Augmentation of opioid induced antinociception by the atypical antipsychotic drug risperidone in mice

Shaul Schreiber, Maria M. Backer, Ronit Weizman, Chaim G. Pick*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

33 Scopus citations

Abstract

Risperidone is a novel atypical neuroleptic with a favorable profile of side effects due to its unique pharmacological activity: it exhibits both potent dopamine D2 and 5-HT2 receptor blocking activity, as well as high affinity for α1 and α2 adrenergic receptors and histamine H1 receptor. We found that risperidone has a potent antinociceptive effect in the tailflick assay with an ED50 of 26.4 mg/kg. This effect of risperidone was antagonized by naloxone (P < 0.05). This sensitivity to naloxone indicates that at least some of the analgesic effects of risperidone are mediated by an opioid mechanism of action. β-FNA (μ1 μ2-antagonist), naloxonazine (α1-antagonist) and norbinaltorphamine (nor-BNI; K1-analgesia) reversed risperidone antinociceptive effect (P < 0.05). Naltrindole (δ-antagonist) only partially reversed risperidone antinociceptive effect. We found that the sensitivity of risperidone antinociceptive effect to selective antagonists implies involvement of μ1-, μ2- and K1-opioid and to a lesser extent δ- opioid mechanisms. These results suggest a possible role for risperidone both in the management of pain and in the management of opiate withdrawal and detoxification.

Original languageEnglish
Pages (from-to)25-28
Number of pages4
JournalNeuroscience Letters
Volume228
Issue number1
DOIs
StatePublished - 30 May 1997

Funding

FundersFunder number
Biology Research Center
Eisen Foundation Center
Tel Aviv University

    Keywords

    • Antinociception
    • Atypical neuroleptics
    • Opioid receptor sub- types
    • Risperidone

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