Effects of AF3442 [N-(9-ethyl-9H-carbazol-3-yl)-2-(trifluoromethyl)benzamide], a novel inhibitor of human microsomal prostaglandin E synthase-1, on prostanoid biosynthesis in human monocytes in vitro.

@article{Bruno2010EffectsOA,
  title={Effects of AF3442 [N-(9-ethyl-9H-carbazol-3-yl)-2-(trifluoromethyl)benzamide], a novel inhibitor of human microsomal prostaglandin E synthase-1, on prostanoid biosynthesis in human monocytes in vitro.},
  author={Annalisa Bruno and Luigia Di Francesco and Isabella Coletta and Giorgina Mangano and Maria Alessandra Alisi and Lorenzo Polenzani and Claudio Milanese and Paola Anzellotti and Emanuela Ricciotti and Melania Dovizio and Andrea Di Francesco and Stefania Tacconelli and Marta L Capone and Paola Patrignani},
  journal={Biochemical pharmacology},
  year={2010},
  volume={79 7},
  pages={974-81}
}
Inhibitors of microsomal prostaglandin (PG) E synthase-1 (mPGES-1) are being developed for the relief of pain. Redirection of the PGH(2) substrate to other PG synthases, found both in vitro and in vivo, in mPGES-1 knockout mice, may influence their efficacy and safety. We characterized the contribution of mPGES-1 to PGH(2) metabolism in lipopolysaccharide (LPS)-stimulated isolated human monocytes and whole blood by studying the synthesis of prostanoids [PGE(2), thromboxane (TX)B(2), PGF(2alpha… CONTINUE READING

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