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抑制剂描述:

产品名称:Amitraz

产品别名:见爱必信官网

英文别名:Amitraz

靶点:Adrenergic Receptor

CAS:33089-61-1

纯度:99%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Amitraz是一种非系统性杀螨剂和杀虫剂, 具有α-肾上腺素能激动剂活性, 与中枢神经系统的章鱼胺受体相互作用, 且抑制单胺氧化酶和前列腺素合成。

溶解性:DMSO : 50 mg/mL (170.41 mM; Need ultrasonic)

体外研究:

Amitraz was not cytotoxic to human luteinized granulosa cells at concentrations of 1, 10 or 50 μg/ml for exposures of 2-72 h While the highest concentration of amitraz tested, 100 μg/ml, caused significant cell death after exposures of 24, 48 and 72 h. Amitraz decreased the amount of progesterone produced by each cell after a 4 h exposure; the reduction in progesterone concentration was not caused by decreased cell viability.

体内研究:Amitraz is an α2-adrenergic receptor (α2-AR) agonist that adversely affects the mammalian reproductive system by binding to presynaptic α2-AR in the hypothalamus, thus inhibiting noradrenalin release and decreasing GnRH secretion. When 30 mg/kg of amitraz was administered to rats, the ovulatory LH surge was prevented. Amitraz inhibited insulin but stimulated glucagon secretion in a perfused rat pancreas model. Amitraz also decreased intestinal motility, and inhibited prostaglandin synthesis by bovine seminal vesicle microsomes. Amitraz can be absorbed through the skin and can exert systemic effects via the vascular system in humans. Low doses of AMZ (l-25 mg/kg) decreased motor activity and altered the rates and patterns of responding under schedule-controlled conditions. Intermediate doses (50-100 mg/kg) affect visual-evoked potentials and lower body weight and temperature. In addition, 100 mg/kg produces slight MAO inhibition and characteristic signs of intoxication (e.g., weight loss and hyperreactivity). High doses (>lOO mg/kg) produce more pronounced MAO inhibition, extreme weight loss and hyperreactivity, aggression, and lethality.

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