Desipramine hydrochloride
Desipramine hydrochloride 是去甲肾上腺素转运蛋白 (NET)、5-HT 转运蛋白 (SERT) 和多巴胺转运蛋白 (DAT) 的抑制剂，Kis 分别为 4、61 和 78,720 nM。
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包装价格促销价数量
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50mg￥700.00560.00- +
- 货号: ajci4494
- CAS: 58-28-6
- 别名: 盐酸去甲咪嗪；盐酸地昔帕明
- 分子式: C18H22N2.HCl
- 分子量: 302.84
- 纯度: ＞98%
- 溶解度: ≥ 119.6mg/mL in DMSO
- 储存: Store at 2-8°C
- 库存: 现货
Background
Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with Kis of 4, 61 and 78,720 nM, respectively.
Treatment of rats with Desipramine hydrochloride for 14 days reduces norepinephrine transporter (NET) expression in a dose-dependent manner, as indicated by a reduction of the specific binding of 3H-nisoxetine to the NET in preparations of cerebral cortex (F(3,16)=4.33, p<0.05) and hippocampus (F(3,16)=4.34, p<0.05). This NET down regulation is observed 2 days after discontinuation of chronic Desipramine hydrochloride treatment, a time when plasma and brain concentrations of Desipramine hydrochloride and desmethyldesipramine are undetectable (ie below the 25 ng detection limit of the assay)[2].
参考文献:
[1]. Torres GE, et al. Plasma membrane monoamine transporters: structure, regulation and function. Nat Rev Neurosci. 2003 Jan;4(1):13-25.
[2]. Zhao Z, et al. Norepinephrine transporter regulation mediates the long-term behavioral effects of the antidepressant desipramine. Neuropsychopharmacology. 2008 Dec;33(13):3190-200.
Protocol
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Animal experiment: |
Rats are anesthetized with ketamine (100 mg/kg) and xylazine (10 mg/kg) and implanted subcutaneously with osmotic minipumps preloaded with either vehicle (50% saline, 40% DMSO, and 10% ethanol) or Desipramine hydrochloride at a concentration that delivered 5, 10, or 15 mg/kg per day of the free base. Minipumps are removed, under anesthesia, 14 days later. Rats are tested for antidepressant-like behavior in the forced-swim test 2 to 8 days after pump removal and discontinuation of Desipramine hydrochloride treatment. Following the completion of the behavioral tests, rats are killed by decapitation, their brains are removed, and cerebral cortex and hippocampus are dissected for neurochemical analyses[2]. |
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参考文献: [1]. Torres GE, et al. Plasma membrane monoamine transporters: structure, regulation and function. Nat Rev Neurosci. 2003 Jan;4(1):13-25. |
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