ArticleJournal of anesthesia2011
Dexmedetomidine and clonidine inhibit the function of Na(v)1.7 independent of α(2)-adrenoceptor in adrenal chromaffin cells.
Article in Journal of anesthesia, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 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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Who cites it
13 citing papers in PubMed, 1 synthesis or guideline pooled it, 24 citations in OpenAlex.
- Dexmedetomidine as an adjuvant to local anesthetics in brachial plexus blocks: A meta-analysis of randomized controlled trials.Medicine · 2017Pooled it
- Effects of Dexmedetomidine on Postoperative Quality of Recovery and Electroencephalogram in Elderly Patients Undergoing Total Knee Arthroplasty: A Randomized Clinical Trial.Drug design, development and therapy · 2025Trial
- Trial
- Clonidine Inhibits Interictal-like Epileptiform Events in Prefrontal Cortex Pyramidal Neurons.International journal of molecular sciences · 2026Article
- Dexmedetomidine attenuates inflammation and organ injury partially by upregulating Nur77 in sepsis.Immunity, inflammation and disease · 2023Article
- Guanfacine inhibits interictal epileptiform events and sodium currents in prefrontal cortex pyramidal neurons.Pharmacological reports : PR · 2023Article
- Phenotypic drug screen uncovers the metabolic GCH1/BH4 pathway as key regulator of EGFR/KRAS-mediated neuropathic pain and lung cancer.Science translational medicine · 2022Article
- [Analgesic effect of dexmedetomidine on oxaliplatin-induced neuropathic pain in rats].Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2018Article
- Dexmedetomidine Inhibits Voltage-Gated Sodium Channels viaMediators of inflammation · 2018Article
- Inhibition of the cardiac Na⁺ channel α-subunit Nav1.5 by propofol and dexmedetomidine.Naunyn-Schmiedeberg's archives of pharmacology · 2016Article
- The effect of pretreatment with clonidine on propofol consumption in opium abuser and non-abuser patients undergoing elective leg surgery.Journal of research in medical sciences : the official journal of Isfahan University of Medical Sciences · 2012Article
- Clonidine: an old friend newly rediscovered.Anesthesiology and pain medicine · 2011Article
- Comparison of Local Wound Infiltration with Ropivacaine Alone or Ropivacaine Plus Dexmedetomidine for Postoperative Pain Relief after Lower Segment Cesarean Section.Anesthesia, essays and researchesArticle
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeBesides being administered systemically for sedation and analgesia, α(2)-agonists such as dexmedetomidine and clonidine have been administered with intrathecal, epidural, or perineural injections, leading to an antinociceptive effect at the spinal cord or peripheral nerve level. However, the mechanism for this remains unclear. In the present study, we examined whether dexmedetomidine and clonidine could inhibit the function of tetrodotoxin-sensitive Na(+) channels, which play important roles in the generation of pain.
methodsCultured bovine adrenal chromaffin cells expressing the tetrodotoxin-sensitive Na(v)1.7 Na(+) channel isoform were incubated in KRP buffer containing 2 μCi (22)NaCl for 5 min without or with dexmedetomidine or clonidine in the absence or presence of veratridine, α-scorpion venom, β-scorpion venom, Ptychodiscus brevis toxin-3 or ouabain. Cells were then washed and counted radioactively.
resultsDexmedetomidine and clonidine reduced veratridine-induced (22)Na(+) influx via Na(v)1.7 in a concentration-dependent manner (EC(50) = 50 μM and 530 μM), even in the presence of ouabain, an inhibitor of Na(+), K(+)-ATPase. Dexmedetomidine and clonidine shifted the concentration-response curve of veratridine for (22)Na(+) influx downward without altering the EC(50) of veratridine. Atipamezole and yohimbine, α(2)-antagonists, did not prevent the inhibition of veratridine-induced (22)Na(+) influx by dexmedetomidine. Dexmedetomidine and clonidine combined with lidocaine induced more inhibition of veratridine-induced (22)Na(+) influx than each drug did individually. Atipamezole and yohimbine did not prevent the lidocaine-enhancing effect of dexmedetomidine and clonidine.
conclusionDexmedetomidine and clonidine inhibit the function of Na(v)1.7 independent of α(2)-adrenoceptor. These results may lead to a deeper understanding of the peripheral antinociceptive effects of α (2)-agonists.
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