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.
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Authors | R R Brooks, K E Miller, S S Pelosi Jr, S F Pong, D R Anthony Jr, M M Goldenberg |
Journal | Arzneimittel-Forschung
(Arzneimittelforschung)
Vol. 38
Issue 1
Pg. 59-65
(Jan 1988)
ISSN: 0004-4172 [Print] Germany |
PMID | 3365279
(Publication Type: Journal Article)
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Chemical References |
- Anti-Inflammatory Agents, Non-Steroidal
- Bronchodilator Agents
- Furans
- Immunosuppressive Agents
- Uricosuric Agents
- 5-(5-(4-chlorophenyl-2-furanyl))dihydro-2(3H)-furanone
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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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