多拉菌素

多拉菌素用途

为新型、广谱抗寄生虫药，对胃肠道线虫、肺线虫、螨、蜱和伤口蛆等均有高效，用于治疗家畜线虫病和螨病等体外寄生虫病，主要适用于牛和猪。

多拉菌素作用

多拉菌素用于治疗家畜线虫病和螨病等体外寄生虫病，由基因重组的阿维链霉菌（Streptomyces avermitilis）新菌株发酵而得，与伊维菌素主要差别为C25位为环己基取代，为新型、广谱抗寄生虫药，对胃肠道线虫、肺线虫、眼虫、虱、蜱、螨和伤口蛆均有高效，对体内外寄生虫特别是某些线虫（圆虫）和节肢动物也具有良好的驱杀作用，但对绦虫、吸虫及原生动物无效。其作用机制主要是增加虫体的抑制性递质γ氨基丁酸（GABA）的释放，从而阻断神经信号的传递，使肌肉细胞失去收缩能力，而导致虫体死亡。哺乳动物的外周神经递质为乙酰胆碱，不会受到多拉菌素的影响，多拉菌素不易透过血脑屏障，对中枢神经系统损害极小，对牲畜比较安全。主要特点是血药浓度及半衰期均比伊维菌素高或延长两倍。美国已批准牛、猪专用的注射液和牛专用的浇泼剂。

多拉菌素名称

[ CAS 号 ]:
117704-25-3

[ 中文名 ]:
多拉克丁

[ 英文名 ]:
Doramectin

[中文别名 ]:

多拉菌素

[英文别名 ]:

Doromectin
Doramectina
Doramectin
25-cyclohexyl-avermectin B1
DONGGUAI.P.E
Dectoma
Dectomax
Doramecin

多拉菌素生物活性

[ 描述 ]:

Doramectin具有抗寄生虫活性。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[参考文献]

[1]. Davey RB, Pound JM, Klavons JA, Lohmeyer KH, Freeman JM, Olafson PU. Analysis of doramectin in the serum of repeatedly treated pastured cattle used to predict the probability of cattle fever ticks (Acari: Ixodidae) feeding to repletion. Exp Appl Acarol.

[2]. Wang XJ, Zhang J, Wang JD, Huang SX, Chen YH, Liu CX, Xiang WS. Four new doramectin congeners with acaricidal and insecticidal activity from Streptomyces avermitilis NEAU1069. Chem Biodivers. 2011 Nov;8(11):2117-25. doi: 10.1002/cbdv.201000295.

[3]. Sarre C, Claerebout E, Vercruysse J, Levecke B, Geldhof P, Pardon B, Alvinerie M, Sutra JF, Geurden T. Doramectin resistance in Haemonchus contortus on an alpaca farm in Belgium. Vet Parasitol. 2012 Apr 30;185(2-4):346-51.

[4]. Lobetti R. .Successful resolution of oesophageal spirocercosis in 20 dogs following daily treatment with oral doramectin. Vet J. 2012 Jul;193(1):277-8.

[5]. Wang JB, Pan HX, Tang GL. Production of doramectin by rational engineering of the avermectin biosynthetic pathway. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3320-3.

[相关活性小分子]

多拉菌素物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
967.4±65.0 °C at 760 mmHg

[ 熔点 ]:
116 - 119ºC

[ 分子式 ]:
C₅₀H₇₄O₁₄

[ 分子量 ]:
899.114

[ 闪点 ]:
274.4±27.8 °C

[ 精确质量 ]:
898.507874

[ PSA ]:
170.06000

[ LogP ]:
7.16

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.580

[ 储存条件 ]:
0-6°C

[ 水溶解性 ]:
methanol: soluble

多拉菌素MSDS

详细MSDS(安全技术说明书)

多拉菌素安全信息

[ 符号 ]:

GHS06, GHS09

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H410

[ 警示性声明 ]:
P273-P301 + P310-P501

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

[ 危害码 (欧洲) ]:
T,N,Xi

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
33-45-60-61-36/37-26

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

多拉菌素文献

Anthelmintic resistance in a herd of alpacas (Vicugna pacos).

Can. Vet. J. 53(12) , 1310-3, (2012)

A herd of alpacas was examined because of a history of severe endoparasitism, anemia, hypoproteinemia, and weight loss. Resistance of gastrointestinal nematodes to albendazole, fenbendazole, and doram...

Reversal of P-glycoprotein-mediated multidrug resistance in vitro by doramectin and nemadectin.

J. Pharm. Pharmacol. 62(3) , 393-9, (2010)

Multidrug resistance (MDR) is a serious obstacle encountered in cancer treatment. This study was performed to explore the reversal of MDR by doramectin from the avermectin family and nemadectin belong...

The influence of gastrointestinal parasitism on fecal elimination of doramectin, in lambs.

Ecotoxicol. Environ. Saf. 73(8) , 2017-21, (2010)

A study was done to investigate the effect of parasitism on patterns of doramectin (DRM) fecal elimination in lambs. Fourteen Suffolk Down parasitized lambs (26.9 ± 1.5 kg body weight: bw) were purpos...

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