首页 Neuroscience GlyT Amoxapine
Amoxapine
编号 T1568     别名: CL-67772
CAS 14028-44-5     分子式 C17H16ClN3O     分子量 313.79
靶点: GlyT1b; GlyT2a;
Amoxapine exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.
选择批次  
规格 库存 单价 数量
200 mg 上海现货 420.00
500 mg 上海现货 618.00
1 mL * 10 mM (in DMSO) 上海现货 148.00
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生物活性

产品描述

Amoxapine exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.

靶点活性

GlyT1b,1mM

GlyT2a,92μM

体外活性

在卵母细胞和HEK 293细胞中,Amoxapine可导致急性hERG阻塞,IC50分别为21.6 和5.1 μM。在人类胚胎肾293细胞中,Amoxapine选择性抑制GLYT2a,抑制效果比同种型GLYT1b高出10倍。Amoxapine阻滞反向频变,并引起向左移位的加速失活。Amoxapine处理使HEK 293细胞中运输到细胞膜表面的hERG缓慢减少,其IC50为15.3 μM。

体内活性

Amoxapine(1, 5和10 mg/kg, i.p.),尤其在低剂量下,可使异相睡眠减少并增加慢波睡眠.在整个治疗中,Amoxapine(10 mg/kg, i.p.)会引起异相睡眠的持续降低,但在该睡眠状态下,可发现cericlamine抑制效果的耐受性.Amoxapine(10 mg/kg/day)对P物质,强啡肽和缩胆囊素的水平无影响,但显著增加了大鼠大脑皮层、脊髓和下丘脑中亮氨酸-脑啡肽的水平.Amoxapine(10 mg/kg/day,i.p.)不会改变大鼠大脑皮层阿片受体,但脊髓中δ-和μ-阿片受体结合位点的密度增加,在下丘脑中降低.Amoxapine减弱自发活动,引起强直性昏厥和眼睑下垂,通过改变猴子辨别的回避行为而产生对Apomorphine不断阵痛和amphetamine刻板行为的抑制作用.

化学信息

分子量

313.79

分子式

C17H16ClN3O

CAS

14028-44-5

溶解度

DMSO: 10 mg/mL (31.87 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 3.187 ml 15.934 ml 31.868 ml
5 mM 0.637 ml 3.187 ml 6.374 ml
10 mM 0.319 ml 1.593 ml 3.187 ml
50 mM 0.064 ml 0.319 ml 0.637 ml
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