ArticleNaunyn-Schmiedeberg's archives of pharmacology2004
Functional characterization of large conductance calcium-activated K+ channel openers in bladder and vascular smooth muscle.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
What it found
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Who cites it
26 citing papers in PubMed, 50 citations in OpenAlex.
- BK Channels Orchestrate Cardiac Homeostasis Through Mitochondrial Uncoupling Proteins.bioRxiv : the preprint server for biology · 2026Article
- Differential effects of TRPM4 channel inhibitors on Guinea pig urinary bladder smooth muscle excitability and contractility: Novel 4-chloro-2-[2-(2-chloro-phenoxy)-acetylamino]-benzoic acid (CBA) versus classical 9-phenanthrol.Pharmacology research & perspectives · 2022Article
- Urinary bladder smooth muscle ion channels: expression, function, and regulation in health and disease.American journal of physiology. Renal physiology · 2020Review
- Central role of the BK channel in urinary bladder smooth muscle physiology and pathophysiology.American journal of physiology. Regulatory, integrative and comparative physiology · 2014Review
- NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions.The Journal of pharmacology and experimental therapeutics · 2014Article
- BK channel activators and their therapeutic perspectives.Frontiers in physiology · 2014Review
- Single-channel biophysical and pharmacological characterizations of native human large-conductance calcium-activated potassium channels in freshly isolated detrusor smooth muscle cells.Pflugers Archiv : European journal of physiology · 2013Article
- Ca2+ -activated K+ channel (KCa) stimulation improves relaxant capacity of PDE5 inhibitors in human penile arteries and recovers the reduced efficacy of PDE5 inhibition in diabetic erectile dysfunction.British journal of pharmacology · 2013Article
- SK channel-selective opening by SKA-31 induces hyperpolarization and decreases contractility in human urinary bladder smooth muscle.American journal of physiology. Regulatory, integrative and comparative physiology · 2013Article
- Suppression of human detrusor smooth muscle excitability and contractility via pharmacological activation of large conductance Ca2+-activated K+ channels.American journal of physiology. Cell physiology · 2012Article
- Do β3-adrenergic receptors play a role in guinea pig detrusor smooth muscle excitability and contractility?American journal of physiology. Renal physiology · 2012Article
- Role of potassium ion channels in detrusor smooth muscle function and dysfunction.Nature reviews. Urology · 2011Review
- Large conductance Ca2+ -activated K+ channel activation with NS1619 decreases myogenic and neurogenic contractions of rat detrusor smooth muscle.European journal of pharmacology · 2011Article
- Large-conductance voltage- and Ca2+-activated K+ channels regulate human detrusor smooth muscle function.American journal of physiology. Cell physiology · 2011Article
- On benzofuroindole analogues as smooth muscle relaxants.Journal of biomedicine & biotechnology · 2011Review
- Effects of bladder outlet obstruction on properties of Ca2+-activated K+ channels in rat bladder.American journal of physiology. Regulatory, integrative and comparative physiology · 2010Article
- BK channel activation by NS11021 decreases excitability and contractility of urinary bladder smooth muscle.American journal of physiology. Regulatory, integrative and comparative physiology · 2010Article
- Intracellular Na(+) modulates large conductance Ca(2+)-activated K (+) currents in human umbilical vein endothelial cells.Pflugers Archiv : European journal of physiology · 2008Article
- Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and beta-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2008Review
- Small-conductance, Ca(2+) -activated K+ channel 2 is the key functional component of SK channels in mouse urinary bladder.American journal of physiology. Regulatory, integrative and comparative physiology · 2008Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Calcium activated K(+) channels (K(Ca) channels) are found in a variety of smooth muscle tissues, the most characterized of which are the large conductance K(Ca) channels (BK(Ca) or maxi-K(+) channels). Recent medicinal chemistry efforts have identified novel BK(Ca) openers including 2-amino-5-(2-fluoro-phenyl)-4-methyl-1H-pyrrole-3-carbonitrile (NS-8), BMS-204352 and its analog 3-(5-chloro-2-hydroxy-phenyl)-3-hydroxy-6-trifluoromethyl-1,3-dihydro-indol-2-one (compound 1), and 5,7-dichloro-4-(5-chloro-2-hydroxy-phenyl)-3-hydroxy-1H-quinolin-2-one (compound 2). Although these compounds are effective BK(Ca) openers as shown by electrophysiological methods, little is known about their effects on smooth muscle contractility. In this study, the responsiveness of structurally diverse BK(Ca) openers-NS-8, compounds 1 and 2 and the well characterized nonselective NS-1619-was assessed using segments of endothelium denuded rat aorta, rat and guinea pig detrusor precontracted with extracellular K(+), and Landrace pig detrusor stimulated by electrical field. In all preparations, the compounds tested inhibited or completely abolished contractions with similar potencies (-logIC(50) values: 3.8 to 5.1). In rat aorta, in the presence of 80 mM K(+), the compounds significantly shifted the concentration-response curve to the right compared with those obtained in 30 mM K(+). These data are consistent with K(+) channel (BK(Ca) channel) activation as the underlying mechanism of relaxation by compounds that share the electrophysiological property of BK(Ca) current activation. The similar potencies at detrusor and vascular smooth muscle suggest that the achievement of smooth muscle selectivity in vitro with the representative compounds examined in this study may prove to be a challenge when targeting BK(Ca) channels for smooth muscle indications such as overactive bladder.
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