A novel phosphodiesterase type 4 inhibitor, YM976 (4-(3-chlorophenyl)-1,7-diethylpyrido[2,3-d]pyrimidin-2(1H)-one), with little emetogenic activity.

@article{Aoki2000ANP,
  title={A novel phosphodiesterase type 4 inhibitor, YM976 (4-(3-chlorophenyl)-1,7-diethylpyrido[2,3-d]pyrimidin-2(1H)-one), with little emetogenic activity.},
  author={Makoto Aoki and Masanobu Kobayashi and Jun Ishikawa and Yuji Saita and Yoshito Terai and Kiyoshige Takayama and K. Miyata and Toshimitsu Yamada},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2000},
  volume={295 1},
  pages={255-60}
}
We synthesized a novel phosphodiesterase type 4 (PDE4) inhibitor, YM976, that is structurally different from the other PDE4 inhibitors like rolipram. In the present study, the pharmacological profile of YM976 was investigated. YM976 exhibited a strong and competitive inhibition against PDE4 purified from human peripheral leukocytes with an IC(50) of 2.2 nM. IC(50) values of rolipram and RP73401 were 820 and 0.43 nM, respectively. Test compounds had no effects on the other PDE isozymes, PDE1, -2… CONTINUE READING

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