| 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, administered intraperitoneally (i.p.) at doses of 1, 5, and 10 mg/kg, notably at lower doses, was found to decrease paradoxical sleep and increase slow-wave sleep. Throughout the treatment period, a consistent reduction in paradoxical sleep was observed with Amoxapine (10 mg/kg, i.p.), although tolerance to the inhibition effect of cericlamine was noted in this sleep phase. Additionally, Amoxapine (10 mg/kg/day) did not affect the levels of Substance P, dynorphin, and cholecystokinin, but significantly increased leucine-enkephalin levels in the rat cortex, spinal cord, and hypothalamus. Despite not altering opioid receptor binding in the rat cortex, Amoxapine (10 mg/kg/day, i.p.) increased the density of δ- and μ-opioid receptor binding sites in the spinal cord and decreased it in the hypothalamus. Moreover, Amoxapine attenuated spontaneous activity, induced catalepsy and ptosis, and exhibited inhibitory effects on the dyskinetic movements induced by Apomorphine and stereotypy behaviors induced by amphetamine, through altering avoidance behaviors discerned by monkeys. |
| 体内活性 | In both oocytes and HEK 293 cells, Amoxapine induces acute hERG channel blockade with IC50 values of 21.6 and 5.1 μM, respectively. In human embryonic kidney 293 cells, it selectively inhibits GLYT2a over its isotype GLYT1b by a factor of 10. Amoxapine leads to a blockade of reverse frequency dependence and causes a leftward shift with accelerated inactivation. Treatment with Amoxapine results in a gradual reduction of hERG transport to the cell membrane surface in HEK 293 cells, with an IC50 of 15.3 μM. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 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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| 关键字 | inhibit | Inhibitor | CL 67772 | Amoxapine | CL67772 |
| 相关产品 | Sarcosine | Opiranserin hydrochloride | Iclepertin | Org 25543 hydrochloride | Opiranserin | Bitopertin (R enantiomer) | LY2365109 hydrochloride | Bitopertin | PF-03463275 | ALX-1393 |
| 相关库 | FDA上市及药典收录分子库 | 经典已知活性库 | 神经退行性疾病化合物库 | 神经信号分子库 | 药物功能重定位化合物库 | 血脑屏障通透化合物库 | 抑制剂库 | 抗心血管疾病化合物库 | FDA 上市药物库 | 已知活性化合物库 |
United States
