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

doi:10.1007/BF02142554

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

IRCCS Ospedale San Raffaele

Research output: Contribution to journal › Article

Abstract

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 language	English
Pages (from-to)	247-249
Number of pages	3
Journal	Agents and Actions
Volume	23
Issue number	3-4
DOIs	https://doi.org/10.1007/BF02142554
Publication status	Published - May 1988

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ASJC Scopus subject areas

Toxicology
Pharmacology (medical)

Cite this

Netti, C., Guidobono, F., Sibilia, V., Villa, I., Cazzamalli, E., & Pecile, A. (1988). Central effects of histamine H2-receptor agonists and antagonists on nociception in the rat. Agents and Actions, 23(3-4), 247-249. https://doi.org/10.1007/BF02142554

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abstract = "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.",

author = "C. Netti and F. Guidobono and V. Sibilia and I. Villa and E. Cazzamalli and A. Pecile",

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AU - Netti, C.

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AU - Cazzamalli, E.

AU - Pecile, A.

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