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恩他卡朋

恩他卡朋用途

Entacapone是特异的外周活性的邻苯二酚-O-甲基转移酶(COMT)抑制剂,IC50为151 nM。

恩他卡朋名称

[ CAS 号 ]:
130929-57-6

[ 中文名 ]:
恩他卡朋

[ 英文名 ]:
Entacapone

[中文别名 ]:

[英文别名 ]:

Comtan
Comtes
OR-611
MFCD00866580
Comtess
Entacapone

恩他卡朋生物活性

[ 描述 ]:

Entacapone是特异的外周活性的邻苯二酚-O-甲基转移酶(COMT)抑制剂,IC50为151 nM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> COMT

信号通路 >> 神经信号通路 >> COMT

研究领域 >> 神经疾病

[参考文献]

[1]. Piccini P, Brooks DJ, Korpela K, The catechol-O-methyltransferase(COMT) inhibitor entacapone enhances the pharmacokinetic and clinical response to Sinemet CR in Parkinson's disease. J Neurol Neurosurg Psychiatry. 2000 May;68(5):589-94.

[2]. Di Giovanni S, Eleuteri S, Paleologou KE, Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J Biol Chem. 2010 May 14;285(20):1494

[3]. Sethi KD, Hauser RA, Isaacson SH, Levodopa/carbidopa/entacapone 200/50/200 mg (Stalevo 200) in the treatment of Parkinson's disease: a case series. Cases J. 2009 Jul 30;2:7134.

[4]. Poulopoulos M, Waters C. Carbidopa/levodopa/entacapone: the evidence for its place in the treatment of Parkinson's disease. Core Evid. 2010 Jul 27;5:1-10.

[相关活性小分子]

血清胺盐酸盐 | 托卡朋 | 奥匹卡朋 | 夫洛丙酮 | 恩他卡朋钠盐

恩他卡朋物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
526.6±50.0 °C at 760 mmHg

[ 熔点 ]:
162-1630C

[ 分子式 ]:
C₁₄H₁₅N₃O₅

[ 分子量 ]:
305.286

[ 闪点 ]:
272.3±30.1 °C

[ 精确质量 ]:
305.101166

[ PSA ]:
130.38000

[ LogP ]:
2.38

[ 外观性状 ]:
黄色粉末

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.642

[ 储存条件 ]:
-20°C Freezer

恩他卡朋MSDS

详细MSDS(安全技术说明书)

恩他卡朋安全信息

[ 危害码 (欧洲) ]:
Xn,T,F

[ 风险声明 (欧洲) ]:
R10:Flammable. R20/21/22:Harmful by inhalation, in contact with skin and if swallowed . R37/38:Irritating to respiratory system and skin . R41:Risk of serious damage to eyes. R62:Possible risk of impaired fertility. R38:Irritating to the skin. R36/37/38:Ir

[ 安全声明 (欧洲) ]:
S26-S36-S39-S45-S36/37/39-S16

[ 危险品运输编码 ]:
UN 1986 3/PG 3

[ WGK德国 ]:
1

[ RTECS号 ]:
KM5250000

[ 包装等级 ]:
III

[ 危险类别 ]:
3

[ 海关编码 ]:
2942000000

恩他卡朋合成路线

详细合成路线

恩他卡朋制备

1.83g 3,4-二羟基-5-硝基苯甲醛和1.5g N,N-二乙基氰基乙酰胺和催化量的哌啶乙酸盐溶于40ml干燥乙醇中,搅拌过夜,得2.23g粗品,收率73%,熔点153～156℃.

2. 在90℃下加热,将3.0kg粗品溶于含80gHBr(或40gHCl)的8.0kg乙酸(或甲酸)中.缓慢冷却到20℃,并在此温度搅拌20h,然后在15℃搅拌6h.过滤收集析出的结晶,先小心地用冷的(4℃)1L甲苯-乙酸(1:lv/v)的混合液洗,再用1L的冷甲苯洗.在真空和45℃下干燥,得2.4kg结晶性的纯的恩他卡朋,收率80％,mp162~163℃.

恩他卡朋海关

[ 海关编码 ]: 2942000000

恩他卡朋文献

Dog UDP-glucuronosyltransferase enzymes of subfamily 1A: cloning, expression, and activity.

Drug Metab. Dispos. 43(1) , 107-18, (2014)

Understanding drug glucuronidation in the dog, a preclinical animal, is important but currently poorly characterized at the level of individual enzymes. We have constructed cDNAs for the 10 dog UDP-gl...

Comparison of IPX066 with carbidopa-levodopa plus entacapone in advanced PD patients.

Parkinsonism Relat. Disord. 20(12) , 1335-40, (2014)

IPX066, an investigational extended-release carbidopa-levodopa (CD-LD) preparation, has demonstrated a rapid attainment and prolonged maintenance of therapeutic LD plasma concentrations in advanced Pa...

Entacapone and prostate cancer risk in patients with Parkinson's disease.

Mov. Disord 30(5) , 724-8, (2015)

The association between Parkinson's disease (PD) and prostate cancer, both common in elderly men, is disputable. In the STRIDE-PD study, prostate cancer developed in 9 patients (3.7%) receiving levodo...

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