ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2015
Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude.
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 16 papers.
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Who cites it
16 citing papers in PubMed, 23 citations in OpenAlex.
- Cardiorespiratory failure and sudden death induced by carfentanil exposure: Involvement of central mu1 opioid receptors.Toxicology and applied pharmacology · 2025Article
- Roles of peripheral and central µAmerican journal of physiology. Lung cellular and molecular physiology · 2025Article
- Opioid system and related ligands: from the past to future perspectives.Journal of anesthesia, analgesia and critical care · 2024Review
- HDAC6 Inhibition Reverses Cisplatin-Induced Mechanical Hypersensitivity via Tonic Delta Opioid Receptor Signaling.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2022Article
- Kappa opioids inhibit the GABA/glycine terminals of rostral ventromedial medulla projections in the superficial dorsal horn of the spinal cord.The Journal of physiology · 2022Article
- Fentanyl-induced hyperalgesia and analgesic tolerance in male rats: common underlying mechanisms and prevention by a polyamine deficient diet.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Article
- Lipid bound extended release buprenorphine (high and low doses) and sustained release buprenorphine effectively attenuate post-operative hypersensitivity in an incisional pain model in mice (Animal models and experimental medicine · 2021Article
- Buprenorphine alters microglia and astrocytes acutely following diffuse traumatic brain injury.Scientific reports · 2021Article
- A Narrative Pharmacological Review of Buprenorphine: A Unique Opioid for the Treatment of Chronic Pain.Pain and therapy · 2020Review
- Use of Flavored Tablets of Gabapentin and Carprofen to Attenuate Postoperative Hypersensitivity in an Incisional Pain Model in Rats (Journal of the American Association for Laboratory Animal Science : JAALAS · 2020Article
- Opioid Receptors in Immune and Glial Cells-Implications for Pain Control.Frontiers in immunology · 2020Review
- Treating Chronic Pain: An Overview of Clinical Studies Centered on the Buprenorphine Option.Drugs · 2018Review
- Prevention and reversal of latent sensitization of dorsal horn neurons by glial blockers in a model of low back pain in male rats.Journal of neurophysiology · 2017Article
- Morphine-induced hyperalgesia involves mu opioid receptors and the metabolite morphine-3-glucuronide.Scientific reports · 2017Article
- The developmental emergence of differential brainstem serotonergic control of the sensory spinal cord.Scientific reports · 2017Article
- Use of Liposomal Bupivacaine for Postoperative Analgesia in an Incisional Pain Model in Rats (Journal of the American Association for Laboratory Animal Science : JAALAS · 2017Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Due to its distinct pharmacological profile and lower incidence of adverse events compared with other opioids, buprenorphine is considered a safe option for pain and substitution therapy. However, despite its wide clinical use, little is known about the synaptic effects of buprenorphine in nociceptive pathways. Here, we demonstrate dose-dependent, bimodal effects of buprenorphine on transmission at C-fiber synapses in rat spinal cord dorsal horn in vivo. At an analgesically active dose of 1500 μg·kg(-1), buprenorphine reduced the strength of spinal C-fiber synapses. This depression required activation of spinal opioid receptors, putatively μ1-opioid receptors, as indicated by its sensitivity to spinal naloxone and to the selective μ1-opioid receptor antagonist naloxonazine. In contrast, a 15,000-fold lower dose of buprenorphine (0.1 μg·kg(-1)), which caused thermal and mechanical hyperalgesia in behaving animals, induced an enhancement of transmission at spinal C-fiber synapses. The ultra-low-dose buprenorphine-induced synaptic facilitation was mediated by supraspinal naloxonazine-insensitive, but CTOP-sensitive μ-opioid receptors, descending serotonergic pathways, and activation of spinal glial cells. Selective inhibition of spinal 5-hydroxytryptamine-2 receptors (5-HT2Rs), putatively located on spinal astrocytes, abolished both the induction of synaptic facilitation and the hyperalgesia elicited by ultra-low-dose buprenorphine. Our study revealed that buprenorphine mediates its modulatory effects on transmission at spinal C-fiber synapses by dose dependently acting on distinct μ-opioid receptor subtypes located at different levels of the neuraxis.
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