ArticleCNS neuroscience & therapeutics2016
NS383 Selectively Inhibits Acid-Sensing Ion Channels Containing 1a and 3 Subunits to Reverse Inflammatory and Neuropathic Hyperalgesia in Rats.
Article in CNS neuroscience & therapeutics, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 27 citations in OpenAlex.
- Acid-sensing ion channels and their role in controlling pain in the post-operative stage.International journal of physiology, pathophysiology and pharmacology · 2026Review
- Tricyclic Isatin Derivatives as Anti-Inflammatory Compounds with High Kinase Binding Affinity.Molecules (Basel, Switzerland) · 2025Article
- The role of acid-sensing ion channels in monosodium urate-induced gouty pain in mice.Pflugers Archiv : European journal of physiology · 2024Article
- TASK inhibition by mild acidosis increases CaAmerican journal of physiology. Lung cellular and molecular physiology · 2023Article
- Inhibition of P2X7 receptors by Lu AF27139 diminishes colonic hypersensitivity and CNS prostanoid levels in a rat model of visceral pain.Purinergic signalling · 2022Article
- Acid-Sensing Ion Channels in Glial Cells.Membranes · 2022Review
- Acid-sensing ion channel 3: An analgesic target.Channels (Austin, Tex.) · 2021Review
- Oximes: Novel Therapeutics with Anticancer and Anti-Inflammatory Potential.Biomolecules · 2021Review
- The Role of ASIC1a in Epilepsy: A Potential Therapeutic Target.Current neuropharmacology · 2021Review
- Neurodegenerative Disease: What Potential Therapeutic Role of Acid-Sensing Ion Channels?Frontiers in cellular neuroscience · 2021Review
- Systematic Review of Systemic and Neuraxial Effects of Acetaminophen in Preclinical Models of Nociceptive Processing.Journal of pain research · 2021Review
- Pharmacological characterization of a novel, potent, selective, and orally active fatty acid amide hydrolase inhibitor, PKM-833 [(R)-N-(pyridazin-3-yl)-4-(7-(trifluoromethyl)chroman-4-yl)piperazine-1-carboxamide] in rats: Potential for the treatment of inflammatory pain.Pharmacology research & perspectives · 2020Article
- Animal, Herb, and Microbial Toxins for Structural and Pharmacological Study of Acid-Sensing Ion Channels.Frontiers in pharmacology · 2020Review
- Spider venom peptides as potential drug candidates due to their anticancer and antinociceptive activities.The journal of venomous animals and toxins including tropical diseases · 2019Review
- Acid-Sensing Ion Channels as Potential Therapeutic Targets in Neurodegeneration and Neuroinflammation.Mediators of inflammation · 2017Review
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsHere, we investigate the pharmacology of NS383, a novel small molecule inhibitor of acid-sensing ion channels (ASICs).
methodsASIC inhibition by NS383 was characterized in patch-clamp electrophysiological studies. Analgesic properties were evaluated in four rat behavioral models of pain.
resultsNS383 inhibited H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. However, NS383 was completely inactive at homomeric ASIC2a. Heteromeric receptors containing AISC2a, such as ASIC1a+2a and ASIC2a+3, were only partially inhibited, presumably as a result of stoichiometry-dependent binding. NS383 (10-60 mg/kg, i.p.), amiloride (50-200 mg/kg, i.p.), acetaminophen (100-400 mg/kg, i.p.), and morphine (3-10 mg/kg, i.p.) all dose-dependently attenuated nocifensive behaviors in the rat formalin test, reversed pathological inflammatory hyperalgesia in complete Freund's adjuvant-inflamed rats, and reversed mechanical hypersensitivity in the chronic constriction injury model of neuropathic pain. However, in contrast to acetaminophen and morphine, motor function was unaffected by NS383 at doses at least 8-fold greater than those that were effective in pain models, whilst analgesic doses of amiloride were deemed to be toxic.
conclusionsNS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. It is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits.
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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.