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溴夫定

溴夫定用途

Brivudine是具有抗病毒活性的胸苷类似物,用于治疗早期急性带状疱疹。

溴夫定名称

[ CAS 号 ]:
69304-47-8

[ 中文名 ]:
溴夫定

[ 英文名 ]:
Brivudine

[中文别名 ]:

[英文别名 ]:

5-[(E)-2-bromoethenyl]-2'-deoxyuridine
Brivudine
BrVDU
Bromovinyldeoxyuridine
MFCD00058585
5-[(E)-2-Bromovinyl]-2'-deoxyuridine
Zostrex
BVDU
Uridine, 5-[(E)-2-bromoethenyl]-2'-deoxy-
(E)-5-(2-Bromovinyl)-2'-deoxyuridine

溴夫定生物活性

[ 描述 ]:

Brivudine是具有抗病毒活性的胸苷类似物,用于治疗早期急性带状疱疹。

[ 相关类别 ]:

信号通路 >> 抗感染 >> CMV

研究领域 >> 感染

[体外研究]

Brivudine是胸苷的类似物,并且被掺入病毒DNA中。它阻断DNA聚合酶的作用,从而抑制病毒复制。与参考化合物如阿昔洛韦或喷昔洛韦相比,它对水痘-带状疱疹病毒具有更强的抗病毒作用[1]。它具有高水平的选择性抗水痘带状疱疹病毒(VZV)活性,抑制VZV复制,可能通过竞争性抑制病毒DNA聚合酶,或作为脱氧胸苷三磷酸的替代底物,导致病毒DNA链断裂[2]。

[体内研究]

在每天一次125毫克的剂量下,brivudine在减少新水疱产生的时间方面已被证明优于阿昔洛韦,并且缩短了疱疹后神经痛的持续时间[1]。

[参考文献]

[1]. Rabasseda X, et al. Brivudine: a herpes virostatic with rapid antiviral activity and once-daily dosing. Drugs Today (Barc). 2003 May;39(5):359-71.

[2]. Keam SJ, et al. Brivudin (bromovinyl deoxyuridine). Drugs. 2004;64(18):2091-7; discussion 2098-9.

[相关活性小分子]

乐特莫韦 | BENZIMIDAVIR 苯并咪唑核苷 | B220 | 托美洛韦

溴夫定物理化学性质

[ 密度 ]:
1.9±0.1 g/cm3

[ 沸点 ]:
382.9ºC at 760 mmHg

[ 熔点 ]:
165ºC

[ 分子式 ]:
C₁₁H₁₃BrN₂O₅

[ 分子量 ]:
333.135

[ 闪点 ]:
185.4ºC

[ 精确质量 ]:
332.000763

[ PSA ]:
104.55000

[ LogP ]:
-0.80

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 折射率 ]:
1.709

[ 储存条件 ]:
库房通风低温干燥

[ 水溶解性 ]:
Soluble in water and methanol.

溴夫定MSDS

溴夫定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YU7355000

CHEMICAL NAME :: Uridine, 5-(2-bromovinyl)-2'-deoxy-, (E)-

CAS REGISTRY NUMBER :: 69304-47-8

LAST UPDATED :: 199509

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C11-H13-Br-N2-O5

MOLECULAR WEIGHT :: 333.17

WISWESSER LINE NOTATION :: T6NVMVJ E1U1E A- ET5OTJ B1Q CQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1420 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 10920 mg/kg/52W-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Liver - other changes Nutritional and Gross Metabolic - changes in chlorine

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Human HeLa cell

DOSE/DURATION :: 4 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 267,125,1992

溴夫定安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
YU7355000

溴夫定合成路线

溴夫定文献

Characterization of pyrimidine nucleoside phosphorylase of Mycoplasma hyorhinis: implications for the clinical efficacy of nucleoside analogues.

Biochem. J. 445(1) , 113-23, (2012)

In the present paper we demonstrate that the cytostatic and antiviral activity of pyrimidine nucleoside analogues is markedly decreased by a Mycoplasma hyorhinis infection and show that the phosphorol...

Synthesis of nucleoside-based antiviral drugs in ionic liquids.

Bioorg. Med. Chem. Lett. 18(20) , 5640-2, (2008)

Nucleoside-based antiviral drugs have been synthesized using imidazolium-based ionic liquids as reaction medium. The ionic liquids were proved to be better solvents for all the nucleoside in terms of ...

Retained sensitivity to cytotoxic pyrimidine nucleoside analogs in thymidine kinase 2 deficient human fibroblasts.

Nucleosides Nucleotides Nucleic Acids 29(1) , 1-13, (2010)

Thymidine kinase 2 (TK2) is a mitochondrial deoxyribonucleoside kinase that phosphorylates several nucleoside analogs used in anti-viral and anti-cancer therapy. A fibroblast cell line with decreased ...

更多文献

溴夫定

溴夫定用途

溴夫定名称

溴夫定生物活性

溴夫定物理化学性质

溴夫定MSDS

详细MSDS(安全技术说明书)

溴夫定毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

溴夫定安全信息

溴夫定合成路线

详细合成路线

溴夫定文献

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