Effect of 17β-Estradiol on mRNA Expression of Large- Conductance, Voltage-Dependent, and Calcium-Activated Potassium Channel α and β Subunits in Guinea Pig

Endocrine ◽  
2003 ◽  
Vol 20 (3) ◽  
pp. 227-238 ◽  
Author(s):  
Khalid Jamali ◽  
Barry R. Naylor ◽  
Martin J. Kelly ◽  
Oline K. Ronnekleiv
Keyword(s):  
Guinea Pig ◽  
Potassium Channel ◽  
Mrna Expression ◽  
Voltage Dependent ◽  
17Β Estradiol ◽  
Α And Β Subunits ◽  
Calcium Activated Potassium Channel

Single delayed rectifier potassium channels from rabbit coronary artery myocytes

1993 ◽  
Vol 264 (4) ◽  
pp. H1146-H1153 ◽  
Author(s):  
K. A. Volk ◽  
E. F. Shibata
Keyword(s):  
Coronary Artery ◽  
Potassium Channels ◽  
Potassium Channel ◽  
Time Course ◽  
Delayed Rectifier ◽  
Voltage Dependent ◽  
Rabbit Coronary Artery ◽  
State Models ◽  
Calcium Activated Potassium Channel ◽  
Ik Channel

Cell-attached patches from rabbit coronary artery single smooth muscle cells contained two distinct potassium channel types, namely a large conductance calcium-activated potassium channel and a smaller voltage-activated potassium channel representing the delayed rectifier (IK). When a physiological potassium ion gradient was used, the average slope conductance of single IK channels was 7.26 pS. The time course of activation measured from ensemble averages was well fit by a single exponential raised to the power of 2 and was voltage dependent. Experiments were then performed with potassium (140 mM) on both sides of the membrane to resolve single IK channel currents during deactivation. Ensemble averages of this activity were well described by a two-component exponential, and the time constants were voltage dependent. Mean open times were significantly shorter during deactivation than during activation. Closed time distributions typically had two components. These kinetic characteristics were used in testing various state models for voltage-dependent potassium channels.

New Insights on KCa3.1 Channel Modulation

2020 ◽  
Vol 26 (18) ◽  
pp. 2096-2101
Author(s):  
Giuseppe Manfroni ◽  
Francesco Ragonese ◽  
Lorenzo Monarca ◽  
Andrea Astolfi ◽  
Loretta Mancinelli ◽  
...  
Keyword(s):  
Potassium Channel ◽  
Critical Role ◽  
Calcium Signalling ◽  
Typical Feature ◽  
Open Probability ◽  
Pharmacological Agents ◽  
Channel Modulation ◽  
Calcium Dependent ◽  
Modelling Techniques ◽  
Calcium Activated Potassium Channel

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.

scholarly journals Cooperative interactions among subunits of a voltage-dependent potassium channel. Evidence from expression of concatenated cDNAs.

1992 ◽  
Vol 267 (33) ◽  
pp. 23742-23745
Author(s):  
R.S. Hurst ◽  
M.P. Kavanaugh ◽  
J Yakel ◽  
J.P. Adelman ◽  
R.A. North
Keyword(s):  
Potassium Channel ◽  
Cooperative Interactions ◽  
Voltage Dependent
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