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阿维菌素

阿维菌素用途

Avermectin B1a 是一种抗寄生虫剂,能够使线虫瘫痪。

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阿维菌素名称

[ CAS 号 ]:
65195-55-3

[ 中文名 ]:
阿维菌素

[ 英文名 ]:
Avermectin B1a

[中文别名 ]:

[英文别名 ]:

5-O-Demethyl Antibiotic C 076A1a
Abamectinum [Latin]
Abamectin B1a
AVERMECTIN B1A
Abamectine [French]
[3H]-Abamectin B1a
Abamectin komponente B1a
22,23-dihydroavermectinh B1a
abamectin component B1a
Avermectin B(1)a

阿维菌素生物活性

[ 描述 ]:

Avermectin B1a 是一种抗寄生虫剂,能够使线虫瘫痪。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[体外研究]

[3H] AVM B1a优先与来自大鼠脑的几个区域的突触膜结合。 [3H] AVM B1a与完整单层颗粒细胞的特异性结合随孵育时间迅速增加,并在24℃下约20分钟后达到平衡。较高浓度的[3H] AVM B1a导致显着更大的非特异性结合,在25nM时为60％。各种AVM类似物还在完整小脑神经元中产生[3H] AVM B1a结合的浓度依赖性抑制。 AVM B1a和莫昔克丁的效力相似(IC50值分别为120和126 nM)[3]。来自小鼠脑突触小泡的AVMB1a刺激的氯化物流出来自GABA不敏感的氯通道的激活,并且这种作用不同于它们先前记录的对小鼠脑制剂中GABA门控氯通道的影响[4]。

[体内研究]

当AVM B1a浓度高于83.3 mg/kg时,细菌受到显着抑制,而真菌在土壤中受损较少。高浓度AVM B1a也抑制了土壤呼吸,这与土壤类型不同。 AVM B1a对土壤蚯蚓的半致死剂量(LD50)在滤纸接触试验中估计为4.63 mg×cm2,在人工土壤中处理7天和14天后分别为24.13和17.06 mg/kg [1]。在人工土壤中,AVM B1a对蚯蚓的LC50分别为24.1 mg/kg和17.1 mg/kg,持续7天和14天。在暴露于无AVM B1a土壤后1天内,两组中分别消除了约80.0％和94.8％的AVM B1a,但在蚯蚓相对较长时间内发现了痕量的AVM B1a [2]。。

[参考文献]

[1]. Sun Y, et al. [Effects of avermectin B1a on soil microorganism and earthworm (Eisenia fetida)]. Ying Yong Sheng Tai Xue Bao. 2005 Nov;16(11):2140-3.

[2]. Sun Y, et al. Bioaccumulation and elimination of avermectin B1a in the earthworms (Eisenia fetida). Chemosphere. 2005 Jul;60(5):699-704.

[3]. Huang J, et al. Avermectin B1a binds to high- and low-affinity sites with dual effects on the gamma-aminobutyric acid-gated chloride channel of cultured cerebellar granule neurons. J Pharmacol Exp Ther. 1997 Apr;281(1):261-6.

[4]. Payne GT, et al. Activation of gamma-aminobutyric acid insensitive chloride channels in mouse brain synaptic vesicles by avermectin B1a. J Biochem Toxicol. 1991 Winter;6(4):283-92.

[相关活性小分子]

阿维菌素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
940.9±65.0 °C at 760 mmHg

[ 熔点 ]:
157-162ºC

[ 分子式 ]:
C₄₈H₇₂O₁₄

[ 分子量 ]:
873.077

[ 闪点 ]:
268.1±27.8 °C

[ 精确质量 ]:
872.492188

[ PSA ]:
170.06000

[ LogP ]:
6.51

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.571

[ 储存条件 ]:
通风低温干燥

阿维菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CL1200000

CHEMICAL NAME :: Avermectin A1a, 5-O-demethyl-

CAS REGISTRY NUMBER :: 65195-55-3

LAST UPDATED :: 199706

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C48-H72-O14

MOLECULAR WEIGHT :: 873.20

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD20 - Lethal Dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 mg/kg

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

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 32,94,1984

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

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 32,94,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 19 mg/kg

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

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 42,1786,1994

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

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 32,94,1984

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阿维菌素安全信息

[ 危险品运输编码 ]:
UN 2588

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2932999099

阿维菌素合成路线

详细合成路线

阿维菌素上下游产品

阿维菌素上游产品

阿维菌素下游产品

阿维菌素海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%