| 体内研究: |
Lofepramine (28-45 mg/kg, i.p., 实验前 1 h) 仅降低了用 SKF 525A 预处理的 28 mg/kg 大鼠对这两种药物的摄取,并降低了 45 mg/kg 健康大鼠对 5-HT 和 Noradrenaline 的摄取。 Lofepramine (50 mg /kg, i.p., 前 30 min 在脑室内给予 3H-5-HT (0.75 μCi) 或3H-NA (1.2 μCi) 可有效抑制 Noradrenaline 摄取到两个组分 (P2- 和 S-组分) 中。 Lofepramine (20 mg /kg, i.p., 每日一次, 连续 2 周) 及其去甲基代谢物 DMI (Desipramine) ,DML (Desmethyl Lofepramine) 和 DDMI (Desmethyl Desipramin) 在 OB (嗅球切除) 模型中表现出抗抑郁活性。 |
| 参考文献: |
1. Segawa T, et al. Effect of lofepramine and other antidepressants on the uptake of 5-hydroxytryptamine and noradrenaline into rat brain monoaminergic neurons. J Pharm Pharmacol. 1977 Mar;29(3):139-42. 2. Lancaster SG, et al. Lofepramine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs. 1989 Feb;37(2):123-40. 3. McIntyre RS, et al. The neurogenic compound, NSI-189 phosphate: a novel multi-domain treatment capable of pro-cognitive and antidepressant effects. Expert Opin Investig Drugs. 2017 Jun;26(6):767-770. 4. Kelly JP, et al. An investigation of the antidepressant properties of lofepramine and its desmethylated metabolites in the forced swim and olfactory bulbectomized rat models of depression. Eur Neuropsychopharmacol. 1999 Jan;9(1-2):101-5. |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.387 ml |
11.934 ml |
23.868 ml |
| 5 mM |
0.477 ml |
2.387 ml |
4.774 ml |
| 10 mM |
0.239 ml |
1.193 ml |
2.387 ml |
| 50 mM |
0.048 ml |
0.239 ml |
0.477 ml |
|
| 注意: |
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