Hypothermic and antipyretic effects of 3-methyl- and 3-phenyl-5-hydroxy-5-trichloromethyl-4,5-dihydro-1H-pyrazole-1-carboxyamides in mice.

Abstract

The effect of novel pyrazolines, 3-methyl-5-hydroxy-5-trichloromethyl-4,5-dihydro-1H-pyrazole-1-carboxyamide (MPCA) and 3-phenyl-5-hydroxy-5-trichloromethyl-4,5-dihydro-1H-pyrazole-1-carboxyamide (PPCA) on body temperature and endotoxin-induced fever was investigated in mice. The subcutaneous (s.c.) administration of 1.5 mmol/kg dipyrone, MPCA or PPCA and the intracerebroventricular (i.c.v.) administration of 225 nmol dipyrone reduced basal rectal temperature. Intracerebroventricular administration of 225 nmol MPCA or PPCA did not alter basal rectal temperature. The administration of 0.15 mmol/kg (s.c.) or 25 nmol (5 microl) dipyrone (i.c.v.), MPCA or PPCA had no effect on basal rectal temperature, but reversed lipopolysaccharide-induced fever. These results suggest that MPCA and PPCA cause antipyresis, which is similar to that caused by dipyrone, and may be useful antipyretic agents.

• Authors: Fabiane R Souza, Vanessa T Souza, Viviane Ratzlaff, Lysandro P Borges, Marlí R Oliveira, Helio G Bonacorso, Nilo Zanatta, Marcos A P Martins, Carlos F Mello
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 451 Issue 2 Pg. 141-7 (Sep 13 2002) ISSN: 0014-2999 [Print] Netherlands
• PMID: 12231383 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 3-methyl-5-hydroxy-5-trichloromethyl-1H-1-pyrazolcarboxyamide
• 3-phenyl-5-hydroxy-5-trichloromethyl-4,5-dihydro-1H-pyrazole-1-carboxyamide
• Analgesics, Non-Narcotic
• Lipopolysaccharides
• Pyrazoles
• Pyrazolones
• pyrazolone
• Dipyrone

Topics

• Analgesics, Non-Narcotic (chemistry, pharmacology, therapeutic use)
• Animals
• Body Temperature (drug effects, physiology)
• Dipyrone (chemistry, pharmacology)
• Fever (chemically induced, drug therapy)
• Hypothermia (chemically induced)
• Lipopolysaccharides (pharmacology)
• Male
• Mice
• Pyrazoles (chemistry, pharmacology, therapeutic use)
• Pyrazolones