Photoaffinity Ligand for the Inhalational Anesthetic Sevoflurane Allows Mechanistic Insight into Potassium Channel Modulation

2017 ◽  
Vol 12 (5) ◽  
pp. 1353-1362 ◽  
Author(s):  
Kellie A. Woll ◽  
Wesley Peng ◽  
Qiansheng Liang ◽  
Lianteng Zhi ◽  
Jack A. Jacobs ◽  
...  

1986 ◽  
Vol 124 (1) ◽  
pp. 287-306
Author(s):  
S. A. Siegelbaum ◽  
F. Belardetti ◽  
J. S. Camardo ◽  
M. J. Shuster

Using single-channel recording, we have been able to obtain some insight into the molecular mechanism of a modulatory transmitter action in Aplysia sensory neurones. Our results show that serotonin produces a slow EPSP and increases action potential duration in the sensory neurones by producing prolonged closures of the S potassium channel. Such closures appear to be mediated by cyclic AMP-dependent phosphorylation of a membrane protein which may be the channel. Modulation of S channels by serotonin also occurs in sensory neurone growth cones. This provides the first direct evidence that channel modulation occurs in nerve processes and increases the likelihood of channel modulation at the nerve terminal.



2018 ◽  
Vol 150 (4) ◽  
pp. 517-520 ◽  
Author(s):  
Keith K. Khoo ◽  
Stephan A. Pless

Khoo and Pless examine new work that provides mechanistic insight into the role of the intrinsic ligand in KCNH ion channels.​





2020 ◽  
Vol 26 (18) ◽  
pp. 2096-2101
Author(s):  
Giuseppe Manfroni ◽  
Francesco Ragonese ◽  
Lorenzo Monarca ◽  
Andrea Astolfi ◽  
Loretta Mancinelli ◽  
...  

The human intermediate conductance calcium-activated potassium channel, KCa3.1, is involved in several pathophysiological conditions playing a critical role in cell secretory machinery and calcium signalling. The recent cryo-EM analysis provides new insights for understanding the modulation by both endogenous and pharmacological agents. A typical feature of this channel is the low open probability in saturating calcium concentrations and its modulation by potassium channel openers (KCOs), such as benzo imidazolone 1-EBIO, without changing calcium-dependent activation. In this paper, we proposed a model of KCOs action in the modulation of channel activity. The KCa3.1 channel has a very rich pharmacological profile with several classes of molecules that selectively interact with different binding sites of the channel. Among them, benzo imidazolones can be openers (positive modulators such as 1-EBIO, DC-EBIO) or blockers (negative modulators such as NS1619). Through computation modelling techniques, we identified the 1,4-benzothiazin-3-one as a promising scaffold to develop new KCa3.1 channel modulators. Further studies are needed to explore the potential use of 1-4 benzothiazine- 3-one in KCa3.1 modulation and its pharmacological application.



RSC Advances ◽  
2021 ◽  
Vol 11 (34) ◽  
pp. 20961-20969
Author(s):  
Yunqing He ◽  
Wanli Nie ◽  
Ying Xue ◽  
Qishan Hu

Hydrosilylation or amination products? It depends on water amount and nucleophiles like excess water or produced/added amines.





2021 ◽  
Vol 154 (12) ◽  
pp. 124313
Author(s):  
L. M. Hunnisett ◽  
P. F. Kelly ◽  
S. Bleay ◽  
F. Plasser ◽  
R. King ◽  
...  




Sign in / Sign up

Export Citation Format

Share Document