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The Efficacy of Eslicarbazepine Acetate in Models of Trigeminal, Neuropathic, and Visceral Pain: The Involvement of 5-HT1B/1D Serotonergic and CB1/CB2 Cannabinoid Receptors.

AbstractBACKGROUND:
Many clinical pain states that are difficult to treat share a common feature of sensitization of nociceptive pathways. Drugs that could normalize hyperexcitable neural activity (e.g., antiepileptic drugs) may be useful in relieving these pain states. Eslicarbazepine acetate (ESL) is a novel antiepileptic drug derived from carbamazepine/oxcarbazepine with a more favorable metabolic profile and potentially better tolerability. We examined the efficacy of ESL in models of inflammatory and neuropathic pain and the potential mechanism involved in its action.
METHODS:
The antinociceptive effects of ESL were assessed in mice models of trigeminal (orofacial formalin test), neuropathic (streptozotocin-induced diabetic neuropathy model), and visceral pain (writhing test). The influence of 5-HT1B/1D serotonin receptor (GR 127935) and CB1 (AM251) and CB2 cannabinoid receptor (AM630) antagonists on the antinociceptive effect of ESL was tested in the model of trigeminal pain.
RESULTS:
ESL exhibited significant and dose-dependent antinociceptive effects in the second phase of the orofacial formalin test (P ≤ 0.011), in the tail-flick test in diabetic mice (P ≤ 0.013), and in the writhing test (P ≤ 0.003). GR 127935 (P ≤ 0.038) and AM251 and AM630 (P ≤ 0.013 for both antagonists) significantly inhibited the antinociceptive effect of ESL in a dose-related manner.
CONCLUSIONS:
ESL exhibited efficacy in models of trigeminal, neuropathic, and visceral pain. In the trigeminal pain model, the antinociceptive effect of ESL is, at least in part, mediated by 5-HT1B/1D serotonin and CB1/CB2 cannabinoid receptors. This study indicates that ESL could be useful in the clinical treatment of inflammatory and neuropathic pain.
AuthorsMaja A Tomić, Uroš B Pecikoza, Ana M Micov, Radica M Stepanović-Petrović
JournalAnesthesia and analgesia (Anesth Analg) Vol. 121 Issue 6 Pg. 1632-9 (Dec 2015) ISSN: 1526-7598 [Electronic] United States
PMID26465930 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Dibenzazepines
  • Receptor, Cannabinoid, CB1
  • Receptor, Cannabinoid, CB2
  • Receptor, Serotonin, 5-HT1B
  • Receptor, Serotonin, 5-HT1D
  • eslicarbazepine acetate
Topics
  • Animals
  • Diabetic Neuropathies (drug therapy, pathology)
  • Dibenzazepines (pharmacology, therapeutic use)
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Pain Measurement (drug effects, methods)
  • Receptor, Cannabinoid, CB1 (physiology)
  • Receptor, Cannabinoid, CB2 (physiology)
  • Receptor, Serotonin, 5-HT1B (physiology)
  • Receptor, Serotonin, 5-HT1D (physiology)
  • Treatment Outcome
  • Trigeminal Nerve Diseases (drug therapy, pathology)
  • Visceral Pain (drug therapy, pathology)

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