molecular and functional characterization of voltage-gated sodium channels in human sperm

2009 ◽  
Vol 7 (1) ◽  
pp. 71 ◽  
Author(s):  
Francisco M Pinto ◽  
Cristina G Ravina ◽  
Manuel Fernández-Sánchez ◽  
Manuel Gallardo-Castro ◽  
Antonio Cejudo-Román ◽  
...  
Keyword(s):  
Sodium Channels ◽  
Functional Characterization ◽  
Human Sperm ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels
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