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Journal articles on the topic 'Potassium channel openers'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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1

Hedlund, H. "Potassium channel openers for treatment of bladder hyperactivity." Urologia Journal 63, no. 4 (1996): 445–47. http://dx.doi.org/10.1177/039156039606300406.

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The potassium (K+) channel openers induce hyperpolarization by ATP-sensitive K+ channels. This group of compounds has been demonstrated to effectively relax the human detrusor and reduce bladder hyperactivity in obstructed rats. In patients with overactive bladders, oral administration and intravenous infusion of different K+ channel openers were without significant effect on urodynamic variables. In conscious dogs, a new K+ channel opener was found to increase bladder compliance with reduced micturition frequency. K+ channel openers have an interesting potential for the treatment of bladder h

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2

Ozcan, Cevher, Martin Bienengraeber, Petras P. Dzeja, and Andre Terzic. "Potassium channel openers protect cardiac mitochondria by attenuating oxidant stress at reoxygenation." American Journal of Physiology-Heart and Circulatory Physiology 282, no. 2 (2002): H531—H539. http://dx.doi.org/10.1152/ajpheart.00552.2001.

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K+ channel openers have been recently recognized for their ability to protect mitochondria from anoxic injury. Yet the mechanism responsible for mitochondrial preservation under oxidative stress is not fully understood. Here, mitochondria were isolated from rat hearts and subjected to 20-min anoxia, followed by reoxygenation. At reoxygenation, increased generation of reactive oxygen species (ROS) was associated with reduced ADP-stimulated oxygen consumption, blunted ATP production, and disrupted mitochondrial structural integrity coupled with cytochrome c release. The prototype K+ channel open

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3

Seth, Vikas, Mushtaq Ahmad, Prerna Upadhyaya, Monika Sharma, and Vijay Moghe. "Effect of Potassium Channel Modulators on Morphine Withdrawal in Mice." Substance Abuse: Research and Treatment 4 (January 2010): SART.S6211. http://dx.doi.org/10.4137/sart.s6211.

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The present study was conducted to investigate the effect of potassium channel openers and blockers on morphine withdrawal syndrome. Mice were rendered dependent on morphine by subcutaneous injection of morphine; four hours later, withdrawal was induced by using an opioid antagonist, naloxone. Mice were observed for 30 minutes for the withdrawal signs ie, the characteristic jumping, hyperactivity, urination and diarrhea. ATP-dependent potassium (K+ATP) channel modulators were injected intraperitoneally (i.p.) 30 minutes before the naloxone. It was found that a K+ATP channel opener, minoxidil (

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4

Duty, Susan, and Arthur H. Weston. "Potassium Channel Openers." Drugs 40, no. 6 (1990): 785–91. http://dx.doi.org/10.2165/00003495-199040060-00002.

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5

Lawson, Kim. "Is there a Therapeutic Future for ‘Potassium Channel Openers’?" Clinical Science 91, no. 6 (1996): 651–63. http://dx.doi.org/10.1042/cs0910651.

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1. Potassium channels, which control cell electrical activity, are among the most regulated of all ion channels in biology. Promotion of activity in K+ channels by a wide range of physiological factors tends to stabilize cell function. 2. The discovery of synthetic molecules (e.g. cromakalim) that ‘directly’ open ATP-sensitive K+ channels has led to a new direction in pharmacology. ATP-sensitive K+ channel-opening properties have subsequently been demonstrated in a diverse range of chemical structures (synthetic and endogenous). 3. The existence of so many different subtypes of K+ channels has

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6

Morley, J. "Potassium channel openers and asthma." Clinical Reviews in Allergy 12, no. 1 (1994): 109–20. http://dx.doi.org/10.1007/bf02815513.

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7

Menasché, Philippe, Egidijus Kevelaitis, Christian Mouas, Christian Grousset, Armand Piwnica, and Gérard Bloch. "Preconditioning with potassium channel openers:." Journal of Thoracic and Cardiovascular Surgery 110, no. 6 (1995): 1606–14. http://dx.doi.org/10.1016/s0022-5223(95)70020-x.

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8

Atwal, Karnail S., Suzanne Moreland, John R. McCullough, Brian C. O'Reilly, Syed Z. Ahmed, and Diane E. Normandin. "Aryl cyanoguanidine potassium channel openers." Bioorganic & Medicinal Chemistry Letters 2, no. 1 (1992): 83–86. http://dx.doi.org/10.1016/s0960-894x(00)80661-7.

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9

Atwal, Karnail S., Suzanne Moreland, John R. McCullough, Syed Z. Ahmed, and Diane E. Normandin. "Benzopyranyl-cyanoguanidine potassium channel openers." Bioorganic & Medicinal Chemistry Letters 2, no. 1 (1992): 87–90. http://dx.doi.org/10.1016/s0960-894x(00)80662-9.

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10

Frank, C. A., J. M. Forst, T. Grant, et al. "Dihydropyridine KATP potassium channel openers." Bioorganic & Medicinal Chemistry Letters 3, no. 12 (1993): 2725–26. http://dx.doi.org/10.1016/s0960-894x(01)80751-4.

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11

Nardi, Antonio, and Søren-Peter Olesen. "Acrylamides as potassium channel openers." Expert Opinion on Therapeutic Patents 17, no. 10 (2007): 1215–26. http://dx.doi.org/10.1517/13543776.17.10.1215.

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12

Bantel, Carsten, Mervyn Maze, and Stefan Trapp. "Noble Gas Xenon Is a Novel Adenosine Triphosphate-sensitive Potassium Channel Opener." Anesthesiology 112, no. 3 (2010): 623–30. http://dx.doi.org/10.1097/aln.0b013e3181cf894a.

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Background Adenosine triphosphate-sensitive potassium (KATP) channels in brain are involved in neuroprotective mechanisms. Pharmacologic activation of these channels is seen as beneficial, but clinical exploitation by using classic K channel openers is hampered by their inability to cross the blood-brain barrier. This is different with the inhalational anesthetic xenon, which recently has been suggested to activate KATP channels; it partitions freely into the brain. Methods To evaluate the type and mechanism of interaction of xenon with neuronal-type KATP channels, these channels, consisting o

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13

Gomma, Abuzeid H., Henry J. Purcell, and Kim M. Fox. "Potassium Channel Openers in Myocardial Ischaemia." Drugs 61, no. 12 (2001): 1705–10. http://dx.doi.org/10.2165/00003495-200161120-00002.

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14

Auchampach, J. A., M. Maruyama, and G. J. Gross. "Cardioprotective Actions of Potassium Channel Openers." European Heart Journal 15, suppl C (1994): 89–94. http://dx.doi.org/10.1093/eurheartj/15.suppl_c.89.

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15

Andersson, Karl-Erik. "Clinical Pharmacology of Potassium Channel Openers." Pharmacology & Toxicology 70, no. 4 (1992): 244–54. http://dx.doi.org/10.1111/j.1600-0773.1992.tb00466.x.

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16

Dȩbska, Grażyna, Rebecca May, Anna Kicińska, Adam Szewczyk, Christian E. Elger, and Wolfram S. Kunz. "Potassium channel openers depolarize hippocampal mitochondria." Brain Research 892, no. 1 (2001): 42–50. http://dx.doi.org/10.1016/s0006-8993(00)03187-5.

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17

Weston, A. H. "Pharmacological actions of potassium-channel openers." European Journal of Pharmacology 183, no. 1 (1990): 70. http://dx.doi.org/10.1016/0014-2999(90)91323-4.

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18

Carlsen, J. E. "Clinical trials of potassium channel openers." European Journal of Pharmacology 183, no. 1 (1990): 70–71. http://dx.doi.org/10.1016/0014-2999(90)91324-5.

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19

Edwards, Gillian, and Arthur H. Weston. "Pharmacology of the potassium channel openers." Cardiovascular Drugs and Therapy 9, S2 (1995): 185–93. http://dx.doi.org/10.1007/bf00878465.

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20

Haverkamp, Wilhelm, Martin Borggrefe, and G�nter Breithardt. "Electrophysiologic effects of potassium channel openers." Cardiovascular Drugs and Therapy 9, S2 (1995): 195–202. http://dx.doi.org/10.1007/bf00878466.

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21

Wrzosek, Antoni, Bartłomiej Augustynek, Monika Żochowska, and Adam Szewczyk. "Mitochondrial Potassium Channels as Druggable Targets." Biomolecules 10, no. 8 (2020): 1200. http://dx.doi.org/10.3390/biom10081200.

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Mitochondrial potassium channels have been described as important factors in cell pro-life and death phenomena. The activation of mitochondrial potassium channels, such as ATP-regulated or calcium-activated large conductance potassium channels, may have cytoprotective effects in cardiac or neuronal tissue. It has also been shown that inhibition of the mitochondrial Kv1.3 channel may lead to cancer cell death. Hence, in this paper, we examine the concept of the druggability of mitochondrial potassium channels. To what extent are mitochondrial potassium channels an important, novel, and promisin

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22

Nishikawa, Masakuni, Maki Gohda, Sumio Matzno, Takeshi Uchida, Norifumi Nakamura, and Masahiro Watanabe. "Vasorelaxant properties of AL0671, a novel potassium channel opener, in comparison with other potassium channel openers." Japanese Journal of Pharmacology 61 (1993): 116. http://dx.doi.org/10.1016/s0021-5198(19)51370-1.

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23

Atwal, Karnail S. "Myocardial Protection with the ATP-Sensitive Potassium Channel Openers." Current Medicinal Chemistry 3, no. 4 (1996): 227–38. http://dx.doi.org/10.2174/092986730304220302110212.

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Abstract: The ATP-sensitive potassium channel (KArP) openers (e.g., Cromakalim) were originally developed for the treatment of hypertension, primarily due to their potent peripheral vasodilating properties. However, the clinical studies have failed to demonstrate any advantage of these compounds over the more established antihypertensive agents. Experimen tal studies have shown that the KArP openers may be effective for the treat ment of a variety of diseases (asthma, urinary incontinence, ischemia etc.) besides hypertension. However, their clinical utility is limited due to lack of tissue s

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24

Kicińska, A., G. D bska, W. Kunz, and A. Szewczyk. "Mitochondrial potassium and chloride channels." Acta Biochimica Polonica 47, no. 3 (2000): 541–51. http://dx.doi.org/10.18388/abp.2000_3977.

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Channels selective for potassium or chloride ions are present in inner mitochondrial membranes. They probably play an important role in mitochondrial events such as the formation of delta pH and regulation of mitochondrial volume changes. Mitochondrial potassium and chloride channels could also be the targets for pharmacologically active compounds such as potassium channel openers and antidiabetic sulfonylureas. This review describes the properties, pharmacology, and current observations concerning the functional role of mitochondrial potassium and chloride channels.

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25

Debska, G., A. Kicińska, J. Skalska, and A. Szewczyk. "Intracellular potassium and chloride channels: an update." Acta Biochimica Polonica 48, no. 1 (2001): 137–44. http://dx.doi.org/10.18388/abp.2001_5120.

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Channels selective for potassium or chloride ions are present in all intracellular membranes such as mitochondrial membranes, sarcoplasmic/endoplasmic reticulum, nuclear membrane and chromaffin granule membranes. They probably play an important role in events such as acidification of intracellular compartments and regulation of organelle volume. Additionally, intracellular ion channels are targets for pharmacologically active compounds, e.g. mitochondrial potassium channels interact with potassium channel openers such as diazoxide. This review describes current observations concerning the prop

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26

Nardi, A., V. Calderone, and S. Olesen. "Potassium Channel Openers: The Case of BK Channel Activators." Letters in Drug Design & Discovery 3, no. 4 (2006): 210–18. http://dx.doi.org/10.2174/157018006776743242.

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27

Elinder, Fredrik. "Potassium channel openers targeting different sites of the channel." Biophysical Journal 122, no. 3 (2023): 294a. http://dx.doi.org/10.1016/j.bpj.2022.11.1665.

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28

Wu, Yong-Jin, and Steven Dworetzky. "Recent Developments on KCNQ Potassium Channel Openers." Current Medicinal Chemistry 12, no. 4 (2005): 453–60. http://dx.doi.org/10.2174/0929867053363045.

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29

&NA;. "Pluses and minuses of potassium channel openers ???" Inpharma Weekly &NA;, no. 916 (1993): 11. http://dx.doi.org/10.2165/00128413-199309160-00024.

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30

Denda, M., M. Tsutsumi, K. Inoue, D. Crumrine, K. R. Feingold, and P. M. Elias. "Potassium channel openers accelerate epidermal barrier recovery." British Journal of Dermatology 157, no. 5 (2007): 888–93. http://dx.doi.org/10.1111/j.1365-2133.2007.08198.x.

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31

Quast, U. "Potassium channel openers: pharmacological and clinical aspects." Fundamental & Clinical Pharmacology 6, no. 7 (1992): 279–93. http://dx.doi.org/10.1111/j.1472-8206.1992.tb00122.x.

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32

Kicinska, Anna, Jolanta Skalska, and Adam Szewczyk. "Mitochondria and Big-Conductance Potassium Channel Openers." Toxicology Mechanisms and Methods 14, no. 1-2 (2004): 63–65. http://dx.doi.org/10.1080/15376520490257491.

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33

Al-Karagholi, Mohammad Al-Mahdi. "Involvement of Potassium Channel Signalling in Migraine Pathophysiology." Pharmaceuticals 16, no. 3 (2023): 438. http://dx.doi.org/10.3390/ph16030438.

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Migraine is a primary headache disorder ranked as the leading cause of years lived with disability among individuals younger than 50 years. The aetiology of migraine is complex and might involve several molecules of different signalling pathways. Emerging evidence implicates potassium channels, predominantly ATP-sensitive potassium (KATP) channels and large (big) calcium-sensitive potassium (BKCa) channels in migraine attack initiation. Basic neuroscience revealed that stimulation of potassium channels activated and sensitized trigeminovascular neurons. Clinical trials showed that administrati

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34

Vyas, Vivek K., Palak Parikh, Jonali Ramani, and Manjunath Ghate. "Medicinal Chemistry of Potassium Channel Modulators: An Update of Recent Progress (2011-2017)." Current Medicinal Chemistry 26, no. 12 (2019): 2062–84. http://dx.doi.org/10.2174/0929867325666180430152023.

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Background: Potassium (K+) channels participate in many physiological processes, cardiac function, cell proliferation, neuronal signaling, muscle contractility, immune function, hormone secretion, osmotic pressure, changes in gene expression, and are involved in critical biological functions, and in a variety of diseases. Potassium channels represent a large family of tetrameric membrane proteins. Potassium channels activation reduces excitability, whereas channel inhibition increases excitability. Objective: Small molecule K+ channel activators and inhibitors interact with voltage-gated, inwa

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35

Qiu, Bo, Yuhong Wang, Congxin Li, Huicai Guo, and Yanfang Xu. "Utility of the JT Peak Interval and the JT Area in Determining the Proarrhythmic Potential of QT-Shortening Agents." Journal of Cardiovascular Pharmacology and Therapeutics 24, no. 2 (2018): 160–71. http://dx.doi.org/10.1177/1074248418791999.

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Drug-induced long QT increases the risk of ventricular tachyarrhythmia known as torsades de pointes (TdP). Many biomarkers have been used to predict TdP. At present, however, there are few biomarkers for arrhythmias induced by QT-shortening drugs. The objective of the present study was to identify the best biomarkers for predicting arrhythmias caused by the 4 potassium channel openers ICA-105574, NS-1643, R-L3, and pinacidil. Our results showed that, at higher concentrations, all 4 potassium channel openers induced ventricular tachycardia (VT) and ventricular fibrillation (VF) in Langendorff-p

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36

Atwal, Kamail S., and Gary J. Grover. "Treatment of Myocardial Ischemia with ATP-Sensitive Potassium Channel (KATP) Openers." Current Pharmaceutical Design 2, no. 5 (1996): 585–95. http://dx.doi.org/10.2174/1381612802666221004183709.

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ATP-sensitive potassium channel (KATP) openers are potent antihypertensive agents due to their peripheral vasodilating properties. Although KATP openers have been shown to be direct cardioprotective agents, they carry a certain degree of liability for their use as cardioprotective agents. Their potent coronary and peripheral vasodilating properties can cause complications such as coronary artery steal and hypotension resulting in underperfusion of the tissue already at risk. Also, cardioprotection is not related to action potential shortening and the development of agents devoid of this activi

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37

Su, Tzu-Rong, Wen-Shan Zei, Ching-Chyuan Su, George Hsiao, and Min-Jon Lin. "The Effects of the KCNQ Openers Retigabine and Flupirtine on Myotonia in Mammalian Skeletal Muscle Induced by a Chloride Channel Blocker." Evidence-Based Complementary and Alternative Medicine 2012 (2012): 1–9. http://dx.doi.org/10.1155/2012/803082.

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The purpose of this study was to investigate the effect of KCNQ (potassium channel, voltage-gated, KQT-like subfamily) openers in preventing myotonia caused by anthracene-9-carboxylic acid (9-AC, a chloride channel blocker). An animal model of myotonia can be elicited in murine skeletal muscle by 9-AC treatment. KCNQ openers, such as retigabine and flupirtine, can inhibit the increased twitch amplitude (0.1 Hz stimulation) and reduce the tetanic fade (20 Hz stimulations) observed in the presence of 9-AC. Furthermore, the prolonged twitch duration of skeletal muscle was also inhibited by retiga

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38

Henry, P., and D. Escande. "Do potassium channel openers compete with ATP to activate ATP sensitive potassium channels?" Cardiovascular Research 28, no. 6 (1994): 754–59. http://dx.doi.org/10.1093/cvr/28.6.754.

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39

Pryce, Gareth, Sofia Sisay, Gavin Giovannoni, David L. Selwood, and David Baker. "Neuroprotection in an Experimental Model of Multiple Sclerosis via Opening of Big Conductance, Calcium-Activated Potassium Channels." Pharmaceuticals 16, no. 7 (2023): 972. http://dx.doi.org/10.3390/ph16070972.

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Big conductance calcium-activated (BK) channel openers can inhibit pathologically driven neural hyperactivity to control symptoms via hyperpolarizing signals to limit neural excitability. We hypothesized that BK channel openers would be neuroprotective during neuroinflammatory, autoimmune disease. The neurodegenerative disease was induced in a mouse experimental autoimmune encephalomyelitis model with translational value to detect neuroprotection in multiple sclerosis. Following the treatment with the BK channel openers, BMS-204253 and VSN16R, neuroprotection was assessed using subjective and

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40

Lee, Sang-Yeon, Hyun Been Choi, Mina Park, et al. "Novel KCNQ4 variants in different functional domains confer genotype- and mechanism-based therapeutics in patients with nonsyndromic hearing loss." Experimental & Molecular Medicine 53, no. 7 (2021): 1192–204. http://dx.doi.org/10.1038/s12276-021-00653-4.

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AbstractLoss-of-function variant in the gene encoding the KCNQ4 potassium channel causes autosomal dominant nonsyndromic hearing loss (DFNA2), and no effective pharmacotherapeutics have been developed to reverse channel activity impairment. Phosphatidylinositol 4,5-bisphosphate (PIP2), an obligatory phospholipid for maintaining KCNQ channel activity, confers differential pharmacological sensitivity of channels to KCNQ openers. Through whole-exome sequencing of DFNA2 families, we identified three novel KCNQ4 variants related to diverse auditory phenotypes in the proximal C-terminus (p.Arg331Gln

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41

Atwal, Karnail S., Gary J. Grover, Syed Z. Ahmed, et al. "Cardioselective anti-ischemic ATP-sensitive potassium channel openers." Journal of Medicinal Chemistry 36, no. 24 (1993): 3971–74. http://dx.doi.org/10.1021/jm00076a027.

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42

Challinor-Rogers, Joanne L., and Grant A. McPherson. "POTASSIUM CHANNEL OPENERS AND OTHER REGULATORS OF KATPCHANNELS." Clinical and Experimental Pharmacology and Physiology 21, no. 8 (1994): 583–97. http://dx.doi.org/10.1111/j.1440-1681.1994.tb02559.x.

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43

Lawson, Kim, and Mark J. Dunne. "Peripheral channelopathies as targets for potassium channel openers." Expert Opinion on Investigational Drugs 10, no. 7 (2001): 1345–59. http://dx.doi.org/10.1517/13543784.10.7.1345.

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44

Higgins, Gill. "Is there room for the potassium channel openers?" Inpharma Weekly &NA;, no. 858 (1992): 8–9. http://dx.doi.org/10.2165/00128413-199208580-00008.

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45

Weston, A. H. "Potassium channel openers: effects on the vascular system." Japanese Journal of Pharmacology 58 (1992): 232–37. http://dx.doi.org/10.1016/s0021-5198(19)59919-x.

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46

Edwards, G., and A. H. Weston. "Potassium channel openers and vascular smooth muscle relaxation." Pharmacology & Therapeutics 48, no. 2 (1990): 237–58. http://dx.doi.org/10.1016/0163-7258(90)90082-d.

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47

Garlid, Keith D., Petr Paucek, Vladimir Yarov-Yarovoy, Xiaocheng Sun, and Peter A. Schindler. "The Mitochondrial K Channel as a Receptor for Potassium Channel Openers." Journal of Biological Chemistry 271, no. 15 (1996): 8796–99. http://dx.doi.org/10.1074/jbc.271.15.8796.

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48

Lawson, Kim. "Potassium channel openers as potential therapeutic weapons in ion channel disease." Kidney International 57, no. 3 (2000): 838–45. http://dx.doi.org/10.1046/j.1523-1755.2000.00923.x.

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49

Liin, Sara I., Per-Eric Lund, Johan E. Larsson, Johan Brask, Björn Wallner, and Fredrik Elinder. "Biaryl sulfonamide motifs up- or down-regulate ion channel activity by activating voltage sensors." Journal of General Physiology 150, no. 8 (2018): 1215–30. http://dx.doi.org/10.1085/jgp.201711942.

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Voltage-gated ion channels are key molecules for the generation of cellular electrical excitability. Many pharmaceutical drugs target these channels by blocking their ion-conducting pore, but in many cases, channel-opening compounds would be more beneficial. Here, to search for new channel-opening compounds, we screen 18,000 compounds with high-throughput patch-clamp technology and find several potassium-channel openers that share a distinct biaryl-sulfonamide motif. Our data suggest that the negatively charged variants of these compounds bind to the top of the voltage-sensor domain, between t

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50

Manfroni, Giuseppe, Francesco Ragonese, Lorenzo Monarca, et al. "New Insights on KCa3.1 Channel Modulation." Current Pharmaceutical Design 26, no. 18 (2020): 2096–101. http://dx.doi.org/10.2174/1381612826666200316152645.

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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 propose

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