Central effects of histamine H2-receptor agonists and antagonists on nociception in the rat

C. Netti, F. Guidobono, V. Sibilia, I. Villa, E. Cazzamalli, A. Pecile

Research output: Contribution to journalArticle


The effects of intracerebroventricular injection of histamine H2-receptor agonists (4-methylhistamine, 4-MeH; dimaprit, DIM), H2-antagonists (cimetidine, CIM; ranitidine, RAN; famotidine, FAM) and of the DIM chemical analogue SK&F 91487 on hot-plate latency in rats were examined. Both DIM (0.4-0.8 μmol/rat) and 4-MeH (0.4-0.8 μmol/rat) significantly enhanced the pain threshold, whereas SF&F 91487 (0.8 μmol/rat) had no effect, indicating that DIM antinociception is specifically due to its activity on histamine (HA) receptors. The H2-antagonists CIM (0.8 μmol/rat) and RAN (0.6 μmol/rat) also enhanced the pain threshold, while FAM (0.03 μmol/rat) did not modify pain latency. When injected before 4-MeH, FAM reduced the antinociceptive effect of 4-MeH. These findings suggest that the antinociceptive activity of CIM and RAN is not related to specific blockade of H2-receptors and that the activation of HA-H2-receptors is inhibitory to nociception.

Original languageEnglish
Pages (from-to)247-249
Number of pages3
JournalAgents and Actions
Issue number3-4
Publication statusPublished - May 1988


ASJC Scopus subject areas

  • Toxicology
  • Pharmacology (medical)

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