ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2015
Actions of bupivacaine, a widely used local anesthetic, on NMDA receptor responses.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 68 citations in OpenAlex.
- Intraperitoneal ketamine versus bupivacaine for postoperative pain control after laparoscopic cholecystectomy - a double-blind randomized controlled trial.BMC anesthesiology · 2025Trial
- Posterior scalp block with bupivacaine and dexmedetomidine for pain management in posterior fossa surgeries: a prospective, double blind randomized controlled trial.Pain management · 2025Trial
- Molecular Mechanisms of Local Anesthetic Toxicity: From Ion Channel Dysregulation to Mitochondrial Dysfunction and Tissue-Specific Injury.International journal of molecular sciences · 2026Review
- Structural determinants for GPCR-mediated inhibition of TASK K2P channels by diacylglycerol and its dysfunction in disease.The EMBO journal · 2026Article
- Targeting NaInternational journal of molecular sciences · 2026Review
- Article
- Baricity of spinal bupivacaine and the incidence of hypotension in non-obstetric surgery: A systematic review.European journal of anaesthesiology and intensive care · 2025Review
- The Effects of Synthetic Polymers on the Release Patterns of Bupivacaine Hydrochloride from Sodium Hyaluronate Hydrogels.Biomedicines · 2024Article
- Article
- Fusing multiplex heterogeneous networks using graph attention-aware fusion networks.Scientific reports · 2024Article
- The Stable Gastric Pentadecapeptide BPC 157 Pleiotropic Beneficial Activity and Its Possible Relations with Neurotransmitter Activity.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Bedside greater occipital nerve block with bupivacaine for the treatment of recalcitrant scalp pruritus.JAAD case reports · 2024Article
- Simultaneous determination of meloxicam and bupivacaine via a novel modified dual wavelength method and an advanced chemometric approach.Scientific reports · 2024Article
- Anti-Adhesive Resorbable Indomethacin/Bupivacaine-Eluting Nanofibers for Tendon Rupture Repair: In Vitro and In Vivo Studies.International journal of molecular sciences · 2023Article
- The Effect of Intrathecal Bupivacaine Plus Dextrose 5% and Fentanyl Compared with Bupivacaine Alone on the Onset and Duration of Analgesia in Patients Undergoing Lower-Limb Orthopedic Surgery.Advances in orthopedics · 2023Article
- Effects of Hyperbaric and Isobaric Bupivacaine on Hemodynamic Profiles and Block Characteristics Among Parturients Undergoing Elective Cesarean Section Under Spinal Anesthesia: A Randomized Controlled Trial.Journal of pain research · 2023Article
- Article
- Liposomal bupivacaine does not decrease postoperative opioid use or length of hospital stay in patients undergoing anterior cervical discectomy and fusion.Journal of spine surgery (Hong Kong) · 2022Article
- Inhibition of NMDA receptors through a membrane-to-channel path.Nature communications · 2022Article
- Bupivacaine reduces GlyT1 expression by potentiating the p-AMPKα/BDNF signalling pathway in spinal astrocytes of rats.Scientific reports · 2022Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
NMDA receptors mediate excitatory neurotransmission in brain and spinal cord and play a pivotal role in the neurological disease state of chronic pain, which is caused by central sensitization. Bupivacaine is the indicated local anesthetic in caudal, epidural, and spinal anesthesia and is widely used clinically to manage acute and chronic pain. In addition to blocking Na(+) channels, bupivacaine affects the activity of many other channels, including NMDA receptors. Importantly, bupivacaine inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization. We used recombinant NMDA receptors expressed in HEK293 cells and found that increasing concentrations of bupivacaine decreased channel open probability in GluN2 subunit- and pH-independent manner by increasing the mean duration of closures and decreasing the mean duration of openings. Using kinetic modeling of one-channel currents, we attributed the observed current decrease to two main mechanisms: a voltage-dependent "foot-in-the-door" pore block and an allosteric gating effect. Further, the inhibition was state-independent because it occurred to the same degree whether the drug was applied before or after glutamate stimulation and was mediated by extracellular and intracellular inhibitory sites, via hydrophilic and hydrophobic pathways. These results predict that clinical doses of bupivacaine would decrease the peak and accelerate the decay of synaptic NMDA receptor currents during normal synaptic transmission. These quantitative predictions inform possible applications of bupivacaine as preventative and therapeutic approaches in chronic pain.
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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.