伊维菌素

伊维菌素用途

Ivermectin是广泛使用于人类和动物的抗寄生虫剂。它是P2X4和α7 nAChRs的正异构效应物。

伊维菌素作用

伊维菌素主要对体内线虫和体表节肢动物具有良好驱杀作用。对牛、羊的血矛线虫、奥斯特线虫、古柏线虫、毛圆线虫（包括艾氏毛圆线虫）、圆形线虫、仰口线虫、细颈线虫、毛首线虫、食道口线虫、网尾线虫以及绵羊夏伯特线虫成虫、第四期幼虫驱除率97％～100％。对节肢动物亦很有效，如蝇蛆、螨和虱等。对嚼虱和绵羊羊蜱蝇疗效稍差。伊维菌素对蜱以及粪便中繁殖的蝇也极有效，药物虽不能立即使蜱死亡，但能影响摄食、蜕皮和产卵，从而降低生殖能力。对血蝇的作用相似。对猪的蛔虫、红色猪圆线虫、兰氏类圆线虫、毛首线虫、食道口线虫、后圆线虫、有齿冠尾线虫成虫及未成熟虫体驱除率达94％～100％，对肠道内旋毛虫（肌肉内旋毛虫无效）也极有效，对猪血虱和猪疥螨也有良好控制作用。对吸虫和绦虫无效。

伊维菌素名称

[ CAS 号 ]:
70288-86-7

[ 中文名 ]:
依维菌素

[ 英文名 ]:
Ivermectin

[中文别名 ]:

[英文别名 ]:

Vermic
mk933
Ivosint
EINECS 274-536-0
22,23-dihydroavermectin B1
MFCD00869511
Mectizan
mk-0933
CARDOMEC
IVOMEC

伊维菌素生物活性

[ 描述 ]:

Ivermectin是广泛使用于人类和动物的抗寄生虫剂。它是P2X4和α7 nAChRs的正异构效应物。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[体外研究]

伊维菌素(IVM)是异源表达的P2X4和可能的异聚P2X4/P2X6通道的特异性正变构效应子。在亚微摩尔范围内(EC50 = 250nM),IVM的作用是快速且可逆的,导致由ATP引起的P2X4通道电流的振幅增加和减慢的失活。在不改变P2X4通道的离子选择性的情况下,IVM还显着增加ATP和正常低效激动剂a,b-亚甲基-ATP的效力,而不改变P2X4通道的离子选择性[1]。 IVM激活寄生虫神经和肌肉中的谷氨酸门控氯通道,导致膜超极化和肌肉麻痹。 IVM的主要作用方式很可能是破坏寄生虫的摄食活动,导致饥饿[2]。在微摩尔范围内预先施用伊维菌素可强烈增强随后在非洲爪蟾卵母细胞和K-28细胞中重建的神经元鸡或人α7烟碱乙酰胆碱受体的乙酰胆碱诱发电流[3]。伊维菌素激活大鼠重组α1β2γ2sGABAA受体。用10mM GABA激活通道导致电流在1ms内上升至其最大振幅。 GABA的EC50值为7.5μM[4]。

[参考文献]

[1]. Khakh BS, et al. Allosteric control of gating and kinetics at P2X(4) receptor channels. J Neurosci. 1999 Sep 1;19(17):7289-99.

[2]. Priel A, et al. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004 Mar;123(3):281-93.

[3]. Krause RM, et al. Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor. Mol Pharmacol. 1998 Feb;53(2):283-94.

[4]. Adelsberger H, et al. Activation of rat recombinant alpha(1)beta(2)gamma(2S) GABA(A) receptor by the insecticide ivermectin. Eur J Pharmacol. 2000 Apr 14;394(2-3):163-70.

[相关活性小分子]

伊维菌素物理化学性质

[ 熔点 ]:
155 °C

[ 分子式 ]:
C₄₈H₇₄O₁₄

[ 分子量 ]:
875.09300

[ 精确质量 ]:
874.50800

[ PSA ]:
170.06000

[ LogP ]:
5.60140

[ 外观性状 ]:
白色至灰白色固体

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: ≤1.0% KF

伊维菌素MSDS

详细MSDS(安全技术说明书)

伊维菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: IH7891500

CHEMICAL NAME :: 22,23-Dihydroavermectin B1

CAS REGISTRY NUMBER :: 70288-86-7

LAST UPDATED :: 199309

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 :: 29500 ug/kg

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

REFERENCE :: AJVRAH American Journal of Veterinary Research. (American Veterinary Medical Assoc., 930 N. Meacham Rd., Schaumburg, IL 60196) V.1- 1940- Volume(issue)/page/year: 53,2032,1992

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - cattle

DOSE/DURATION :: 8 mg/kg

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

REFERENCE :: SCIEAS Science. (American Assoc. for the Advancement of Science, 1333 H St., NW, Washington, DC 20005) V.1- 1895- Volume(issue)/page/year: 221,823,1983 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 73 mg/kg

SEX/DURATION :: multigeneration

TOXIC EFFECTS :: Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - delayed effects

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 27,523,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 655 mg/kg

SEX/DURATION :: multigeneration

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - other postnatal measures or effects

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 27,523,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 72 mg/kg

SEX/DURATION :: female 6-20 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: NETEEC Neurotoxicology and Teratology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.9- 1987- Volume(issue)/page/year: 10,267,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 36 mg/kg

SEX/DURATION :: female 6-20 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

REFERENCE :: NETEEC Neurotoxicology and Teratology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.9- 1987- Volume(issue)/page/year: 10,267,1988

伊维菌素安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
61-25-36-36/38-22

[ 安全声明 (欧洲) ]:
53-26-45-36

[ 危险品运输编码 ]:
UN 2811 6.1/PG 2

[ WGK德国 ]:
3

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2932999099

伊维菌素制备

1.由阿维菌素氢化而成。含22,23-二氢B_1a与B_1b的比例为8:2

2.由相应的不饱和化合物在苯中，在催化及作用下，在室温下常压氢化制得。

伊维菌素海关

[ 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%

伊维菌素文献

Permethrin and ivermectin for scabies.

N. Engl. J. Med. 362(8) , 717-25, (2010)

Cytokine responses to egg protein in previously allergic children who developed tolerance naturally.

Ann. Allergy Asthma Immunol. 113(6) , 667-670.e4, (2014)

[Comparative activity of different groups of insecticides against permethrin-resistant lice (anoplura: pediculidae)].

Med. Parazitol. (Mosk.) (1) , 20-7, (2013)

The activity of insecticides (CK50, CK95 ) from different chemical classes against permethrin-resistant body and head lice was investigated. Having developed resistance to pyrethroids (permethrin, d-p...

更多文献

伊维菌素相关知识

伊维菌素的作用与功效是什么？

2022-04-21 10:48:19

标题：伊维菌素的作用与功效是什么？　　1928年，弗莱明发现青霉素，人类跟细菌以及各种寄生虫的战斗从此变得更加主动，近一个世纪以来，人类陆续发现发现或者生物合成了越来越多的抗生素，用于对抗细菌感染或者其它疾病。70年代中期，阿维菌素被发现，可以用来对抗寄生虫，科学家坎贝尔和大村智在深入研究阿维菌素...