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Yohimbine both increases and decreases nociceptive thresholds in rats: Evaluation of the dose-response relationship

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Summary

The effect of yohimbine on a response to nociceptive stimulation mediated by supraspinal structures was studied after subcutaneous administration in doses from 0.25 mg/kg up to 25 mg/kg. The results showed that to describe adequately the dose-response relationship of yohimbine in pain modulation, characteristics of opposing effects had to be considered: low doses with an ED50-value of 0.56 mg/kg were found to dose-dependently facilitate nociception whereas high doses instead induced antinociception with an ED50 of 4.74 mg/kg. The possible capacity of α2-adrenoceptors to modulate responses to nociception is discussed.

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Authors and Affiliations

  1. Department of Pharmacology, Central Research and Control Laboratory of the National Corporation of Swedish Pharmacies, Apoteksbolaget AB, Box 3045, S-171 03, Solna, Sweden

    Gudrun H. M. Paalzow

  2. Department of Biopharmaceutics and Pharmacokinetics, University of Uppsala, Box 580, S-751 23, Uppsala, Sweden

    Lennart K. Paalzow

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  1. Gudrun H. M. Paalzow
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  2. Lennart K. Paalzow
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Paalzow, G.H.M., Paalzow, L.K. Yohimbine both increases and decreases nociceptive thresholds in rats: Evaluation of the dose-response relationship. Naunyn-Schmiedeberg's Arch. Pharmacol. 322, 193–197 (1983). https://doi.org/10.1007/BF00500764

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  • DOI: https://doi.org/10.1007/BF00500764

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