Amoxapine 是一种dibenzoxazepine家族的四环抗抑郁药，常被归类为仲胺三环类抗抑郁药。

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.

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.

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。

14028-44-5

C17H16ClN3O

313.79

阿莫沙平;CL-67772

DMSO:10 mg/mL (31.87 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years