| 名称 | Amoxapine |
| 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. |
| 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。 |
| 存储条件 | store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 8.06 mg/mL (25.69 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (3.19 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | Inhibitor | inhibit | GlyT2a | GlyT1b | CL67772 | CL 67772 | Amoxapine |
| 相关产品 | Adipic dihydrazide | Aceglutamide | Cysteamine hydrochloride | Doxycycline | Neomycin sulfate | BES | Terbinafine hydrochloride | Metronidazole | Hydroxychloroquine | Dimethyl sulfoxide | Sulfamethoxazole sodium | Paeonol |
| 相关库 | 抑制剂库 | 血脑屏障通透化合物库 | 经典已知活性库 | 已知活性化合物库 | 肝脏毒性化合物库 | ReFRAME 相关化合物库 | FDA上市及药典收录分子库 | FDA 上市药物库 | 免疫/炎症分子化合物库 | 神经退行性疾病化合物库 | 口服活性化合物库 | 药物功能重定位化合物库 |