Literature DB >> 8273586

Effects of pyridinyl imidazole compounds on murine TNF-alpha production.

D L Olivera1, J T Laydon, L Hillegass, A M Badger, J C Lee.   

Abstract

The effects of SK&F 86002 and other pyridinyl imidazole compounds on murine cytokine production were investigated. In vitro, SK&F 86002 inhibited LPS stimulated TNF-alpha production by the RAW 264.7 cell line and by oil elicited peritoneal macrophages with an IC50 of 5 microM. In general, the activity was reflective of previous results obtained with human monocytes as SK&F 86002 and its analogs demonstrated identical rank order potency for TNF-alpha inhibition in both species. These compounds also inhibited TNF-alpha in vivo in a murine model of endotoxin shock. Following oral administration, SK&F 86002 and its analogs reduced serum TNF-alpha levels by > 80% and afforded 100% protection from lethality. In contrast, tenidap, a novel anti-inflammatory drug, had minimal to no effect on murine TNF-alpha production in the same assays. These data further extend the pharmacological profile of the pyridinyl imidazoles by demonstrating that these compounds potently inhibit murine TNF-alpha production both in vitro and in vivo.

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Year:  1993        PMID： 8273586     DOI： 10.1007/bf01972719

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


  8 in total

1.  SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.

Authors:  D E Griswold; P J Marshall; E F Webb; R Godfrey; J Newton; M J DiMartino; H M Sarau; J G Gleason; G Poste; N Hanna
Journal:  Biochem Pharmacol       Date:  1987-10-15       Impact factor: 5.858

Review 2.  Biologic activities and mechanisms of action of tumor necrosis factor-alpha/cachectin.

Authors:  M Jäättelä
Journal:  Lab Invest       Date:  1991-06       Impact factor: 5.662

3.  Modification of proinflammatory cytokine production by the antirheumatic agents tenidap and naproxen. A possible correlate with clinical acute phase response.

Authors:  J D Sipe; L M Bartle; L D Loose
Journal:  J Immunol       Date:  1992-01-15       Impact factor: 5.422

4.  Effect of SK&F 86002 on cytokine production by human monocytes.

Authors:  J C Lee; L Rebar; J T Laydon
Journal:  Agents Actions       Date:  1989-06

Review 5.  Interleukins and tumor necrosis factor in inflammation.

Authors:  J S Warren
Journal:  Crit Rev Clin Lab Sci       Date:  1990       Impact factor: 6.250

6.  Are tolfenamic acid and tenidap dual inhibitors of 5-lipoxygenase and cyclo-oxygenase?

Authors:  K E Proudman; R M McMillan
Journal:  Agents Actions       Date:  1991-09

7.  Inhibition of interleukin 1 synthesis by tenidap: a new drug for arthritis.

Authors:  I G Otterness; M L Bliven; J T Downs; E J Natoli; D C Hanson
Journal:  Cytokine       Date:  1991-07       Impact factor: 3.861

8.  Protective effect of SK&F 86002, a novel dual inhibitor of arachidonic acid metabolism, in murine models of endotoxin shock: inhibition of tumor necrosis factor as a possible mechanism of action.

Authors:  A M Badger; D Olivera; J E Talmadge; N Hanna
Journal:  Circ Shock       Date:  1989-01
  8 in total
  1 in total

1.  SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1.

Authors:  Margit Schwartz; Sabine Böckmann; Philipp Borchert; Burkhard Hinz
Journal:  Oncotarget       Date:  2018-05-01
  1 in total

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