Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor entacapone

@article{Nissinen1992BiochemicalAP,
  title={Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor entacapone},
  author={Erkki Nissinen and I B Lind{\'e}n and Eija Schultz and Pentti Pohto},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={1992},
  volume={346},
  pages={262-266}
}
Entacapone, OR-611, was found to be a potent peripherally acting inhibitor of catechol-O-methyl-transferase (COMT). IC50 values of 10 nmol/1 and 160 nmol/1 were obtained for rat duodenum and liver-soluble COMT, respectively. There were no effects on other catecholamine metabolizing enzymes. Entacapone showed reversible, tight-binding type of inhibition of soluble rat liver COMT with a K; value of 14 nmol/1 and it also caused 50% inhibition of rat duodenal, erythrocyte, liver and striatal COMT… CONTINUE READING

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