Desipramine hydrochloride |
Catalog No.GC10126 |
El clorhidrato de desipramina es un inhibidor del transportador de noradrenalina (NET), el transportador de 5-HT (SERT) y el transportador de dopamina (DAT) con Kis de 4, 61 y 78.720 nM, respectivamente.
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Cas No.: 58-28-6
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
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]. |
References: [1]. Torres GE, et al. Plasma membrane monoamine transporters: structure, regulation and function. Nat Rev Neurosci. 2003 Jan;4(1):13-25. |
Cas No. | 58-28-6 | SDF | |
Chemical Name | 3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine hydrochloride | ||
Canonical SMILES | CNCCCN1C2=CC=CC=C2CCC3=CC=CC=C13.Cl | ||
Formula | C18H22N2.HCl | M.Wt | 302.84 |
Solubility | ≥ 119.6mg/mL in DMSO | Storage | Store at 2-8°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.3021 mL | 16.5104 mL | 33.0207 mL |
5 mM | 0.6604 mL | 3.3021 mL | 6.6041 mL |
10 mM | 0.3302 mL | 1.651 mL | 3.3021 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >99.00%
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