ArticleBritish journal of pharmacology2014
Vasorelaxant effects of novel Kv 7.4 channel enhancers ML213 and NS15370.
Article in British journal of pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 40 citations in OpenAlex.
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- Cycling matters: Sex hormone regulation of vascular potassium channels.Channels (Austin, Tex.) · 2023Review
- Dual regulation of Kv7.2/7.3 channels by long-chain n-alcohols.The Journal of general physiology · 2023Article
- Marked oestrous cycle-dependent regulation of rat arterial KBritish journal of pharmacology · 2023Article
- Sexual dimorphism in prostacyclin-mimetic responses within rat mesenteric arteries: A novel role for KBritish journal of pharmacology · 2022Article
- Kv7 channel trafficking by the microtubule network in vascular smooth muscle.Acta physiologica (Oxford, England) · 2021Review
- Allisartan ameliorates vascular remodeling through regulation of voltage-gated potassium channels in hypertensive rats.BMC pharmacology & toxicology · 2021Article
- Chemical modulation of Kv7 potassium channels.RSC medicinal chemistry · 2021Review
- Activation of KCNQ4 as a Therapeutic Strategy to Treat Hearing Loss.International journal of molecular sciences · 2021Review
- Dynein regulates Kv7.4 channel trafficking from the cell membrane.The Journal of general physiology · 2021Article
- Nitric Oxide Signals Through IRAG to Inhibit TRPM4 Channels and Dilate Cerebral Arteries.Function (Oxford, England) · 2021Article
- SMIT (Sodium-Myo-Inositol Transporter) 1 Regulates Arterial Contractility Through the Modulation of Vascular Kv7 Channels.Arteriosclerosis, thrombosis, and vascular biology · 2020Article
- Acetaminophen (Paracetamol) Metabolites Induce Vasodilation and Hypotension by Activating Kv7 Potassium Channels Directly and Indirectly.Arteriosclerosis, thrombosis, and vascular biology · 2020Article
- KFrontiers in physiology · 2020Article
- Genome-wide association study identifies locus at chromosome 2q32.1 associated with syncope and collapse.Cardiovascular research · 2020Article
- KCNQ5 activation is a unifying molecular mechanism shared by genetically and culturally diverse botanical hypotensive folk medicines.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Impaired Kv7 channel function in cerebral arteries of a tauopathy mouse model (rTg4510).Physiological reports · 2018Article
- Angiotensin II Promotes KHypertension (Dallas, Tex. : 1979) · 2018Article
- 4-Aminopyridine: a pan voltage-gated potassium channel inhibitor that enhances KBritish journal of pharmacology · 2018Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
background and purposeThe KCNQ-encoded voltage-gated potassium channel family (Kv 7.1-Kv 7.5) are established regulators of smooth muscle contractility, where Kv 7.4 and Kv 7.5 predominate. Various Kv 7.2-7.5 channel enhancers have been developed that have been shown to cause a vasorelaxation in both rodent and human blood vessels. Recently, two novel Kv 7 channel enhancers have been identified, ML213 and NS15370, that show increased potency, particularly on Kv 7.4 channels. The aim of this study was to characterize the effects of these novel enhancers in different rat blood vessels and compare them with Kv 7 enhancers (S-1, BMS204352, retigabine) described previously. We also sought to determine the binding sites of the new Kv 7 enhancers. KEY
resultsBoth ML213 and NS15370 relaxed segments of rat thoracic aorta, renal artery and mesenteric artery in a concentration-dependent manner. In the mesenteric artery ML213 and NS15370 displayed EC50 s that were far lower than other Kv 7 enhancers tested. Current-clamp experiments revealed that both novel enhancers, at low concentrations, caused significant hyperpolarization in mesenteric artery smooth muscle cells. In addition, we determined that the stimulatory effect of these enhancers relied on a tryptophan residue located in the S5 domain, which is the same binding site for the other Kv 7 enhancers tested in this study. CONCLUSIONS AND IMPLICATIONS: This study has identified and characterized ML213 and NS15370 as potent vasorelaxants in different blood vessels, thereby highlighting these new compounds as potential therapeutics for various smooth muscle disorders.
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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.