Nitecapone is a reversible inhibitor of S-COMT (IC50 values of 300 nM in rat liver)

S-COMT:300 nM

At high micromolar to millimolar concentrations in in vitro research studies, nitecapone is an effective antioxidant, nitric oxide radical scavenger, and iron chelator that can protect cells from lipid peroxidation[1]

After single administration, both?nitecapone?and OR-486 reduced mechanical nociceptive thresholds and thermal nociceptive latencies (hot plate test) at 2 and 3 h, regardless of their brain penetration. These effects were still present after chronic treatment with COMT inhibitors for 5 days. Intraplantar injection of carrageenan reduced nociceptive latencies and both COMT inhibitors potentiated this reduction without modifying inflammation. CGP 28014 shortened paw flick latencies. OR-486 did not modify hot plate times in Comt gene deficient mice. Intrathecal?nitecapone?modified neither thermal nor mechanical nociception[2].

Used single and repeated administration of a peripherally restricted, short-acting (nitecapone) and also a centrally acting (3,5-dinitrocatechol, OR-486) COMT inhibitor.?We also tested CGP 28014, an indirect inhibitor of COMT enzyme.?Effects of OR-486 on thermal nociception were also studied in COMT deficient mice.?Effects on spinal pathways were assessed in rats given intrathecal nitecapone[2].