產(chǎn)品目錄

規(guī)格	5mg
CAS	65195-55-3
別名
化學(xué)名
分子式	C48H72O14
分子量	873.08
溶解度	Chloroform: Slightly soluble,Methanol: Slightly soluble
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Avermectin B1a is a modulator of gamma-aminobutyric acid (GABA)-controlled chloride ion channels [1].

Avermectin B1a is a macrocyclic lactone derivative and possesses anthelmintic and insecticidal activities. It was obtained from the fermentation products of Streptomyces avermitilis. Avermectin B1a is usually worked as an anthelmintic and insecticidal agent. It suppresses the signal transmission of nematodes from the central command interneurons to the peripheral motoneurons. The mechanism of this action is that avermectin B1a can enhance the effects of glutamate on the gamma-aminobutyric acid (GABA)-controlled chloride ion channels, causing an influx of chloride ions into the cells. It subsequently leads to hyperpolarisation and subsequent paralysis of the neuromuscular systems. The excitatory effects can be reversed by the chloride ion channel blocker picrotoxin. Since mammals do not have this kind of ion channels, avermectin B1a has no toxicity for mammals [1 and 2].

In rat brain synaptic membranes, avermectin B1a significantly enhanced GABA binding up to 80% over control at concentration of 7 μM. Avermectin B1a also showed protection efficacy for GABA receptors from denaturation when the synaptic membranes were incubated at 60° C with 50 mM Tris-Cl. In the lobster stretcher muscle, treatment of avermectin B1a resulted in the block of IPSPs and the reduction of EPSPs. Besides that, avermectin B1a was found to have promoting effects on benzodiazepine binding. It enhanced flunitrazepan binding to synaptic membranes with EC50 value 50-fold lower than that of GABA [3 and 4].

When given to cattle, the oral administration of avermectin B1a at dose of 0.1 mg/kg reduced more than 95% of T. colubriformis, T. axei, Haemonchus placei, C. oncophora, Cooperia punctate, Ostertagia ostertagi, Oesophagostomum radiatum and Dictyocaulus viviparus. When given to sheep at the same dose, avermectin B1a administration caused also 95% above reduction of Trichostrongylus axei, Haemonchus contortus, Cooperia oncophora, Trichostrongylus colubriformis, Ostertagia circumcincta and Oesophagostomum columbianum [5].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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