Desipramine HCl

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Chemical Structure| 58-28-6 同义名 : 盐酸地昔帕明 ;Desipramine Hydrochloride; Desmethylimipramine; NSC-114901; JB-8181; G-35020; EX-4355; Norimipramine
CAS号 : 58-28-6
货号 : A914953
分子式 : C18H23ClN2
纯度 : 98%
分子量 : 302.84
MDL号 : MFCD00058108
存储条件:

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(346.72 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(330.21 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Desipramine HCl 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[1]. Treatment of rats with 15 mg/kg per day desipramine reduced NET (norepinephrine transporter) expression, measured by (3)H-nisoxetine binding and SDS-PAGE/immunoblotting, in cerebral cortex and hippocampus and reduced the time of immobility in the forced-swim test. The antidepressant-like effect on forced-swim behavior was evident 2 days following discontinuation of desipramine treatment when plasma and brain levels of desipramine and its major metabolite desmethyldesipramine were not detectable[2]. Fewer subjects reported adverse events following treatment with desipramine alone than when receiving desipramine with cinacalcet (33 versus 86%), the most frequent of which (nausea and headache) have been reported for patients treated with either desipramine or cinacalcet[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01179828 Low Back Pain Phase 3 Completed - Switzerland ... 展开 >> Andreas Siegenthaler Dep. of Anesthesiolgy and Pain therapy, Bern University Hospital, Switzerland, 3010 Bern 收起 <<
NCT00704860 Major Depression Phase 4 Completed - Canada, Ontario ... 展开 >> University of Ottawa Institute of Mental Health Research Ottawa, Ontario, Canada, K1Z 7K4 收起 <<
NCT00000241 Substance-Related Disorders Phase 2 Completed - United States, California ... 展开 >> Friends Research Institute Los Angeles, California, United States, 90025 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.51mL

3.30mL

1.65mL

33.02mL

6.60mL

3.30mL

参考文献

[1]Torres GE, Gainetdinov RR, Caron MG. Plasma membrane monoamine transporters: structure, regulation and function. Nat Rev Neurosci. 2003;4(1):13-25

[2]Zhao Z, Baros AM, Zhang HT, et al. Norepinephrine transporter regulation mediates the long-term behavioral effects of the antidepressant desipramine. Neuropsychopharmacology.2008;33(13):3190-3200

[3]Harris RZ, Salfi M, Posvar E, Hoelscher D, Padhi D. Pharmacokinetics of desipramine HCl when administered with cinacalcet HCl. Eur J Clin Pharmacol. 2007;63(2):159-163