CP-66,248, a new anti-inflammatory agent, is a potent inhibitor of leukotriene B4 and prostanoid synthesis in human polymorphonuclear leucocytes in vitro

Eicosanoids. 1988;1(1):35-9.

Abstract

The effects of (Z)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H- indole-1-carboxamide (CP-66,248), a new anti-inflammatory agent, were tested on the synthesis of the pro-inflammatory arachidonic acid metabolites, LTB4 and PGE2, in isolated human peripheral polymorphonuclear leucocytes. At clinically achievable (i.e. plasma) drug concentration, CP-66,248 reduced A 23187-stimulated LTB4 (IC50 18 +/- 1 microM) and PGE2 (IC50 32 +/- 8 nM) synthesis. The corresponding IC50 values for arachidonic acid-induced LTB4 and PGE2 production were 13 +/- 4 microM and 65 +/- 15 nM, respectively. The inhibitory action of CP-66,248 towards 5-lipoxygenase was comparable with that of timegadine and exceeded that of caffeic acid, and its action against the cyclo-oxygenase pathway was similar to that of other NSAIDs tested. The dual inhibition of cyclo-oxygenase and lipoxygenase pathways of arachidonic acid metabolism is likely to be involved in the anti-inflammatory, antipyretic and analgetic action of CP-66,248 detected in a variety of experimental models.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Arachidonate 5-Lipoxygenase / metabolism
  • Arachidonic Acids / pharmacology
  • Calcimycin / pharmacology
  • Cyclooxygenase Inhibitors
  • Dinoprostone / biosynthesis*
  • Dinoprostone / metabolism
  • Humans
  • In Vitro Techniques
  • Indoles / pharmacology*
  • Leukotriene B4 / biosynthesis*
  • Leukotriene B4 / metabolism
  • Lipoxygenase Inhibitors
  • Neutrophils / drug effects*
  • Neutrophils / metabolism
  • Oxindoles
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Thromboxane B2 / biosynthesis*
  • Thromboxane B2 / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Arachidonic Acids
  • Cyclooxygenase Inhibitors
  • Indoles
  • Lipoxygenase Inhibitors
  • Oxindoles
  • Leukotriene B4
  • Calcimycin
  • Thromboxane B2
  • tenidap
  • Arachidonate 5-Lipoxygenase
  • Prostaglandin-Endoperoxide Synthases
  • Dinoprostone