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Naloxone-induced analgesia: Involvement of κ-opiate receptors
Abstract
Rats treated with an acute high dose (30 mg/kg) or 4 days with a lower dose (5 mg/kg) of naloxone or naltrexone show an analgesic response at the hot-plate test. This paradoxical analgesic effect of the two mu-opiate receptor antagonists is blocked by the kappa opiate receptor antagonist MR 1452, and is modulated by the kappa opiate receptor agonist U 50-488. Our results suggest that kappa opiate receptors are involved in naloxone-induced analgesia and are consistent with a high degree of plasticity of the opiatergic system.
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“Surprisingly, however, the level of mechanical antinociception produced by orphine was higher in the presence of naloxone in the current experimental setup, potentially indicating the involvement of other (subtypes of) (opioid) receptors (Bianchi and Panerai, 1993; Hamann et al., 2008, 2004; Suarez-Roca and Maixner, 1993).”
From Elucidating the harm potential of brorphine analogues as new synthetic opioids: Synthesis, in vitro, and in vivo characterization (2024) · cites this paper as Bianchi and Panerai, 1993
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Vandeputte, M. M., Bilel, S., Tirri, M., Corli, G., Bassi, M., Layle, N. K., Fantinati, A., Walther, D., Iula, D. M., Baumann, M. H., et al. (2024) · Neuropharmacology · doi:10.1016/j.neuropharm.2024.110113 · Cited by 19
Metadata
- Authors
- Bianchi, M., & Panerai, A. E.
- Affiliations
- University of Milan (IT)
- Corresponding author
- Panerai, Alberto E.
- ORCID
- Panerai, Alberto E.
- Venue
- Pharmacology Biochemistry and Behavior
- Publisher
- Elsevier BV
- Published
- 1993-09
- Volume
- 46
- Issue
- 1
- Pages
- 145-148
- ISSN
- 0091-3057 (ISSN-L)
- OpenAlex
- W2095029167
- Cited by
- 21
- References
- 1
- Citations by year
- 2025: 1 · 2024: 3 · 2021: 1 · 2013: 1
- FWCI
- 0.36
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Pharmacology Biochemistry and Behavior (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Health Sciences › Medicine › Physiology (medical) › Pain Mechanisms and Treatments
- Health Sciences › Medicine › Anesthesiology and Pain Medicine › Pain Management and Opioid Use
- Keywords
- naloxone, naltrexone, kappa opioid receptor, U50,488, hot plate test, opioid analgesia
- MeSH terms
- Analgesia, Analgesics, Animals, Benzomorphans, Male, Naloxone, Naltrexone, Narcotic Antagonists, Pyrrolidines, Rats, Sprague-Dawley, Pain Threshold, Receptors, Opioid, mu, Receptors, Opioid, kappa, 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer, Rats
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