Name | Nitecapone |
Description | Nitecapone is a reversible inhibitor of S-COMT (IC50 values of 300 nM in rat liver) |
Animal Research | 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]. |
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]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 2.5 mg/mL (9.43 mM)
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Keywords | GSH | glutathione | OR-462 | Inhibitor | ROS | Parkinson | Nitecapone | COMT | OR 462 | inhibit | OR462 | allodynia |
Inhibitors Related | Serotonin hydrochloride | Risedronate Sodium | Risedronic Acid | 3-Methoxybenzamide | Entacapone | OU749 | Ibandronate sodium | Testosterone propionate | Alendronate sodium hydrate | Flopropione |
Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Antioxidant Compound Library | Inhibitor Library | Orally Active Compound Library | Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Oxidation-Reduction Compound Library |