| 产品描述: | Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy |
| 靶点: |
5-HT1C Receptor:6.39 (pKi);5-HT2 Receptor:8.10 (pKi);sPLA2:4.66 (pKi);DopamineReceptor;5-HTReceptor;Antibacterial;AdrenergicReceptor;Norepinephrine;HistamineReceptor |
| 体内研究: |
Trimipramine maleate (5 mg/kg/d; 14 d; chronic administration) acts as functions in rats:1. Increasing concentration of regional 5-HT. 5-HT is highest in the frontal cortex and the hippocampus, followed by the olfactory tubercles and the hypothalamus. 2. Decreasing the number of frontal cortex 5-HT2 and striatal DA D2 receptors. 3. Increasing in the brain regional level of monoamines and metabolites. thus indicates a greater synthesis rate for dopamine (DA) and 5-HT coinciding with an adaptive down regulation of 5-HT2 and DA D2 receptors |
| 参考文献: |
1. Jenck F, et al. Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs. Eur J Pharmacol. 1993 Feb 9;231(2):223-9. 2. Haenisch B, et al. Inhibitory potencies of trimipramine and its main metabolites at human monoamine and organic cation transporters. Psychopharmacology (Berl). 2011 Sep. 217(2):289-95. 3. Juorio AV, et al. The effects of chronic trimipramine treatment on biogenic amine metabolism and on dopamine D2, 5-HT2 and tryptamine binding sites in rat brain. Gen Pharmacol. 1990;21(5):759-62. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.436 ml |
12.18 ml |
24.36 ml |
| 5 mM |
0.487 ml |
2.436 ml |
4.872 ml |
| 10 mM |
0.244 ml |
1.218 ml |
2.436 ml |
| 50 mM |
0.049 ml |
0.244 ml |
0.487 ml |
|
| 注意: |
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