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={A. Duplantier and M. S. Biggers and R. J. Chambers and J. Cheng and K. Cooper and D. Damon and J. F. Eggler and K. Kraus and A. Marfat and H. Masamune and J. Pillar and J. T. Shirley and J. Umland and J. W. Watson},
  journal={Journal of medicinal chemistry},
  year={1996},
  volume={39 1},
  pages={
          120-5
        }
}
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… Expand
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