Literature DB >> 6433676

The antiinflammatory profile of (5H-dibenzo[a,d]-cyclohepten-5-ylidene)acetic acid (WY-41,770), an agent possessing weak prostaglandin synthetase inhibitory activity that is devoid of gastric side effects.

R P Carlson, L J Datko, J Chang, S T Nielsen, A J Lewis.   

Abstract

Wy-41,770 [(5H-dibenzo[a,d]cyclohepten-5-ylidene)acetic acid], a novel acrylic acid, was compared to indomethacin and aspirin in standard antiinflammatory, analgesic and antipyretic animal models. The acute antiinflammatory, analgesic and antipyretic activity of Wy-41,770 (oral ED50S 50-170 mg/kg) was similar to aspirin; however, it was considerably more potent orally in adjuvant arthritis in the rat (ED50, 16 mg/kg) and urate-induced synovitis in the dog (ED50, 4.5 mg/kg). Wy-41,770 was a weak inhibitor of prostaglandin biosynthesis and did not inhibit either 5- or 15-lipoxygenase. Furthermore, the cellular migration characteristic of carrageenan pleurisy was not affected by Wy-41,770. Unlike a majority of NSAIDs, it produced no gastric irritation in rats after either acute or chronic oral administration over the range 400-800 mg/kg. The major mechanism of action of Wy-41,770 has yet to be identified but does not seem to involve interference of arachidonic acid metabolism.

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Year:  1984        PMID: 6433676     DOI: 10.1007/bf01978903

Source DB:  PubMed          Journal:  Agents Actions        ISSN: 0065-4299


  15 in total

1.  A method for measurement of analgesic activity on inflamed tissue.

Authors:  L O RANDALL; J J SELITTO
Journal:  Arch Int Pharmacodyn Ther       Date:  1957-09-01

2.  Some quantitative temporal characteristics of carrageenin-induced pleurisy in the rat.

Authors:  R Vinegar; J F Truax; J L Selph
Journal:  Proc Soc Exp Biol Med       Date:  1973-07

3.  Quantitative determination of prostaglandins and malondialdehyde formed by the arachidonate oxygenase (prostaglandin synthetase) system of bovine seminal vesicle.

Authors:  R J Flower; H S Cheung; D W Cushman
Journal:  Prostaglandins       Date:  1973-09

4.  Inhibitory effects of indomethacin, aspirin and certain other drugs on inflammations induced in rat and dog by carrageenan, sodium urate and ellagic acid.

Authors:  C G van Arman; R P Carlson; E A Risley; R H Thomas; G W Nuss
Journal:  J Pharmacol Exp Ther       Date:  1970-11       Impact factor: 4.030

5.  Leukotrienes: a new class of mediators of immediate hypersensitivity reactions and inflammation.

Authors:  B Samuelsson
Journal:  Adv Prostaglandin Thromboxane Leukot Res       Date:  1983

6.  Drugs which inhibit prostaglandin biosynthesis.

Authors:  R J Flower
Journal:  Pharmacol Rev       Date:  1974-03       Impact factor: 25.468

7.  Changes in cellular enzyme levels and the inhibition of selective release of lysosomal hydrolases from macrophages by indomethacin.

Authors:  C Finlay; P Davies; A C Allison
Journal:  Agents Actions       Date:  1975-10

8.  Anti-inflammatory and related properties of 2-(2,4-dichlorophenoxy)phenylacetic acid (fenclofenac).

Authors:  D C Atkinson; E C Leach
Journal:  Agents Actions       Date:  1976-09

9.  An analysis of the gastro-intestinal side-effects of non-steroidal anti-inflammatory drugs, with particular reference to comparative studies in man and laboratory species.

Authors:  K D Rainsford
Journal:  Rheumatol Int       Date:  1982       Impact factor: 2.631

10.  Neutral protease activation of peritoneal macrophage prostaglandin synthesis.

Authors:  J Chang; F Wigley; D Newcombe
Journal:  Proc Natl Acad Sci U S A       Date:  1980-08       Impact factor: 11.205

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  3 in total

1.  Fine structural damage to the intestinal mucosa induced by two non-steroid anti-inflammatory drugs of varying potency as prostaglandin synthesis inhibitors.

Authors:  K D Rainsford; S A Fox
Journal:  Agents Actions       Date:  1985-03

2.  Lymphoid abnormalities in rats with adjuvant-induced arthritis. I. Mitogen responsiveness and lymphokine synthesis.

Authors:  S C Gilman; J F Daniels; R E Wilson; R P Carlson; A J Lewis
Journal:  Ann Rheum Dis       Date:  1984-12       Impact factor: 19.103

3.  Modulation of mouse ear edema by cyclooxygenase and lipoxygenase inhibitors and other pharmacologic agents.

Authors:  R P Carlson; L O'Neill-Davis; J Chang; A J Lewis
Journal:  Agents Actions       Date:  1985-12
  3 in total

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