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Characterization of 5-[5-(4-chlorophenyl-2-furanyl)]dihydro-2(3H)-furanone as a nonsteroidal antiinflammatory drug.

Abstract
5-[5-(4-Chlorophenyl-2-furanyl)]dihydro-2(3H)-furanone (F-1044), a nonsteroidal antiinflammatory drug related to orpanoxin, lacks the usual acid moiety of such agents. F-1044 had antiinflammatory activity equivalent to ibuprofen's and orpanoxin's in the carrageenin-induced paw edema model in normal and adrenalectomized rats. Antiinflammatory activity was also expressed in the guinea pig UV-induced erythema and rat established arthritis models. F-1044 was a more potent analgesic than ibuprofen and orpanoxin in the rat paw pressure assay. In contrast to the reference agents, F-1044 raised the pain threshold of both the yeast-injected and non-injected paws, suggesting a central component to its analgesic action. F-1044 was more potent than ibuprofen and orpanoxin in the rat brewer's yeast pyresis model. Based on its low activity in inhibiting bradykinin-induced bronchoconstriction in guinea pigs and low gastric irritation activity in rats. F-1044 appears to have a mechanisms of action that involves more than simple inhibition of prostaglandin synthesis. Thus F-1044 is a nonsteroidal antiinflammatory agent with unique chemical and pharmacological features.
AuthorsR R Brooks, K E Miller, S S Pelosi Jr, S F Pong, D R Anthony Jr, M M Goldenberg
JournalArzneimittel-Forschung (Arzneimittelforschung) Vol. 38 Issue 1 Pg. 59-65 (Jan 1988) ISSN: 0004-4172 [Print] Germany
PMID3365279 (Publication Type: Journal Article)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Bronchodilator Agents
  • Furans
  • Immunosuppressive Agents
  • Uricosuric Agents
  • 5-(5-(4-chlorophenyl-2-furanyl))dihydro-2(3H)-furanone
Topics
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (pharmacology)
  • Arthritis, Experimental (prevention & control)
  • Bronchodilator Agents
  • Furans (antagonists & inhibitors, pharmacology)
  • Guinea Pigs
  • Immunosuppressive Agents
  • Male
  • Mice
  • Rats
  • Rats, Inbred Strains
  • Stomach Ulcer (chemically induced)
  • Uricosuric Agents

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