7-methoxyderivative of tacrine is a potent open channel blocker of NMDA receptors

2017 ◽  
Vol 381 ◽  
pp. 490-491
Author(s):  
M. Horak ◽  
M. Kaniakova ◽  
O. Soukup ◽  
J. Korabecny
Keyword(s):  
Nmda Receptors ◽  
Open Channel ◽  
Channel Blocker ◽  
Open Channel Blocker

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

Evidence That Xenon Does Not Produce Open Channel Blockade of the NMDA Receptor

2008 ◽  
Vol 99 (4) ◽  
pp. 1983-1987 ◽  
Author(s):  
Henry U. Weigt ◽  
Oliver Adolph ◽  
Michael Georgieff ◽  
Eva M. Georgieff ◽  
Karl J. Föhr
Keyword(s):  
Nmda Receptor ◽  
Nmda Receptors ◽  
Open Channel ◽  
Channel Blocker ◽  
Channel Blockers ◽  
Cell Recording ◽  
Neuro2a Cells ◽  
Induced Currents ◽  
Mutant Receptors ◽  
Open Channel Blocker

Previous studies had not excluded the possibility that the mechanism by which Xenon (Xe) blocks N-methyl-d-aspartate (NMDA) receptors might be that of an open-channel blocker. We tested this possibility on mutant NMDA receptors carrying an alanine (A) to cysteine (C) mutation located within the SYTANLAAF-motif of the third transmembrane region (TM3). This mutation was shown to yield constitutively open ion channels after modification with a thiol-modifying reagent. We expressed such mutant channels in Neuro2A cells and recorded glutamate (50 μM)-induced currents in the whole cell recording mode. Although Xe (3.5 mM) blocked the currents through the wild-type receptor NR1-1a/NR2A and NR1-1a/NR2B by ∼40% and those through the mutant receptors NR1-1a/NR2A(A650C) or NR1-1a/NR2B(A651C) by ∼30%, it was unable to block the currents through the methane thiosulfonate etyhlammonium-modified mutant receptors. On the other hand, established open-channel blockers of the NMDA receptor such as MK-801 (1 μM) or Mg ions (Mg2+; 1 mM) were able to block these permanently open channels. These results suggest that Xe does not act as a classical open-channel blocker at the NMDA receptor.

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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