116313-94-1
中文名称
硝替卡朋
英文名称
Nitecapone
CAS
116313-94-1
分子式
C12H11NO6
分子量
265.22
MOL 文件
116313-94-1.mol
更新日期
2025/04/30 20:07:21
116313-94-1 结构式
基本信息
中文别名
硝替卡朋 英文别名
OR 462Nitecapone
3-(3,4-Dihydroxy-5-nitrobenzylidene)pentane-2,4-dione
3-[(3,4-Dihydroxy-5-nitrophenyl)methylene]-2,4-pentanedione
所属类别
生物化工：抑制剂物理化学性质
熔点171-173°C
沸点495.3±45.0 °C(Predicted)
密度1.451±0.06 g/cm3(Predicted)
储存条件-20°C冷冻
溶解度DMSO：可溶15mg/mL，澄清
酸度系数(pKa)5.60±0.50(Predicted)
形态粉末
颜色白色至米色
常见问题列表
简介
硝替卡朋(OR-462) 是一种药物，可作为儿茶酚 O-甲基转移酶 (COMT) 的选择性抑制剂。它已获得抗帕金森药物专利。
用途
硝替卡朋可用作儿茶酚-O-甲基转移酶(COMT)抑制剂。
生物活性
Nitecapone (OR-462) 是一个短效的、具有口服活性的、儿茶酚-O-甲基转移酶 (COMT) 的抑制剂，具有胃肠道保护和抗氧化活性。Nitecapone (OR-462) 可清除活性氧和一氧化氮，防止脂质过氧化。体外研究
Nitecapone (1-100 μM) reducesd GSH (reduced glutathione) depletion induced by ROO - by 11-38% and oxidation to oxidized glutathione (GSSG) by 32-45%.
体内研究
Nitecapone (30 mg/kg, ip daily for 13 days) reduces development and symptoms of neuropathic pain after spinal nerve ligation in rats.
| Animal Model: | Eighty-six male Wistar rats, weighing 140-350 g. |
| Dosage: | 30 mg/kg (3.3 mL/kg). |
| Administration: | IP, once daily for 13 days. |
| Result: |
Selectively and specifically inhibits COMT in the peripheral tissues, and to some extent in the CNS for ca. 3 h.
Increased the thresholds for the mechanical stimuli and thus reduced mechanical allodynia. Reduced the number of positive reactions of the ipsilateral paws when compared with the baselines in the nitecapone-pretreated rats. |