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Anti-inflammatory activity of orpanoxin administered orally and topically to rodents.

Abstract
Orpanoxin, a nonsteroidal anti-inflammatory drug (NSAID) lacking gastric ulcerogenic effects in the therapeutic dose range in rats, was compared with six reference NSAIDs for oral activity in the rat paw carrageenin-induced edema assay. Tested NSAIDs were ranked on the basis of oral mg/kg ED50 values: piroxicam, 0.55; orpanoxin, 35.6; diflunisal, 59.6; benoxaprofen, greater than 300; tolmetin sodium, greater than 300; and sulindac, greater than 300. Zomepirac sodium was inactive. Only the three most potent compounds produced greater than 60% inhibition of edema. Inhibition was generally greater at 4 h than at 6 h post carrageenin for all compounds. Oral activity of orpanoxin was also demonstrated in the guinea-pig u.v.-induced erythema model (ED50 = 24.2 mg/kg p.o. when given 1 h before irradiation) and in the mouse ear croton oil induced edema test (ED50 value = 131 mg/kg p.o.). Topical activity of orpanoxin was assessed in both the guinea-pig and mouse models. In the guinea-pig u.v.-induced erythema model, application (1 h after u.v.) of 1, 5, and 10% (w/v) orpanoxin creams (containing 10% urea) significantly inhibited erythema at 2, 3, and 4 h post-irradiation. Orpanoxin, mefenamic acid, and indomethacin as 1% creams inhibited total erythema scores 70, 92 and 74%, respectively. Evidence for topical activity in the mouse ear assay was also obtained for orpanoxin in diethyl ether or 10% urea cream, but not in dimethylsulfoxide. It was concluded that orpanoxin has anti-inflammatory activity comparable to reference NSAIDs in the rat paw edema test, is active orally in rat, mouse, and guinea-pig models, and shows topical activity in the guinea-pig and the mouse.
AuthorsR R Brooks, K R Bonk, G E Decker, K E Miller
JournalAgents and actions (Agents Actions) Vol. 16 Issue 5 Pg. 369-76 (Jul 1985) ISSN: 0065-4299 [Print] Switzerland
PMID4050616 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Anti-Inflammatory Agents
  • Propionates
  • Thiazines
  • Piroxicam
  • Diflunisal
  • Croton Oil
  • Carrageenan
  • orpanoxin
Topics
  • Administration, Oral
  • Administration, Topical
  • Animals
  • Anti-Inflammatory Agents (therapeutic use)
  • Carrageenan
  • Croton Oil
  • Diflunisal (therapeutic use)
  • Edema (chemically induced, drug therapy)
  • Erythema (drug therapy, etiology)
  • Guinea Pigs
  • Inflammation (chemically induced, drug therapy)
  • Male
  • Mice
  • Piroxicam
  • Propionates (administration & dosage, therapeutic use)
  • Rats
  • Rats, Inbred Strains
  • Thiazines (therapeutic use)
  • Ultraviolet Rays

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