116313-94-1
中文名稱
硝替卡朋
英文名稱
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
2024/11/19 11:42:47
116313-94-1 結(jié)構(gòu)式
基本信息
中文別名
硝替卡朋 英文別名
OR 462Nitecapone
3-(3,4-Dihydroxy-5-nitrobenzylidene)pentane-2,4-dione
3-[(3,4-Dihydroxy-5-nitrophenyl)methylene]-2,4-pentanedione
所屬類別
生物化工：抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)171-173°C
沸點(diǎn)495.3±45.0 °C(Predicted)
密度1.451±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C冷凍
溶解度DMSO：可溶15mg/mL，澄清
酸度系數(shù)(pKa)5.60±0.50(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
簡(jiǎn)介
硝替卡朋(OR-462) 是一種藥物，可作為兒茶酚 O-甲基轉(zhuǎn)移酶 (COMT) 的選擇性抑制劑。它已獲得抗帕金森藥物專利。
用途
硝替卡朋可用作兒茶酚-O-甲基轉(zhuǎn)移酶(COMT)抑制劑。
生物活性
Nitecapone (OR-462) 是一個(gè)短效的、具有口服活性的、兒茶酚-O-甲基轉(zhuǎn)移酶 (COMT) 的抑制劑，具有胃腸道保護(hù)和抗氧化活性。Nitecapone (OR-462) 可清除活性氧和一氧化氮，防止脂質(zhì)過氧化。體外研究
Nitecapone (1-100 μM) reducesd GSH (reduced glutathione) depletion induced by ROO - by 11-38% and oxidation to oxidized glutathione (GSSG) by 32-45%.
體內(nèi)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. |