General properties and clinical possibilities of new selective inhibitors of catechol O-methyltransferase.

@article{Kaakkola1994GeneralPA,
  title={General properties and clinical possibilities of new selective inhibitors of catechol O-methyltransferase.},
  author={Seppo Kaakkola and Ariel Gordin and Pekka T. M{\"a}nnist{\"o}},
  journal={General pharmacology},
  year={1994},
  volume={25 5},
  pages={813-24}
}
1. The structure of catechol O-methyltransferase (COMT) has been recently characterized and a series of new and selective COMT inhibitors developed. 2. Entacapone, nitecapone and tolcapone are nitrocatechol-type potent COMT inhibitors in vitro (Ki in nanomolar range). They are also very selective for COMT and active in vivo even after oral administration. CGP 28014 is a pyridine derivative that is active only in vivo. 3. In animal studies, these compounds inhibit effectively the O-methylation… CONTINUE READING
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