Structure-activity relationships of .mu.-conotoxin GIIIA: structure determination of active and inactive sodium channel blocker peptides by NMR and simulated annealing calculations

Biochemistry ◽  
1992 ◽  
Vol 31 (50) ◽  
pp. 12577-12584 ◽  
Author(s):  
Kaori Wakamatsu ◽  
Daisuke Kohda ◽  
Hideki Hatanaka ◽  
Jean Marc Lancelin ◽  
Yukisato Ishida ◽  
...  
Keyword(s):  
Simulated Annealing ◽  
Sodium Channel ◽  
Structure Determination ◽  
Channel Blocker ◽  
Sodium Channel Blocker ◽  
Structure Activity Relationships ◽  
Structure Activity

Voltage Gated Sodium Channel Blockers: Synthesis of Mexiletine Analogues and Homologues

2020 ◽  
Vol 27 ◽  
Author(s):  
Alessia Catalano ◽  
Carlo Franchini ◽  
Alessia Carocci
Keyword(s):  
Sodium Channel ◽  
Channel Blocker ◽  
Parent Compound ◽  
Channel Blockers ◽  
Sodium Channel Blocker ◽  
Starting Point ◽  
Channel Blocking ◽  
Blocking Activity ◽  
Synthetic Routes ◽  
Lateral Sclerosis

: Mexiletine is an antiarrhythmic drug belonging to IB class, acting as sodium channel blocker. Besides its well-known activity on arrhythmias, its usefulness in the treatment of myotonia, myotonic distrophy and amyotrophic lateral sclerosis is now widely recognized. Nevertheless, it has been retired from the market in several countries because of its undesired effects. Thus, several papers were reported in the last years about analogues and homologues of mexiletine being endowed with a wider therapeutic ratio and a more selectivity of action. Some of them showed sodium channel blocking activity higher than the parent compound. It is noteworthy that mexiletine is used in therapy as a racemate even though a difference in the activities of the two enantiomers were widely demonstrated, with (–)-(R)-enantiomer being more active: this finding led several research groups to study mexiletine and its analogues and homologues in their optically active forms. This review summarizes the different synthetic routes used to obtain these compounds. They could represent an interesting starting point to new mexiletine-like compounds without common side effects related to the use of mexiletine.

scholarly journals B-PO04-024 PREDICTION OF A POSITIVE SODIUM CHANNEL BLOCKER PROVOCATION TEST IN PATIENTS SUSPECTED OF BRUGADA SYNDROME

Heart Rhythm ◽  
2021 ◽  
Vol 18 (8) ◽  
pp. S289
Author(s):  
Martijn Hendrik van der Ree ◽  
Jeroen Vendrik ◽  
Tom E. Verstraelen ◽  
Jan A. Kors ◽  
Ahmad S. Amin ◽  
...  
Keyword(s):  
Sodium Channel ◽  
Brugada Syndrome ◽  
Channel Blocker ◽  
Provocation Test ◽  
Sodium Channel Blocker

scholarly journals From Plastic-Bottle-Toxin to Sodium Channel Blocker: A New Role for Bisphenol A

2010 ◽  
Vol 98 (3) ◽  
pp. 114a
Author(s):  
Angelika Lampert ◽  
Andrias O. O'Reilly ◽  
B.A. Wallace ◽  
Christian Alzheimer
Keyword(s):  
Bisphenol A ◽  
Sodium Channel ◽  
Channel Blocker ◽  
Sodium Channel Blocker ◽  
Plastic Bottle

Synthesis of Vixotrigine, a Use-Dependent Sodium Channel Blocker. Part 1: Development of Bulk Supply Routes to Enable Proof of Concept

2020 ◽  
Vol 24 (12) ◽  
pp. 2802-2813 ◽  
Author(s):  
Gerard Giblin ◽  
Adrian Heseltine ◽  
William Kiesman ◽  
David MacPherson ◽  
James Ramsden ◽  
...  
Keyword(s):  
Sodium Channel ◽  
Channel Blocker ◽  
Proof Of Concept ◽  
Sodium Channel Blocker
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