Abstract:
BACKGROUND: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.
journal_name
Anesth Analgjournal_title
Anesthesia and analgesiaauthors
Tomić MA,Pecikoza UB,Micov AM,Stepanović-Petrović RMdoi
10.1213/ANE.0000000000000953subject
Has Abstractpub_date
2015-12-01 00:00:00pages
1632-9issue
6eissn
0003-2999issn
1526-7598journal_volume
121pub_type
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journal_title:Anesthesia and analgesia
pub_type: 杂志文章
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:
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journal_title:Anesthesia and analgesia
pub_type: 杂志文章
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journal_title:Anesthesia and analgesia
pub_type: 杂志文章
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journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章,随机对照试验
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pub_type: 杂志文章,meta分析,评审
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更新日期:2018-01-01 00:00:00
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journal_title:Anesthesia and analgesia
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journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章,随机对照试验
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