Meclofenamate sodium is an inhibitor of both the 5-lipoxygenase and cyclooxygenase pathways of the arachidonic acid cascade in vitro.

@article{Boctor1986MeclofenamateSI,
  title={Meclofenamate sodium is an inhibitor of both the 5-lipoxygenase and cyclooxygenase pathways of the arachidonic acid cascade in vitro.},
  author={Amal M. Boctor and M Eickholt and Thomas A. Pugsley},
  journal={Prostaglandins, leukotrienes, and medicine},
  year={1986},
  volume={23 2-3},
  pages={
          229-38
        }
}
Meclofenamate sodium was compared to other nonsteroidal antiinflammatory drugs in terms of its potency to inhibit the formation of 5-HETE and LTB4 in human leukocytes and the formation of prostaglandin E2 in bovine seminal vesicles as measures of its ability to inhibit the 5-lipoxygenase and cyclooxygenase pathways of the arachidonic acid cascade. Meclofenamate sodium was about 2-4 times less potent than BW-755C in inhibiting 5-lipoxygenase enzyme activity and three times more potent than… Expand
Effect of CI-922, a potential new antiallergy agent, on arachidonic acid metabolism in vitro
TLDR
The parallel inhibition of 5-HETE and LTB4 formation by CI-922 suggests that either direct or indirect inhibition of the 5-lipoxygenase pathway may explain, at least in part, its antiallergy properties. Expand
Modulation of arachidonic acid metabolism by orally administered morniflumate in man
TLDR
In whole blood experiments, morniflumate reduced blood LTB4 synthesis induced by Ca-ionophore A23187 Bx approximately 50%, both after single dose and at steady state; the degree of inhibition showed a pattern similar to the plasma levels of the bioactive metabolite of morn IFLumate (M1). Expand
Orally administered tolfenamic acid inhibits leukotriene synthesis in isolated human peripheral polymorphonuclear leukocytes
TLDR
It is suggested that inhibition of leukotriene synthesis is an additional mechanism of the anti-inflammatory, antimigraine and antidysmenorrhoeic effects of tolfenamic acid, and a possible explanation for its rare gastric and bronchoconstrictive side-effects. Expand
Disparate effects of the prostaglandin synthesis inhibitors, meclofenamate, and flurbiprofen on monkey luteal tissue in vitro.
TLDR
The data indicate that Mec and Flur are potent inhibitors of PG synthesis in primate luteal cells in vitro and higher doses of Mec suppress PG- and gonadotropin-sensitive adenylate cyclase activity and P production. Expand
Effects of non-steroidal anti-inflammatory drugs on polymorphonuclear leukocyte functions in vitro: focus on fenamates
TLDR
It is concluded that NSAIDs with a fenamate structure differ from other NSAIDs by inhibiting PMN functions induced either by receptor-mediated stimulus (LTB4) or calcium ionophore (A23187) at micromolar drug concentrations. Expand
Pharmacological control of human polymorphonuclear leukocyte degranulation by fenamates and inhibitors of receptor-mediated calcium entry and protein kinase C.
TLDR
The results suggest that the suppressive actions of fenamates on PMN degranulation are neither related to the activity of cyclooxygenase nor PMA-activated protein kinase C. Expand
Comparison of in vitro effects of flunixin and tolfenamic acid on human leukocyte and platelet functions
TLDR
It is suggested that inhibition of PMN functions may be an additional mechanism in the antiinflammatory action of tolfenamic acid. Expand
5-lipoxygenase inhibitors and their anti-inflammatory activities.
  • D. Batt
  • Chemistry, Medicine
  • Progress in medicinal chemistry
  • 1992
TLDR
A wide variety of agents have been reported as 5-LO inhibitors, including phenols, partially saturated aromatics, and compounds containing heteroatom-heteroatom bonds, which have been, in general, disappointing, probably because of poor bioavailability caused by lipophilicity and metabolic instability. Expand
Inhibition of human neutrophil function by tolfenamic acid involves inhibition of Ca2+ influx.
TLDR
Tolfenamic acid inhibited in a concentration-dependent manner the degranulation response and Ca2+ influx in neutrophils activated by the chemotactic peptide fMLP or A23187, and increased the cellular cAMP levels up to 1.3-fold in the presence of the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine. Expand
Cellular mechanisms for the control of glucocorticoid metabolism by 11-beta hydroxysteroid dehydrogenase in the human ovary
TLDR
The structure of 1 lpHSDl protein was modelled to develop molecular mechanisms by which prostaglandins, gonadotrophins and cytokines might regulate enzyme activities, and it was found that most phosphorylation sites would lie in the lumen of the endoplasmic reticulum. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 19 REFERENCES
Selective inhibition of the cyclooxygenase pathway of the arachidonic acid cascade by the nonsteroidal antiinflammatory drug isoxicam
The effects of the nonsteroidal antiinflammatory drug isoxicam on prostaglandin formation by HSDM1C1 mouse fibrosarcoma cells grown in culture and 5‐HETE(5(S)‐5‐hydroxy‐6‐trans, 8,11,14‐cisExpand
Differential effects of anti-inflammatory drugs on lipoxygenase and cyclo-oxygenase activities of neutrophils from a reverse passive Arthus reaction.
TLDR
Rat neutrophils isolated from four-hour reverse passive Arthus reaction pleural exudates actively metabolize arachidonic acid and the calcium ionophore A23187 and BRIJ 56 synergistically act to augment the metabolism of exogenously added arachidsonic acid via lipoxygenase. Expand
A new approach to anti-inflammatory drugs.
TLDR
2-pyrazoline inhibits both pathways of arachidonic acid metabolism in vitro and causes a dose-dependent reduction in carrageenin-induced oedema in the rat paw, and BW755C reduces prostaglandin concentration in inflammatory exudates and has a significantly greater effect on leukocyte migration than indomethacin. Expand
Inhibition of the release of slow‐reacting substance of anaphylaxis by inhibitors of lipoxygenase activity
TLDR
This communication compares the effect of benoxaprofen with those of BW755c, another lipoxygenase inhibitor (Higgs et a1 1979), and with two potent P G cyclo oxygengenase inhibitors, indomethacin and piroxicam (Carty et al 1980) on the formation of both lip Oxygenase products and SRS-A. Expand
Selective inhibition of the lipoxygenase metabolic pathway of arachidonic acid by the SRS-A antagonist, FPL 55712.
TLDR
FPL 55712, the SRS-A antagonist, was found to inhibit the formation of lipoxygen enzyme products, but not the cyclooxygenase products, and Proxicromil was qualitatively similar, but markedly less potent. Expand
Increased concentrations of nonesterified arachidonic acid, 12L-hydroxy-5,8,10,14-eicosatetraenoic acid, prostaglandin E2, and prostaglandin F2alpha in epidermis of psoriasis.
TLDR
The increased levels of arachidonic acid and 12L-hydroxy-5,8,10,14-eicosatetraenoic acid in involved epidermis may have diagnostic and pathophysiological importance. Expand
Inhibition of mouse skin tumor promotion by several inhibitors of arachidonic acid metabolism.
TLDR
The results support the hypothesis that at least some of the products of arachidonic acid transformation are essential for tumor promotion. Expand
Dexamethasone-induced inhibition of prostaglandin production dose not result from a direct action on phospholipase activities but is mediated through a steroid-inducible factor.
TLDR
Several indications suggest that dexamethasone may induce the secretion of a non-dialysable, transferable factor able to inhibit prostaglandin production, the mechanism of which remains to be investigated. Expand
Arachidonic acid metabolism in polymorphonuclear leukocytes: effects of ionophore A23187.
  • P. Borgeat, B. Samuelsson
  • Chemistry, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1979
TLDR
The data demonstrate that, in addition to causing release of endogenous substrate, the ionophore also activated the enzymatic system involved in the further transformations of arachidonic acid. Expand
ANTAGONISM BY FENAMATES OF PROSTAGLANDIN ACTION IN GUINEA‐PIG AND HUMAN ALIMENTARY MUSCLE
TLDR
Sodium mefenamate or mefenamic acid, even in high concentrations, had little effect on contractions to PGF2α, but tended to inhibit PGE2‐induced contractions of human gastrointestinal longitudinal muscle. Expand
...
1
2
...