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Journal of Anesthesia

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01-04-2012 | Original Article

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

Authors: Cai Li, Shu-Qin Chen, Bing-Xue Chen, Wen-Qi Huang, Ke-Xuan Liu

Published in: Journal of Anesthesia | Issue 2/2012

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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Title: The antinociceptive effect of intrathecal tramadol in rats: the role of alpha 2-adrenoceptors in the spinal cord
Authors: Cai Li
Shu-Qin Chen
Bing-Xue Chen
Wen-Qi Huang
Ke-Xuan Liu
Publication date: 01-04-2012
Publisher: Springer Japan
Published in: Journal of Anesthesia / Issue 2/2012
Print ISSN: 0913-8668
Electronic ISSN: 1438-8359
DOI: https://doi.org/10.1007/s00540-011-1267-4

2024 ASCO Annual Meeting

Springer Medicine

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

Abstract

Purposes

Methods

Results

Conclusion

2024 ASCO Annual Meeting

Springer Medicine

Abstract

Purposes

Methods

Results

Conclusion

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