PMID: 9427067Jan 14, 1998Paper

Pharmacological profile of JTE-522, a novel prostaglandin H synthase-2 inhibitor, in rats

Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]
M MatsushitaK Wakitani

Abstract

The antinociceptive, antipyretic, and anti-inflammatory effects of JTE-522, a novel selective prostaglandin H synthase (PGHS)-2 inhibitor, were examined in rats. Sheep seminal vesicle PGHS-1 and placenta PGHS-2 were used for in vitro assay, while for in vivo experiments, male rats (4-8 weeks old) were used. JTE-522 and reference compounds (0.01-100 microM) were subjected to enzyme assay. JTE-522 (0.3-30 mg/kg) and indomethacin (0.3-10 mg/kg) were administered orally. JTE-522 inhibited PGHS-2 (IC50: 0.64 microM) without affecting PGHS-1 activity at 100 microM. In rats with yeast-induced hyperalgesia, JTE-522 showed a dose-dependent antinociceptive effect (ED50: 4.4 mg/kg). In rats with yeast-induced pyrexia, JTE-522 significantly reversed the pyrexic response (ED50: 3.9 mg/kg). Orally administered JTE-522 dose-dependently inhibited carrageenin-induced rat paw edema (ED30: 4.7 mg/kg). In rats with adjuvant-induced arthritis, JTE-522 showed a significant inhibitory effect at daily doses of 0.3-3 mg/kg. JTE-522 did not cause severe gastric lesions at oral doses up to 300 mg/kg. Our results indicate that the selective PGHS-2 inhibitor JTE-522 may represent a novel type of anti-inflammatory drug without adverse effects on the gastroi...Continue Reading

Citations

Apr 14, 2000·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·T YamamotoN Nozaki-Taguchi
May 2, 2009·Archives of Pharmacal Research·Yan TongYing-Lin Cao
Dec 20, 2002·International Immunopharmacology·Shigeyuki MatsuzakiMasataka Majima
Nov 26, 2002·British Journal of Clinical Pharmacology·Yasuhiko IkedaMitsuru Takahashi
Oct 5, 2001·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·N HayashiM Monden
Dec 18, 2002·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Toshiaki OkumuraMasataka Majima
Jan 19, 2006·Journal of Bone and Mineral Research : the Official Journal of the American Society for Bone and Mineral Research·Mika KatagiriHiroshi Kawaguchi
Jul 13, 2011·Biochemical Pharmacology·Junko ImanishiSeitaro Mutoh
Dec 30, 1998·Japanese Journal of Pharmacology·K WakitaniM Matsushita
Mar 25, 2006·International Journal of Cancer. Journal International Du Cancer·Toshiya SomaYutaka Shimada
Sep 24, 2004·The Journal of Biological Chemistry·Daisuke InoueToshio Matsumoto

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