生物活性 | |||
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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 | |||||
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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 | |||
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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 |
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