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Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation.

Abstract
The effects of the highly selective histamine H4 receptor antagonists JNJ7777120 and VUF6002 were investigated on the carrageenan-induced inflammation and thermal hyperalgesia in rats. JNJ7777120 (10 and 30 mg/kg, s.c.) and VUF6002 (10 mg/kg, s.c.) significantly reduced paw edema and hyperalgesia provoked by subplantar injection of carrageenan; the effect was evident against the early (2 h) phase of inflammation. An inactive analog of VUF6002, VUF6007 (10 mg/kg, s.c.) slightly aggravated paw edema, while leaving unaltered carrageenan-induced nociception. These findings indicate that histamine H4 receptors participate in the early phase of acute inflammation induced by carrageenan in rats, influencing both edema and thermal hyperalgesia.
AuthorsGabriella Coruzzi, Maristella Adami, Elena Guaita, Iwan J P de Esch, Rob Leurs
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 563 Issue 1-3 Pg. 240-4 (Jun 01 2007) ISSN: 0014-2999 [Print] Netherlands
PMID17382315 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Analgesics
  • Anti-Inflammatory Agents
  • Benzimidazoles
  • Histamine Antagonists
  • Hrh4 protein, rat
  • Indoles
  • Piperazines
  • Receptors, G-Protein-Coupled
  • Receptors, Histamine
  • Receptors, Histamine H4
  • VUF 6002
  • 1-((5-chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine
  • Carrageenan
Topics
  • Analgesics (pharmacology)
  • Animals
  • Anti-Inflammatory Agents (pharmacology)
  • Benzimidazoles (pharmacology)
  • Carrageenan
  • Disease Models, Animal
  • Edema (metabolism, prevention & control)
  • Histamine Antagonists (pharmacology)
  • Hot Temperature
  • Hyperalgesia (etiology, metabolism, prevention & control)
  • Indoles (pharmacology)
  • Inflammation (chemically induced, complications, metabolism, prevention & control)
  • Male
  • Pain Measurement
  • Piperazines (pharmacology)
  • Rats
  • Rats, Wistar
  • Receptors, G-Protein-Coupled (antagonists & inhibitors, metabolism)
  • Receptors, Histamine (metabolism)
  • Receptors, Histamine H4
  • Time Factors

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