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The antinociceptive effect of intrathecal tramadol in rats: the role of alpha 2-adrenoceptors in the spinal cord

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Abstract

Purposes

The alpha 2 (α2)-adrenoceptor is highly important in the antinociception of tramadol administered systemically and intrathecally. However, it is unclear whether tramadol at the spinal level exerts an antinociceptive effect by directly binding with α2-adrenoceptors in the spinal cord. This study was conducted to investigate the relationship between α2-adrenoceptors and the antinociception of tramadol at the spinal level.

Methods

The rat formalin test was designed to determine whether the intrathecal α2-adrenoceptor antagonist yohimbine could reverse the antinociceptive effect of intrathecal tramadol. The binding affinity of tramadol for α2-adrenoceptors in the spinal cord was determined by radioligand binding assay using the labeled α2-adrenoceptor antagonist [3H]-yohimbine.

Results

The nociceptive test showed that intrathecal tramadol induced significant antinociception whereas pretreatment with intrathecal yohimbine partially reversed this antinociception. Scatchard analysis of the binding data showed [3H]-yohimbine had high affinity (K d = 1.79 nM) for the α2-adrenoceptor in the rat spinal cord, and that tramadol inhibited specific binding of [3H]-yohimbine with the spinal cord membranes with a high affinity constant (K i = 34.14 μM) and an IC50 of 68.25 μM, which indicated that tramadol was much less potent than [3H]-yohimbine at binding with α2-adrenoceptors of the spinal cord.

Conclusion

The results suggested that, with very weak binding affinity for α2-adrenoceptors, the antinociception of intrathecal tramadol is partially related to α2-adrenoceptors, and its intrathecal antinociception may mainly involve its indirect activation of α2-adrenoceptors in the spinal cord.

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Acknowledgments

This study was partly supported by “The Fundamental Research Funds for the Central Universities”.

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Authors and Affiliations

  1. Department of Anesthesiology, The First Affiliated Hospital, Sun Yat-sen University, No. 58 Zhongshan 2nd road, 510080, Guangzhou, China

    Cai Li, Bing-Xue Chen, Wen-Qi Huang & Ke-Xuan Liu

  2. Department of Gynecology and Obstetrics, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, China

    Shu-Qin Chen

Authors
  1. Cai Li
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  2. Shu-Qin Chen
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  3. Bing-Xue Chen
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  4. Wen-Qi Huang
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  5. Ke-Xuan Liu
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Corresponding author

Correspondence to Ke-Xuan Liu.

Additional information

C. Li and S.-Q. Chen contributed equally to this work.

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Li, C., Chen, SQ., Chen, BX. et al. The antinociceptive effect of intrathecal tramadol in rats: the role of alpha 2-adrenoceptors in the spinal cord. J Anesth 26, 230–235 (2012). https://doi.org/10.1007/s00540-011-1267-4

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  • DOI: https://doi.org/10.1007/s00540-011-1267-4

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