Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with K i s of 4, 61 and 78,720 nM, respectively.
性状
Solid
IC50 & Target[1][2]
Ki: 4 nM (NET), 61 nM (SERT), 78720 nM (DAT)
体内研究(In Vivo)
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 H-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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (330.21 mM)H2O : 100 mg/mL (330.21 mM; Need ultrasonic)