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Trimipramine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Trimipramine图片
CAS NO:739-71-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
曲米帕明
产品介绍
Trimipramine 是5-HT受体的拮抗剂,其对 5-HT1C,5-HT2和 5-HT1A受体的 pKi值分别为 6.39,8.10,4.66。Trimipramine 也是一种靶向人去甲肾上腺素 (hNAT)、血清素 (hSERT) 和有机阳离子转运体 (hOCT1hOCT2) 的有选择性和强效的抑制剂,其IC50值分别为 4.99 μM、2.11 μM、3.72 μM、8.00 μM。Trimipramine 具有血管活性和抗焦虑作用。
生物活性

Trimipramine is a5-HT receptorantagonist, withpKibinding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1,hOCT2) withIC50values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy[1][2][3].

IC50& Target

5-HT1CReceptor

6.39 (pKi)

5-HT2Receptor

8.10 (pKi)

5-HT1AReceptor

4.66 (pKi)

体外研究
(In Vitro)

Trimipramine displays much higher affinity for 5-HT2than for 5-HT1Creceptors[1].
Trimipramine is a moderate inhibitor of the human NAT and SERT, with the IC50values of 4.99 μM and 2.11 μM, respectively[2].
SERT and NAT could represent a target for the antidepressant effects of trimipramine (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells)[2].

体内研究
(In Vivo)

Trimipramine (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-HT2and striatal DA D2receptors. 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-HT2and DA D2receptors[3].

Animal Model:Male Wistar rats (220-250 g); implanted osmotic minipump subcutaneously in the dorsal thoracic interscapular region[3]
Dosage:5 mg/kg/day
Administration:Delivered by smotic minipump; 14 days
Result:Decreased the number of frontal cortex 5-HT2and striatal DA D2receptors, thus blocked the uptake of 5-HT and dopamine (DA).
Clinical Trial
分子量

294.43

Formula

C20H26N2

CAS 号

739-71-9

中文名称

曲米帕明

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.