| 名稱 | 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. |
| 體外活性 | Amoxapine（1, 5和10 mg/kg, i.p.）,尤其在低劑量下,可使異相睡眠減少并增加慢波睡眠.在整個(gè)治療中,Amoxapine（10 mg/kg, i.p.）會(huì)引起異相睡眠的持續(xù)降低,但在該睡眠狀態(tài)下,可發(fā)現(xiàn)cericlamine抑制效果的耐受性.Amoxapine（10 mg/kg/day）對(duì)P物質(zhì),強(qiáng)啡肽和縮膽囊素的水平無(wú)影響,但顯著增加了大鼠大腦皮層、脊髓和下丘腦中亮氨酸-腦啡肽的水平.Amoxapine（10 mg/kg/day,i.p.）不會(huì)改變大鼠大腦皮層阿片受體,但脊髓中δ-和μ-阿片受體結(jié)合位點(diǎn)的密度增加,在下丘腦中降低.Amoxapine減弱自發(fā)活動(dòng),引起強(qiáng)直性昏厥和眼瞼下垂,通過(guò)改變猴子辨別的回避行為而產(chǎn)生對(duì)Apomorphine不斷陣痛和amphetamine刻板行為的抑制作用. |
| 體內(nèi)活性 | 在卵母細(xì)胞和HEK 293細(xì)胞中,Amoxapine可導(dǎo)致急性hERG阻塞,IC50分別為21.6 和5.1 μM。在人類胚胎腎293細(xì)胞中,Amoxapine選擇性抑制GLYT2a,抑制效果比同種型GLYT1b高出10倍。Amoxapine阻滯反向頻變,并引起向左移位的加速失活。Amoxapine處理使HEK 293細(xì)胞中運(yùn)輸?shù)郊?xì)胞膜表面的hERG緩慢減少,其IC50為15.3 μM。 |
| 存儲(chǔ)條件 | 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.
10% DMSO+90% Saline : 0.81 mg/mL (2.58 mM), Solution.
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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| 關(guān)鍵字 | Inhibitor | inhibit | GlyT2a | GlyT1b | CL67772 | CL 67772 | Amoxapine |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Aceglutamide | Neomycin sulfate | Terbinafine hydrochloride | Hemin | Hydroxychloroquine | Dimethyl sulfoxide | Sodium bicarbonate | Hyaluronic acid sodium (MW 20 kDa) | Sodium diacetate | Sulfamethoxazole sodium | D(+)-Raffinose pentahydrate |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 血腦屏障通透化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 抗菌活性庫(kù) | ReFRAME 相關(guān)化合物庫(kù) | 上市藥物庫(kù) | FDA 上市藥物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 免疫/炎癥分子化合物庫(kù) | 口服活性化合物庫(kù) | 藥物功能重定位化合物庫(kù) |