Effects of external tetraethylammonium ions and quinine on delayed rectifying K+ channels in mouse pancreatic beta‐cells.
Open accessAbstract
1. The whole-cell and outside-out patch configurations of the patch-clamp technique were used to study the mechanisms of block produced by external tetraethylammonium ions (TEA+) and quinine on delayed rectifying K+ channels in mouse pancreatic beta-cells. 2. In whole-cell recordings, TEA+ blocks the delayed outward current (which reflects the activity of delayed rectifying K+ channels by greater than 85%) in a concentration-dependent manner. The block appeared to be 1:1 with a Kd of approximately 1.4 mM at a membrane potential of 0 mV. The value of Kd varied with the membrane potential and there was an e-fold increase for a 70 mV depolarization. 3. Single-channel recordings revealed that delayed rectifying K+ channels have a unitary conductance of 8.5 pS ([K+]1 = 155 mM; [K+]o = 5.6 mM) and a single-channel K+ permeability of 2.8 X 10(-14) cm3 s-1. 4. First latency histograms of channel openings during voltage pulses from -70 to 0 mV peaked after 4 ms. A reaction scheme involving two closed states adequately but not perfectly described the distribution of the first latencies. The openings of the channels were grouped in bursts and the distribution of the closed times required two exponentials with time constants of 2.0 and 13 ms, respectively. The distribution of the open times could be described by a single exponential with a time constant of 25 ms. 5. Channel block produced by TEA+ (1 mM) was associated with a 40% decrease of the single-channel current amplitudes and a red…
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BK channels are blocked by TEA with an IC50 of 100 μM, which is 15- and 200-fold lower than the corresponding values for the delayed rectifier and KATP channel, respectively.
“BK channels are blocked by the broad-spectrum K+ channel blocker TEA with an IC50 of 100µM, which is 15- and 200-fold lower than the corresponding values for the delayed rectifier and KATP channel, respectively (75, 76).”
From Pancreatic β-Cell Electrical Activity and Insulin Secretion: Of Mice and Men (2018) · cites this paper as [76]
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Pancreatic β-Cell Electrical Activity and Insulin Secretion: Of Mice and Men
Rorsman, P., & Ashcroft, F. M. (2018) · Physiological Reviews · doi:10.1152/physrev.00008.2017 · Cited by 793 · see citing works
Self-citationGöpel, S. O., Kanno, T., Barg, S., Eliasson, L., Galvanovskis, J., Renström, E., & Rorsman, P. (1999) · The Journal of General Physiology · doi:10.1085/jgp.114.6.759 · Cited by 137 · see citing works
Self-citation
- Authors
- Bokvist, K., Rorsman, P., & Smith, P. A.
- Affiliations
- University of Gothenburg (SE)
- Venue
- The Journal of Physiology
- Publisher
- Wiley
- Published
- 1990-04
- Volume
- 423
- Issue
- 1
- Pages
- 311-325
- ISSN
- 0022-3751 (ISSN-L)
- 1469-7793
- PMC
- PMC1189759
- OpenAlex
- W2030128200
- Cited by
- 69
- References
- 0
- Citations by year
- 2025: 1 · 2021: 2 · 2019: 1 · 2017: 1 · 2015: 1 · 2014: 1
- FWCI
- 2.28
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- The Journal of Physiology (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Health Sciences › Medicine › Surgery › Pancreatic function and diabetes
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion Transport and Channel Regulation
- Keywords
- tetraethylammonium, quinine, pancreatic beta cells, channel block, single-channel kinetics, single-channel conductance, potassium permeability, binding stoichiometry, membrane potential dependence, channel openers
- MeSH terms
- Animals, Electrophysiology, Evoked Potentials, Islets of Langerhans, Kinetics, Quinine, Tetraethylammonium Compounds, Potassium Channels, Tetraethylammonium, Mice, In Vitro Techniques
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