| 名称 | Nitecapone |
| 描述 | Nitecapone is a reversible inhibitor of S-COMT (IC50 values of 300 nM in rat liver) |
| 动物实验 | 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]. |
| 体外活性 | 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] |
| 体内活性 | 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]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 2.5 mg/mL (9.43 mM)
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| 关键字 | GSH | glutathione | OR-462 | Inhibitor | ROS | Parkinson | Nitecapone | COMT | OR 462 | inhibit | OR462 | allodynia |
| 相关产品 | Risedronate Sodium | Rosmarinic acid | Alendronate sodium hydrate | OU749 | Entacapone | Risedronic Acid | 3-Methoxybenzamide | Minodronic acid monohydrate | Serotonin hydrochloride | Flopropione | Testosterone propionate | Ibandronate sodium |
| 相关库 | 抑制剂库 | 抗帕金森病化合物库 | 经典已知活性库 | 已知活性化合物库 | 氧化还原化合物库 | ReFRAME 相关化合物库 | 抗衰老化合物库 | 神经退行性疾病化合物库 | 口服活性化合物库 | 人代谢物化合物库 |
