Trimipramine maleate 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 maleate 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 (hOCT1、hOCT2) 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 maleate 具有血管活性和抗焦虑作用。
生物活性 | Trimipramine maleate is a5-HT receptorantagonist, withpKibinding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2and 5-HT1A, respectively[1]. Trimipramine maleate 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[2]. Trimipramine maleate has vascular activity and anxiolytic efficacy[3]. |
IC50& Target | 5-HT1CReceptor 6.39 (pKi) | 5-HT2Receptor 8.10 (pKi) | sPLA2 4.66 (pKi) |
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体外研究 (In Vitro) | Trimipramine maleate displays much higher affinity for 5-HT2than for 5-HT1Creceptors[1]. Trimipramine maleate 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 maleate (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells)[2].
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体内研究 (In Vivo) | 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-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). |
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中文名称 | 马来酸三甲丙咪嗪;马来酸曲米帕明;三甲丙咪嗪马来酸盐 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(243.60 mM) H2O : 14.29 mg/mL(34.81 mM;ultrasonic and warming and heat to 60℃) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.4360 mL | 12.1800 mL | 24.3599 mL | 5 mM | 0.4872 mL | 2.4360 mL | 4.8720 mL | 10 mM | 0.2436 mL | 1.2180 mL | 2.4360 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 5.88 mg/mL (14.32 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.09 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.09 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.09 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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