Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.

@article{Duplantier1996BiarylcarboxylicAA,
  title={Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.},
  author={Allen J. Duplantier and Michael S. Biggers and Robert J. Chambers and John B. Cheng and Kevin L. Cooper and David B. Damon and James F. Eggler and Kenneth G. Kraus and Anthony Marfat and Hiroko Masamune and J. S. Pillar and J. T. Shirley and John P. Umland and John W. Watson},
  journal={Journal of medicinal chemistry},
  year={1996},
  volume={39 1},
  pages={
          120-5
        }
}
  • Allen J. Duplantier, Michael S. Biggers, +11 authors John W. Watson
  • Published in
    Journal of medicinal…
    1996
  • Chemistry, Medicine
  • In addition to having desirable inhibitory effects on inflammation, anaphylaxis, and smooth muscle contraction, PDE-IV inhibitors also produce undesirable side effects including nausea and vomiting. In general, compounds that inhibit PDE-IV also potently displace [3H]rolipram from a high-affinity binding site in rat cortex. While this binding site has not been identified, it has been proposed to be an allosteric binding site on the PDE-IV enzyme. Preliminary studies have suggested that the… CONTINUE READING

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