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Amoxapine (CL-67772) 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 (CL-67772) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
200 mg | ¥ 349 | 现货 | |
500 mg | ¥ 535 | 现货 |
产品描述 | Amoxapine (CL-67772) 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 | GlyT2a:92 μM, GlyT1b:1 mM |
体外活性 | 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. |
体内活性 | 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。 |
别名 | 阿莫沙平, CL-67772 |
分子量 | 313.78 |
分子式 | C17H16ClN3O |
CAS No. | 14028-44-5 |
Smiles | ClC=1C=C2C(=NC=3C(OC2=CC1)=CC=CC3)N4CCNCC4 |
密度 | 1.37g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 3.14 mg/mL (10 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
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