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OR-462

OR-462用途

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。

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OR-462名称

[ CAS 号 ]:
116313-94-1

[ 中文名 ]:
硝替卡朋

[ 英文名 ]:
Nitecapone

[英文别名 ]:

Nitecapone
Nitecapona [INN-Spanish]
Nitecapone [INN]
OR 462
Nitecaponum [INN-Latin]

OR-462生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> COMT

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

信号通路 >> 代谢酶/蛋白酶 >> COMT

[体外研究]

硝酸酯类化合物(1-100μM)可将ROO诱导的GSH(还原型谷胱甘肽)耗竭降低11-38%,氧化为氧化型谷胱甘肽(GSSG)降低32-45%[1]。

[体内研究]

硝丙肾上腺素(30mg/kg,每天ip,连续13天)可减少大鼠脊髓神经结扎后神经源性疼痛的发生和症状[3]。动物模型：雄性Wistar大鼠86只,体重140-350克[3]。剂量：30mg/kg(3.3ml/kg)。给药：IP,每天一次,连续13天。结果：选择性、特异性地抑制外周组织和中枢神经系统的COMT持续约3h,提高机械刺激的阈值,从而减少机械性痛觉超敏。与对照组相比,硝酸甘油预处理组大鼠同侧爪子的阳性反应减少。

[参考文献]

[1]. Y J Suzuki, et al. Antioxidant properties of nitecapone (OR-462). Free Radic Biol Med. 1992 Nov;13(5):517-25.

[2]. Marcocci L, et al. Nitecapone: a nitric oxide radical scavenger. Biochemistry and Molecular Biology International, 01 Oct 1994, 34(3):531-541.

[3]. Oleg Kambur, et al. Nitecapone reduces development and symptoms of neuropathic pain after spinal nerve ligation in rats. Eur J Pain. 2011 Aug;15(7):732-40.

OR-462物理化学性质

[ 密度 ]:
1.451g/cm3

[ 沸点 ]:
495.3ºC at 760 mmHg

[ 分子式 ]:
C₁₂H₁₁NO₆

[ 分子量 ]:
265.21900

[ 闪点 ]:
211.6ºC

[ 精确质量 ]:
265.05900

[ PSA ]:
120.42000

[ LogP ]:
2.09060

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
1.95E-10mmHg at 25°C

[ 折射率 ]:
1.645

[ 储存条件 ]:
2-8°C，密封，干燥

OR-462MSDS

详细MSDS(安全技术说明书)

OR-462毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SA1942500

CHEMICAL NAME :: 2,4-Pentanedione, 3-((3,4-dihydroxy-5-nitrophenyl)methylene)-

CAS REGISTRY NUMBER :: 116313-94-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C12-H11-N-O6

MOLECULAR WEIGHT :: 265.24

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987- Volume(issue)/page/year: 69,64,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 507 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987- Volume(issue)/page/year: 69,64,1991

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OR-462安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

OR-462合成路线

详细合成路线

OR-462上下游产品

OR-462上游产品

OR-462下游产品

OR-462文献

D1-like dopamine receptor activation and natriuresis by nitrocatechol COMT inhibitors.

Kidney Int. 59(5) , 1683-94, (2001)

In recent years, several nitrocatechol derivatives (tolcapone, entacapone, and nitecapone) have been developed and found to be highly selective and potent inhibitors of catechol-O-methyltransferase (C...

Extending levodopa action: COMT inhibition.

Neurology 50(6 Suppl 6) , S27-32; discussion S44-8, (1998)

Degradation of levodopa in the periphery is known to be associated with motor fluctuations and dyskinesia in Parkinson's disease (PD) patients. The enzyme catechol-O-methyltransferase (COMT) is respon...

The Helicobacter felis mouse model in assessing anti-Helicobacter therapies and gastric mucosal prostaglandin E2 levels.

Scand. J. Gastroenterol. 31(4) , 334-8, (1996)

The aims of the present study were to assess the usefulness of the Helicobacter felis mouse model in the evaluation of antimicrobial therapies and the effect of Helicobacter infection on gastric mucos...

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