| Description | Nitecapone is a reversible inhibitor of S-COMT (IC50 values of 300 nM in rat liver) |
| In vitro | 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] |
| In vivo | 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]. |
| Animal experiments | 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]. |
| Target activity | S-COMT:300 nM |
| molecular weight | 265.22 |
| Molecular formula | C12H11NO6 |
| CAS | 116313-94-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 2.5 mg/mL (9.43 mM) |
| References | 1. P.T. Männistö, Kaakkola S . Catechol-O-methyltransferase (COMT): Biochemistry, molecular biology, pharmacology, and clinical efficacy of the new selective COMT inhibitors[J]. Pharmacological Reviews, 2000, 51(4):593-628. 2. Inhibitors of catechol‐O‐methyltransferase sensitize mice to pain[J]. British Journal of Pharmacology, 2010, 161(7). 3. Salmela K S , Roine R P , H??K-Nikanne J , et al. Effect of Bismuth and Nitecapone on Acetaldehyde Production by Helicobacter pylori[J]. Scandinavian Journal of Gastroenterology, 1994, 29(6):528-531. |