Antinociceptive activity of N-(4-hydroxyphenacetyl)-4-aminoclonidine, a novel analog of clonidine: Role of opioid receptors and alpha-adrenoceptors

Martin D. Hynes*, Daphne Atlas, Robert R. Ruffolo

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

N-(4-hydroxyphenacetyl)-4-aminoclonidine, a derivative of the alpha-adrenoceptor agonist p-aminoclonidine, was found to exhibit dose-dependent antinociceptive activity in the mouse writhing assay. In this measure of antinociceptive activity it was less potent than clonidine or xylazine. Naloxone, an opioid receptor antagonist, at a dose sufficient to abolish the antinociceptive activity of morphine, did not affect the antinociceptive activity of N-(4-hydroxyphenacetyl)-4-aminoclonidine, clonidine or xylazine. In contrast, yohimbine, a alpha-adrenoceptor antagonist, reduced the antinociceptive activity of N-(4-hydroxyphenacetyl)-4-aminoclonidine, clonidine and xylazine, but not morphine. The affinity of N-(4-hydroxyphenacetyl)-4-aminoclonidine, clonidine and xylazine for alpha-adrenoceptors in rat aorta was correlated highly with the relative potency for writhing inhibition. These results suggest that the antinociceptive activity of N-(4-hydroxyphenacetyl)-4-aminoclonidine is mediated by alpha-adrenoceptors.

Original languageEnglish
Pages (from-to)879-882
Number of pages4
JournalPharmacology Biochemistry and Behavior
Volume19
Issue number5
DOIs
StatePublished - Nov 1983

Keywords

  • Alpha-adrenoceptors
  • Clonidine
  • Morphine
  • N-(4-hydroxyphenacetyl)-4-aminoclonidine
  • Naloxone
  • Opioid receptors
  • Xylazine
  • Yohimbine

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