Faculty Opinions recommendation of A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

2007 ◽  
Author(s):  
Anthony Dickenson
Keyword(s):  
Sodium Channel ◽  
Inflammatory Pain ◽  
Channel Blocker ◽  
Sodium Channel Blocker ◽  
Nav1.8 Sodium Channel

scholarly journals Inhibition of inflammatory pain and cough by a novel charged sodium channel blocker

2021 ◽  
Author(s):  
Ivan Tochitsky ◽  
Sooyeon Jo ◽  
Nick Andrews ◽  
Masakazu Kotoda ◽  
Benjamin Doyle ◽  
...  
Keyword(s):  
Sodium Channel ◽  
Inflammatory Pain ◽  
Channel Blocker ◽  
Sodium Channel Blocker

scholarly journals The Selective Nav1.8 Sodium Channel Blocker A-803467 Affects Electrical Activity in Intracardiac Neurons, but not in Cardiomyocytes

2011 ◽  
Vol 100 (3) ◽  
pp. 421a-422a
Author(s):  
Marieke W. Veldkamp ◽  
Carol A. Remme ◽  
Brendon Scicluna ◽  
Cees A. Schumacher ◽  
Rianne Wolswinkel ◽  
...  
Keyword(s):  
Electrical Activity ◽  
Sodium Channel ◽  
Channel Blocker ◽  
Sodium Channel Blocker ◽  
Nav1.8 Sodium Channel ◽  
Intracardiac Neurons

A-887826 is a structurally novel, potent and voltage-dependent Nav1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats

2010 ◽  
Vol 59 (3) ◽  
pp. 201-207 ◽  
Author(s):  
Xu-Feng Zhang ◽  
Char-Chang Shieh ◽  
Mark L. Chapman ◽  
Mark A. Matulenko ◽  
Ahmed H. Hakeem ◽  
...  
Keyword(s):  
Sodium Channel ◽  
Channel Blocker ◽  
Tactile Allodynia ◽  
Sodium Channel Blocker ◽  
Voltage Dependent ◽  
Nav1.8 Sodium Channel

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.

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