Sodium channel-blocking properties of flecainide, a class IC antiarrhythmic drug, in guinea-pig papillary muscles An open channel blocker or an inactivated channel blocker

1989 ◽  
Vol 339 (4) ◽  
pp. 441-447 ◽  
Author(s):  
Michio Kojima ◽  
Takuyuki Hamamoto ◽  
Takashi Ban
Keyword(s):  
Guinea Pig ◽  
Sodium Channel ◽  
Antiarrhythmic Drug ◽  
Open Channel ◽  
Channel Blocker ◽  
Papillary Muscles ◽  
Channel Blocking ◽  
Open Channel Blocker

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.

7-Methoxyderivative of tacrine is a ‘foot-in-the-door’ open-channel blocker of GluN1/GluN2 and GluN1/GluN3 NMDA receptors with neuroprotective activity in vivo

2018 ◽  
Vol 140 ◽  
pp. 217-232 ◽  
Author(s):  
Martina Kaniakova ◽  
Lenka Kleteckova ◽  
Katarina Lichnerova ◽  
Kristina Holubova ◽  
Kristyna Skrenkova ◽  
...  
Keyword(s):  
Nmda Receptors ◽  
Open Channel ◽  
Channel Blocker ◽  
Neuroprotective Activity ◽  
Open Channel Blocker

A novel role of the antitumor agent tricyclodecan-9-yl-xanthogenate as an open channel blocker of KCNQ1/KCNE1

2018 ◽  
Vol 824 ◽  
pp. 99-107 ◽  
Author(s):  
Meikui Wu ◽  
Makoto Takemoto ◽  
Huan Luo ◽  
Jian-Jun Xu ◽  
Mei-Hong Lu ◽  
...  
Keyword(s):  
Open Channel ◽  
Channel Blocker ◽  
Antitumor Agent ◽  
Open Channel Blocker
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