Nitecapone 是一个具有口服活性的、短效的儿茶酚-O-甲基转移酶(COMT)的抑制剂。它具有胃肠道保护和抗氧化活性,能够清除活性氧和一氧化氮,防止脂质过氧化。
产品描述
Nitecapone is a reversible inhibitor of S-COMT (IC50 values of 300 nM in rat liver)
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].
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].
Cas No.
116313-94-1
分子式
C12H11NO6
分子量
265.221
储存和溶解度
DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years