| Description | 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. |
| In vitro | 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. |
| In vivo | 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。 |
| Target activity | GlyT1b:1 mM, GlyT2a:92 μM |
| Synonyms | 阿莫沙平, CL-67772 |
| molecular weight | 313.78 |
| Molecular formula | C17H16ClN3O |
| CAS | 14028-44-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | 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) |
| References | 1. Núñez E, et al. Br J Pharmacol. 2000 Jan;129(1):200-6. 2. Obers S, et al. Naunyn Schmiedebergs Arch Pharmacol, 2010, 381(5), 385-400. 3. Hamon M, et al. Neuropharmacology, 1987, 26(6), 531-539. 4. Maudhuit C, et al. Neuropharmacology, 1994, 33(8), 12017-1025. 5. Greenblatt EN, et al. Arch Int Pharmacodyn Ther, 1978, 233(1), 107-135. |