Literature DB >> 871089

AHR-5850: a potent anti-inflammatory compound.

L F Sancilio, D L Reese, S Cheung, R S Alphin.   

Abstract

AHR-5850 is a non-steroidal anti-inflammatory compound possessing antipyretic and analgesic properties. AHR-5850 was 16.4 and 22.8 times more potent than phenylbutazone in suppressing acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation, respectively. The analgesic activity of AHR 5850 was 43 times that of acetylsalicylic acid in the Randall-Selitto assay, and 156 and 56.3 times more potent than phenylbutazone in the acetylcholine-induced abdominal constriction in mice and in the bradykinin-induced nociceptive response in dogs, respectively. Single-dose studies showed that AHR-5850 produced less gastric irritation than acetylsalicylic acid when applied topically to the exposed gastric mucosa of cats or when administered orally to rats and dogs. Upon subchronic oral administration to rats, the therapeutic ratio of AHR-5850 was twice that of phenylbutazone. This was based on the ratio of its potency relative to phenylbutazone in producing intestinal lesions to its anti-inflammatory potency relative to phenylbutazone in the adjuvant-induced arthritis.

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Year:  1977        PMID: 871089     DOI: 10.1007/bf01964911

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


  17 in total

1.  Carrageenin-induced edema in hind paw of the rat as an assay for antiiflammatory drugs.

Authors:  C A WINTER; E A RISLEY; G W NUSS
Journal:  Proc Soc Exp Biol Med       Date:  1962-12

2.  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

3.  Suppression of lymphocyte transformation by aspirin.

Authors:  G Opelz; P I Terasaki; A A Hirata
Journal:  Lancet       Date:  1973-09-01       Impact factor: 79.321

4.  Adjuvant-induced arthritis in rats. II. Drug effects on physiologic, biochemical and immunologic parameters.

Authors:  D T Walz; M J DiMartino; A Misher
Journal:  J Pharmacol Exp Ther       Date:  1971-07       Impact factor: 4.030

5.  New method for evaluating topical action of substances on gastric mucosa.

Authors:  R S Alphin; D A Droppleman
Journal:  J Pharm Sci       Date:  1971-09       Impact factor: 3.534

6.  Interactions of anti-inflammatory drugs in carrageenan-induced foot edema of the rat.

Authors:  K F Swingle; T J Grant; L W Jaques; D C Kvam
Journal:  J Pharmacol Exp Ther       Date:  1970-04       Impact factor: 4.030

7.  Levels of three hydrolases in rheumatoid and regenerated synovium.

Authors:  J L Granda; C S Ranawat; A S Posner
Journal:  Arthritis Rheum       Date:  1971 Mar-Apr

8.  Evans blue-carrageenan pleural effusion as a model for the assay of nonsteroidal antirheumatic drugs.

Authors:  L F Sancilio
Journal:  J Pharmacol Exp Ther       Date:  1969-07       Impact factor: 4.030

9.  Application of sequential analysis to Evans blue-carrageenan-induced pleural effusion for screening compounds for anti-inflammatory activity.

Authors:  L F Sancilio; A Fishman
Journal:  Toxicol Appl Pharmacol       Date:  1973-12       Impact factor: 4.219

10.  Anti-inflammatory properties of 4,5-diphenyl-2-oxazolepropionic acid (oxaprozin).

Authors:  M E Rosenthale; A J Begany; A Dervinis; J L Malis; D A Shriver; S L Datko; M I Gluckman
Journal:  Agents Actions       Date:  1974-08
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  6 in total

1.  Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers.

Authors:  T L Ke; G Graff; J M Spellman; J M Yanni
Journal:  Inflammation       Date:  2000-08       Impact factor: 4.092

2.  Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy.

Authors:  D A Gamache; G Graff; M T Brady; J M Spellman; J M Yanni
Journal:  Inflammation       Date:  2000-08       Impact factor: 4.092

3.  QSAR and conformational analysis of the antiinflammatory agent amfenac and analogues.

Authors:  J Ruiz; M López; J Milà; E Lozoya; J J Lozano; R Pouplana
Journal:  J Comput Aided Mol Des       Date:  1993-04       Impact factor: 3.686

4.  The topical anti-inflammatory and analgesic properties of bromfenac in rodents.

Authors:  J C Nolan; L E Wagner; C E Gathright; D J Stephens; L F Sancilio
Journal:  Agents Actions       Date:  1988-08

5.  AHR-10037, a non-steroidal anti-inflammatory compound of low gastric toxicity.

Authors:  L F Sancilio; J C Nolan; L E Wagner; C E Gathright; D D Droppleman; R S Alphin; D A Walsh; W J Welstead
Journal:  Agents Actions       Date:  1990-08

6.  Synergism between subthreshold doses of phenylbutazone and prednisolone in rat hind-paw carrageenan edema.

Authors:  M Sandrini
Journal:  Agents Actions       Date:  1979-04
  6 in total

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