ArticleActa pharmacologica Sinica2018
Enhancing inactivation rather than reducing activation of Nav1.7 channels by a clinically effective analgesic CNV1014802.
Article in Acta pharmacologica Sinica, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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Who cites it
11 citing papers in PubMed, 22 citations in OpenAlex.
- Review
- Sodium Channel Inhibitors in Clinical Development for Pain Management: A Focused Review.CNS drugs · 2026Review
- Discovery of E0199: A novel compound targeting both peripheral NaJournal of pharmaceutical analysis · 2025Article
- Sodium channels as a new target for pain treatment.Frontiers in pharmacology · 2025Review
- Advancements in Non-Addictive Analgesic Diterpenoid Alkaloid Lappaconitine: A Review.International journal of molecular sciences · 2024Review
- Small fibre neuropathy in Fabry disease: a human-derived neuronalBrain communications · 2024Article
- Naphthylisoquinoline alkaloids, a new structural template inhibitor of Nav1.7 sodium channel.Acta pharmacologica Sinica · 2023Article
- Neuropathic ocular surface pain: Emerging drug targets and therapeutic implications.Expert opinion on therapeutic targets · 2022Review
- Discovery of aryl sulfonamide-selective Nav1.7 inhibitors with a highly hydrophobic ethanoanthracene core.Acta pharmacologica Sinica · 2020Article
- Inhibitory effects of lappaconitine on the neuronal isoforms of voltage-gated sodium channels.Acta pharmacologica Sinica · 2019Article
- Review
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The Nav1.7 channel represents a promising target for pain relief. In the recent decades, a number of Nav1.7 channel inhibitors have been developed. According to the effects on channel kinetics, these inhibitors could be divided into two major classes: reducing activation or enhancing inactivation. To date, however, only several inhibitors have moved forward into phase 2 clinical trials and most of them display a less than ideal analgesic efficacy, thus intensifying the controversy regarding if an ideal candidate should preferentially affect the activation or inactivation state. In the present study, we investigated the action mechanisms of a recently clinically confirmed inhibitor CNV1014802 using both electrophysiology and site-directed mutagenesis. We found that CNV1014802 inhibited Nav1.7 channels through stabilizing a nonconductive inactivated state. When the cells expressing Nav1.7 channels were hold at 70 mV or 120 mV, the half maximal inhibitory concentration (IC
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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.