ArticleBritish journal of pharmacology2009
NS11021, a novel opener of large-conductance Ca(2+)-activated K(+) channels, enhances erectile responses in rats.
Article in British journal of pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers, 1 of them a synthesis that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 1 synthesis or guideline pooled it, 54 citations in OpenAlex.
- Pooled it
- Phytochemical-based nanomedicine as a promising therapeutic strategy for erectile dysfunction.Asian journal of andrology · 2026Review
- Cadmium chloride and erectile dysfunction: integrative evidence from network toxicology, Mendelian randomization, andFrontiers in endocrinology · 2026Article
- Small Molecule NS11021 Promotes BK Channel Activation by Increasing Inner Pore Hydration.Journal of chemical information and modeling · 2024Article
- Large conductance voltage-and calcium-activated KFrontiers in pharmacology · 2024Review
- Identification of the Large-Conductance CaMolecules (Basel, Switzerland) · 2021Article
- Novel Emerging Therapies for Erectile Dysfunction.The world journal of men's health · 2021Review
- Calcium-Activated KHandbook of experimental pharmacology · 2021Article
- The Large-Conductance, Calcium-Activated Potassium Channel: A Big Key Regulator of Cell Physiology.Frontiers in physiology · 2021Review
- Molecular mechanism of BK channel activation by the smooth muscle relaxant NS11021.The Journal of general physiology · 2020Article
- The action of a BK channel opener.The Journal of general physiology · 2020Article
- Ionic Channels as Potential Therapeutic Targets for Erectile Dysfunction: A Review.Frontiers in pharmacology · 2020Review
- Specific BK Channel Activator NS11021 Protects Rat Renal Proximal Tubular Cells from Cold Storage-Induced Mitochondrial Injury In Vitro.Biomolecules · 2019Article
- The absence of NIPA2 enhances neural excitability through BK (big potassium) channels.CNS neuroscience & therapeutics · 2019Article
- Novel selective PDE type 1 inhibitors cause vasodilatation and lower blood pressure in rats.British journal of pharmacology · 2017Article
- Down-regulation of KScientific reports · 2017Article
- Small and Intermediate Calcium-Activated Potassium Channel Openers Improve Rat Endothelial and Erectile Function.Frontiers in pharmacology · 2017Article
- Molecular and functional characterization of Kv 7 channels in penile arteries and corpus cavernosum of healthy and metabolic syndrome rats.British journal of pharmacology · 2016Article
- Involvement of transglutaminase 2 and voltage-gated potassium channels in cystamine vasodilatation in rat mesenteric small arteries.British journal of pharmacology · 2016Article
- BK channel activators and their therapeutic perspectives.Frontiers in physiology · 2014Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeLarge-conductance Ca(2+)-activated K(+) channels (BK(Ca)), located on the arterial and corporal smooth muscle, are potential targets for treatment of erectile dysfunction (ED). This study investigated whether NS11021 (1-(3,5-Bis-trifluoromethyl-phenyl)-3-[4-bromo-2-(1H-tetrazol-5-yl)-phenyl]-thiourea), a novel opener of BK(Ca) channels, relaxes erectile tissue in vitro and enhances erectile responses in intact rats. The effects were compared with sildenafil, an inhibitor of phosphodiesterase type 5. EXPERIMENTAL APPROACH: Patch clamp was used to record whole cell current in rat isolated corpus cavernosum smooth muscle cells (SMCs) and human umbilical vein endothelial cells (HUVECs). Isometric tension was measured in intracavernous arterial rings and corpus cavernosum strips isolated from rats and men, and simultaneous measurements of intracellular Ca(2+) concentration ([Ca(2+)](i)) and tension were performed in intracavernous arteries. Erectile response was measured in anaesthetized rats. KEY
resultsIn patch clamp recordings, NS11021 increased currents sensitive to the selective BK(Ca) channel blocker, iberiotoxin (IbTX) in SMCs, but did not modulate K(+) current in HUVECs. NS11021 reduced [Ca(2+)](i) and tension in penile arteries. IbTX inhibited the vasorelaxation induced by NS11021 and sildenafil in human erectile tissue. NS11021 and sildenafil but not vehicle increased erectile responses in anaesthetized rats, an effect which was abolished after pretreatment with tetraethylammonium. CONCLUSIONS AND IMPLICATIONS: NS11021 leads to relaxation of both intracavernous arteries and corpus cavernosum strips primarily through opening of BK(Ca) channels. It is also effective in facilitating erectile responses in anaesthetized rats. These results suggest a potential for use of BK(Ca) openers in the treatment of ED.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.