Synthesis of Skeletal Analogues of Saxitoxin Derivatives and Evaluation of Their Inhibitory Activity on Sodium Ion Channels NaV1.4 and NaV1.5

2011 ◽  
Vol 17 (43) ◽  
pp. 12144-12152 ◽  
Author(s):  
Ryoko Shinohara ◽  
Takafumi Akimoto ◽  
Osamu Iwamoto ◽  
Takatsugu Hirokawa ◽  
Mari Yotsu-Yamashita ◽  
...  
Keyword(s):  
Ion Channels ◽  
Inhibitory Activity ◽  
Sodium Ion ◽  
Sodium Ion Channels

scholarly journals Synthesis and Evaluation of Novel α-Aminoamides Containing Benzoheterocyclic Moiety for the Treatment of Pain

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1716
Author(s):  
Kun Tong ◽  
Ruotian Zhang ◽  
Fengzhi Ren ◽  
Tao Zhang ◽  
Junlin He ◽  
...  
Keyword(s):  
Ion Channels ◽  
Patch Clamp ◽  
Formalin Test ◽  
Sodium Ion ◽  
Inhibitory Potency ◽  
Voltage Gated ◽  
Patch Clamp Electrophysiology ◽  
Sodium Ion Channels

Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds 6a, 6e, and 6f containing the benzofuran group displayed more potent in vivo analgesic activity than ralfinamide in both the formalin test and the writhing assay. Interestingly, they also exhibited potent in vitro anti-Nav1.7 and anti-Nav1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds 6a, 6e, and 6f, which have inhibitory potency for two pain-related Nav targets, could serve as new leads for the development of analgesic medicines.

scholarly journals Guanidinium Toxins and Their Interactions with Voltage-Gated Sodium Ion Channels

Marine Drugs ◽  
2017 ◽  
Vol 15 (10) ◽  
pp. 303 ◽  
Author(s):  
Lorena Durán-Riveroll ◽  
Allan Cembella
Keyword(s):  
Ion Channels ◽  
Sodium Ion ◽  
Voltage Gated ◽  
Sodium Ion Channels
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