Mechanisms of the Antinociceptive Action of Gabapentin

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Gabapentin, a γ-aminobutyric acid (GABA) analogue anticonvulsant, is also an effective analgesic agent in neuropathic and inflammatory, but not acute, pain systemically and intrathecally. Other clinical indications such as anxiety, bipolar disorder, and hot flashes have also been proposed. Since gabapentin was developed, several hypotheses had been proposed for its action mechanisms. They include selectively activating the heterodimeric GABA<sub>B</sub> receptors consisting of GABA<sub>B1a</sub> and GABA<sub>B2</sub> subunits, selectively enhancing the NMDA current at GABAergic interneurons, or blocking AMPA-receptor-mediated transmission in the spinal cord, binding to the <sc><font size = "-2">L</font></sc>-α-amino acid transporter, activating ATP-sensitive K<sup>+</sup> channels, activating hyperpolarization-activated cation channels, and modulating Ca<sup>2+</sup> current by selectively binding to the specific binding site of [<sup>3</sup>H]gabapentin, the α<sub>2</sub>δ subunit of voltage-dependent Ca<sup>2+</sup> channels. Different mechanisms might be involved in different therapeutic actions of gabapentin. In this review, we summarized the recent progress in the findings proposed for the antinociceptive action mechanisms of gabapentin and suggest that the α<sub>2</sub>δ subunit of spinal N-type Ca<sup>2+</sup> channels is very likely the analgesic action target of gabapentin.<br>

収録刊行物

  • Journal of pharmacological sciences  

    Journal of pharmacological sciences 100(5), 471-486, 2006-05-15 

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10018239057
  • NII書誌ID(NCID)
    AA11806667
  • 本文言語コード
    ENG
  • 資料種別
    REV
  • ISSN
    13478613
  • NDL 記事登録ID
    7963241
  • NDL 雑誌分類
    ZS51(科学技術--薬学)
  • NDL 請求記号
    Z53-D199
  • データ提供元
    CJP書誌  CJP引用  NDL  J-STAGE 
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