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Pharmacological properties of 2-[4-(2-thiazolyloxy)-phenyl]-propionic acid (480156-S), a new non-steroidal antiinflammatory agent.

Abstract
In terms of antiinflammatory activity in acute and chronic animal models, 2-[4-(2-thiazolyloxy)-phenyl]-propionic acid (480156-S) was more active than ibuprofen but inferior to indomethacin. The analgesic activities of 480156-S measured by the writhing method and the Randall & Selitto method were comparable or superior to those of indomethacin, diclofenac-Na and ketoprofen. 480156-S also had strong antagonistic action against bradykinin, markedly inhibiting all bradykinin-induced edema and pain reactions (tail licking in mice and flexor reflex of rabbit hind limb). On scald-induced pain in which bradykinin is greatly involved, 480156-S had an obviously stronger analgesic effect than any of the reference drugs. As for its effects on prostaglandin (PG), 480156-S weakly inhibited arachidonic acid-induced edema and pain reactions but also inhibited PGE2 synthesis of bovine vesicular gland microsomes.
AuthorsK Hirose, H Jyoyama, Y Kojima, M Eigyo, H Hatakeyama, F Asanuma, H Umehara, T Yamaguchi
JournalArzneimittel-Forschung (Arzneimittelforschung) Vol. 34 Issue 3 Pg. 280-6 ( 1984) ISSN: 0004-4172 [Print] Germany
PMID6610429 (Publication Type: Journal Article)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Phenylpropionates
  • Prostaglandins
  • 480156-S
  • Carrageenan
Topics
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (toxicity)
  • Arthritis, Experimental (drug therapy)
  • Carrageenan (antagonists & inhibitors)
  • Erythema (drug therapy)
  • Female
  • Gastric Mucosa (drug effects)
  • Guinea Pigs
  • Lethal Dose 50
  • Male
  • Mice
  • Phenylpropionates (pharmacology)
  • Prostaglandins (biosynthesis)
  • Rabbits
  • Rats
  • Rats, Inbred Strains
  • Reflex (drug effects)
  • Stomach Ulcer (chemically induced)

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